Peptide Synthesis Applications

Gain insight into how Protein Technologies' platforms have been applied in research and development related to biomaterials, drug delivery, peptide therapeutics, vaccines and venoms & toxins.

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Therapeutics and Vaccines

Application Notes

Cost-Effective Automated Phosphopeptide Synthesis on the Prelude™ Using Single-Shot™ Deliveries

The use of specially modified amino acids is available for a wide variety of peptide synthesis applications. These modified monomers are frequently extremely expensive and their implementation is limited by these costs.



Multivariable Individual Heating Conditions Tested in Parallel Provide Rapid Process Optimization on Prelude X

The application of heat represents a useful tool to optimize the production of challenging synthetic peptides, and a new technology, induction heating, has been introduced on the Prelude X.


High-throughput parallel synthesis optimization of Glucagon-like Peptide 1 receptor agonists

Poster presented at EPS2018


Synthesis of therapeutic stapled peptides: Fully automated peptide cyclization via olefin metathesis

Poster presented at EPS2018



The Extracellular Surface of the GLP-1 Receptor Is a Molecular Trigger for Biased Agonism Cell.
Wootten D. et al. Cell. 2016 Jun 16; 165(7): 1632-1643.2016

Modular peptide amphiphile micelles improve an antibody-mediated immune response to Group A Streptococcus.
Barrett J.C. et al. ACS Biomater. Sci. Eng.2016

Substoichiometric inhibition of transthyretin misfolding by immune-targeting sparsely populated misfolding intermediates: a potential diagnostic and therapeutic for TTR amyloidoses.
Galant N.J. et al. Scientific Reports, 6, 25080.2016

Two Novel Dermaseptin-Like Antimicrobial Peptides with Anticancer Activities from the Skin Secretion of Pachymedusa dacnicolor.
Shi D. et al. Toxins, 8(5), 144.2016

The frequency of naive and early-activated hapten-specific B cell subsets dictates the efficacy of a therapeutic vaccine against prescription opioid abuse.
Laudenbach M. et al.  Journal of Immunology (Baltimore, Md.?: 1950), 194(12), 5926-5936. 2015

Design and characterization of ebolavirus GP prehairpin intermediate mimics as drug targets.
Clinton T.R. et al. Protein Science: A Publication of the Protein Society, 24(4), 446-463.2015

Peptide Amphiphile Micelles Self-Adjuvant Group A Streptococcal Vaccination.
Trent A. et al. The AAPS Journal, 17(2), 380-388.2015

Structural and antigenic features of the synthetic SF23 peptide corresponding to the receptor binding fragment of diphtheria toxin.
Khrustaleva T.A. et al.  Molecular immunology 63.2 (2015): 235-244.2015

Identification of key residues involved in adrenomedullin binding to the AM1 receptor
Watkins H. et al. British Journal of Pharmacology, 169(1), 143–155.2013

T1BT* structural study of an anti-plasmodial peptide through NMR and molecular dynamics
Topchiy E. et al. Malaria Journal, 12, 104.2013

Development of Potent and Metabolically Stable APJ Ligands with High Therapeutic Potential
Juhl al. ChemMedChem 2016, 11, 2378.2016

The Human Autoantibody Response to Apolipoprotein A-I Is Focused on the C-Terminal Helix: A New Rationale for Diagnosis and Treatment of Cardiovascular Disease?
Pagano S. et al.  PLoS ONE 10(7): e01327802015

Design of a peptide inhibitor of tyrosine kinase 2
Works M.G. et al. Protein Pept Lett. 2014 May;21(5):419-252014

The impact of synthetic analogs of histidine on copper(II) and nickel(II) coordination properties to an albumin-like peptide. Possible leads towards new metallodrugs
Zawisza L. et al. J Inorg Biochem. 2014 Oct;139:1-82014

Immunogenicity Studies of Bivalent Inactivated Virions of EV71/CVA16 Formulated with Submicron Emulsion Systems
Lin C.-W. et al. BioMed Research International Volume 2014 (2014), Article ID 6705062014

Discovery and Characterization of a Potent Interleukin-6 Binding Peptide with Neutralizing Activity In Vivo
Ranganath S. et al. PLoS ONE, 10(11), e0141330.2015

In Vivo Efficacy of Anuran Trypsin Inhibitory Peptides against Staphylococcal Skin Infection and the Impact of Peptide Cyclization
Malik U. et al. Antimicrob Agents Chemother. 2015 Apr;59(4):2113-21.2015

Semienzymatic Cyclization of Disulfide-rich Peptides Using Sortase A
Jia X. et al. J Biol Chem. 2014 Mar 7;289(10):6627-38.2014

Immunogenicity in mice and non-human primates of the Group A Streptococcal J8 peptide vaccine candidate conjugated to CRM197
Caro-Aguilar I. et al. Hum Vaccin Immunother. 2013 Mar;9(3):488-96.2013

Synthesis and characterization of a high-affinity αvβ6-specific ligand for in vitro and in vivo applications.
Shunzi L. et al. Molecular Cancer Therapeutics, 8(5), 1239-1249.2009

Design of Potent and Selective Cathepsin G Inhibitors Based on the Sunflower Trypsin Inhibitor-1 Scaffold
Swedberg J.A. et al. J. Med. Chem. Publication Date (Web): January 3.2017

De-immunized and Functional Therapeutic (DeFT) versions of a long lasting recombinant alpha interferon for antiviral therapy
Mufarrege E.F. et al. Clinical Immunology Volume 176, March 2017, Pages 31–41.2017

DS6: anticandidal, antibiofilm peptide against Candida tropicalis and exhibit synergy with commercial drug
Singh K. et al. Journal of Peptide Science2017

5-LOX in Alzheimer's Disease: Potential Serum Marker and In Vitro Evidences for Rescue of Neurotoxicity by Its Inhibitor YWCS
Shekhar S. et al. Mol Neurobiol (2017). doi:10.1007/s12035-017-0527-1.2017

Selection and structural analysis of the NY25 peptide – A vaccine candidate from hemagglutinin of swine-origin Influenza H1N1
Khrustalev V. V. et al. Microbial Pathogenesis, Volume 125, December 2018, Pages 72-83.2018

Rapid and low-cost multiplex synthesis of chemokine analogs
Paolini-Bertrand M. et al JBC Papers in Press. Published on October 10, 2018 as Manuscript RA118.004370.2018

KS23, a novel peptide derived from adiponectin, inhibits retinal inflammation and downregulates the proportions of Th1 and Th17 cells during experimental autoimmune uveitis
Tian Niu, et al. Journal of Neuroinflammation2020

Synthetic Human ? Defensin-3-C15 Peptide in Endodontics: Potential Therapeutic Agent in Streptococcus gordonii Lipoprotein-Stimulated Human Dental Pulp-Derived Cells
Yeon-Jee Yoo, et al. International Journal of Molecular Sciences2020

A Hybrid Insulin Epitope Maintains High 2D Affinity for Diabetogenic T Cells in the Periphery
Baoyu Liu, et al. Diabetes2020

In vitro leishmanicidal activity of antimicrobial peptide KDEL against Leishmania tarentolae
Lili Cao, et al. Acta Biochimica et Biophysica Sinica2020

Enhancing the Immune Response of a Nicotine Vaccine with Synthetic Small “Non-Natural” Peptides
Le, H.T., et al. Molecules2020

Linear and dendrimeric antiviral peptides: design, chemical synthesis and activity against human respiratory syncytial virus
Kozhikhova, K. et al. Journal of Materials Chemistry B2020

A Novel Anti-Microbial Peptide from Pseudomonas, REDLK Induced Growth Inhibition of Leishmania tarentolae Promastigote In Vitro
Yu, Y. et al. Korean J Parasitol2020

A Novel Anti-Microbial Peptide from Pseudomonas, REDLK Induced Growth Inhibition of Leishmania tarentolae Promastigote In Vitro
Yu, Y. et al. Korean J Parasitol

A Novel Anti-Microbial Peptide from Pseudomonas, REDLK Induced Growth Inhibition of Leishmania tarentolae Promastigote In Vitro
Yu, Y. et al. Korean J Parasitol2020

Oncology peptide therapeutics

Application Notes

Synthesis of [des-Arg7]-Dyn A (1-9)-NH2 peptoid hybrid

Automated solid phase peptide synthesis (SPPS) increases reliability, efficiency, and crude purity for peptides and peptoids.



Flexibility is important for inhibition of the MDM2/p53 protein-protein interaction by cyclic Beta-hairpins
Danelius E. et al. Org. Biomol. Chem., 2016,14, 10386-10393.2016

Serum Stability and Affinity Optimization of an M2 Macrophage-Targeting Peptide (M2pep).
Ngambenjawong C. et al. Theranostics, 6(9), 1403-1414.2016

A Peptide Mimicking a Region in Proliferating Cell Nuclear Antigen Specific to Key Protein Interactions Is Cytotoxic to Breast Cancer.
Smith S. J. et al. Molecular Pharmacology, 87(2), 263-276. 2015

Targeted therapy of colorectal neoplasia with rapamycin in peptide-labeled pegylated octadecyl lithocholate micelles.
Khondee S. et al. Journal of Controlled Release: Official Journal of the Controlled Release Society, 199, 114-121.2015

Targeted bioimaging and photodynamic therapy of cancer cells with an activatable red fluorescent bioprobe.
Hu Fang et al. Analytical chemistry 86.15 (2014): 7987-7995.2014

Simultaneous Inhibition of Key Growth Pathways in Melanoma Cells and Tumor Regression by a Designed Bidentate Constrained Helical Peptide
Dhar A. et al. Biopolymers. 2014 Jul;102(4):344-58.2014

Molecular specialization of breast vasculature: a breast-homing phage-displayed peptide binds to aminopeptidase P in breast vasculature.
Essler M. & Rouslahti E. Proc Natl Acad Sci U S A. 2002 Feb 19;99(4):2252-7.2002

Chemotherapy induces adaptive drug resistance and metastatic potentials via phenotypic CXCR4-expressing cell state transition in ovarian cancer
Lee H.H. et al. PLoS One. 2017 Feb 14;12(2):e0171044.2017

VHH characterization. Comparison of recombinant with chemically synthesized anti‐HER2 VHH
Lucie Hartmann, et al. Protein Science2019

Multiple Synthetic Routes to the Mini-Protein Omomyc and Coiled-coil Domain Truncations
Brown, Z.Z, et al.  J. Org. Chem. Just accepted 2019

Cationic synthetic long peptides-loaded nanogels: An efficient therapeutic vaccine formulation for induction of T-cell responses
Kodalivand, N. et al. Journal of controled release2019

Identification of Key Amino Acids in the Anti-Cancer Activity of CDT Peptide Analogs
Jaylen E. Taylor McNair Scholars Research Journal2020

Venoms and Toxins


Baltikinin: A New Myotropic Tryptophyllin-3 Peptide Isolated from the Skin Secretion of the Purple-Sided Leaf Frog, Phyllomedusa baltea.
Shi D. et al. Toxins, 8(7), 213.2016

AaeAP1 and AaeAP2: Novel Antimicrobial Peptides from the Venom of the Scorpion, Androctonus aeneas: Structural Characterisation, Molecular Cloning of Biosynthetic Precursor-Encoding cDNAs and Engineering of Analogues with Enhanced Antimicrobial and Anticancer Activities.
Du Q. et al. Toxins, 7(2), 219-237. 2015

Mambalgin-1 pain-relieving peptide: stepwise solid-phase synthesis, crystal structure and functional domain for acid-sensing ion channel 1a inhibition
Mourier G. et al. J. Biol. Chem. jbc.M115.702373. doi:10.1074/jbc.M115.702373 2015

Improved Detection of Botulinum Neurotoxin Serotype A by Endopep-MS through Peptide Substrate Modification
Wang D. et al. Analytical Biochemistry, 432(2), 115–123.2013

Comparison of the Catalytic Properties of the Botulinum Neurotoxin subtypes A1 and A5.
Wang D. et al. Biochimica et Biophysica Acta, 1834(12), 2722–2728.2013

High-throughput production of two disulphide-bridge toxins
Upert G. et al. Chem Commun (Camb). 2014 Aug 7;50(61):8408-11.2014

Kv1. 3 channel-blocking immunomodulatory peptides from parasitic worms: implications for autoimmune diseases
Chhabra S. et al. FASEB J. 2014

Vipericidins: a novel family of cathelicidin-related peptides from the venom gland of South American pit vipers.
Falcao C.B. et al. Amino Acids. 2014 Nov;46(11):2561-71.2014

δ-Conotoxins Synthesized Using an Acid-cleavable Solubility Tag Approach Reveal Key Structural Determinants for NaV Subtype Selectivity.
Peigneur S. et al. J Biol Chem. 2014 Dec 19; 289(51): 35341–35350.2014

New α-adrenergic property for synthetic MTβ and CM-3 three-finger fold toxins from black mamba.
Blanchet G. et al. Toxicon. 2013 Dec 1;75:160-7.2013

Peptidomic comparison and characterization of the major components of the venom of the giant ant Dinoponera quadriceps collected in four different areas of Brazil
Cologna C.T. et al. Journal of Proteomics Volume 94, 6 December 2013, Pages 413–422.2013

Inactivation of viruses infecting ectothermic animals by amphibian and piscine antimicrobial peptides.
Chinchar V.G. et al. Virology. 2004 Jun 1;323(2):268-75.2004

Expression, activation, and processing of the recombinant snake venom metalloproteinase, pro-atrolysin E.
Shimokawa K. et al. Arch Biochem Biophys. 1996 Nov 15;335(2):283-94.1996

Analgesic Effects of GpTx-1, PF-04856264 and CNV1014802 in a Mouse Model of NaV1.7-Mediated Pain
Deuis J.R. et al. Toxins 2016, 8(3), 78.2016

Enhanced detection of type C botulinum neurotoxin by the Endopep-MS assay through optimization of peptide substrates.
Wang D. et al. Bioorg Med Chem. 2015 Jul 1;23(13):3667-73.2015

‘Messy’ Processing of χ-conotoxin MrIA Generates Homologues with Reduced hNET Potency
Ziegman R. et al. Mar. Drugs 2019, 17(3), 165.2019

Novel conorfamides from Conus austini venom modulate both nicotinic acetylcholine receptors and acid-sensing ion channels
Jin A.-H. et al. Biochemical Pharmacology, In Press, Accepted Manuscript.2019

Insecticidal spider toxins are high affinity positive allosteric modulators of the nicotinic acetylcholine receptor
Chambers C. et al.  FEBS Lett. Accepted Author Manuscript. 2019

Repurposing the scorpion venom peptide VmCT1 into an active peptide against Gram-negative ESKAPE pathogens
Pedron C.N. et al. Bioorganic Chemistry,Available online 8 June 2019, 103038, In Press, Accepted Manuscript.2019

The effect of lysine substitutions in the biological activities of the scorpion venom peptide VmCT1
Pedron C.N. et al. European Journal of Pharmaceutical Sciences, Available online 7 June 2019. In Press, Accepted Manuscript.2019

Chemical Synthesis, Proper Folding, Nav Channel Selectivity Profile and Analgesic Properties of the Spider Peptide Phlotoxin 1
Nicolas, S. et al. Toxins2019

The wasp venom antimicrobial peptide polybia-CP and its synthetic derivatives display antiplasmodial and anticancer properties
Torres, M. et al. bioengineering & translational medicine2020

Wasp venom peptide as a new antichagasic agent
Albuquerque Freire, K. et al. Toxicon2020



Multifunctional thermoresponsive designer peptide hydrogels.
De Leon-Rodriguez L.M. et al. Acta Biomaterialia Volume 47, 1 January 2017, Pages 40–49.2016

Biocompatibility and Characterization of a Peptide Amphiphile Hydrogel for Applications in Peripheral Nerve Regeneration.
Black K.A. et al. Tissue Engineering. Part A, 21(7-8), 1333-1342. 2015

Protease degradable electrospun fibrous hydrogels.
Wade R. J. et al.  Nature Communications, 6, 6639. 2015

A peptide from human semenogelin I self-assembles into a pH-responsive hydrogel.
Frohm B. et al.  Soft matter 11.2 (2015): 414-421.2015

Photoresponsive elastic properties of azobenzene-containing poly(ethylene-glycol)-based hydrogels.
Rosales A. M. et al. Biomacromolecules, 16(3), 798-806.2015

Development of a cellularly degradable PEG hydrogel to promote articular cartilage extracellular matrix deposition.
Sridhar B. V. et al. Advanced Healthcare Materials, 4(5), 702-713.2015

Design of thiol-ene photoclick hydrogels using facile techniques for cell culture applications
Sawicki L. A. et al. Biomaterials Science, 2(11), 1612-1626.2014

Inhibition of atherosclerosis-promoting microRNAs via targeted polyelectrolyte complex micelles.
Kuo C.-H. et al. Journal of Materials Chemistry. B, Materials for Biology and Medicine, 2(46), 8142-8153.2014

Design and characterization of a synthetically accessible, photodegradable hydrogel for user-directed formation of neural networks.
McKinnon D. D. et al. Biomacromolecules 15.7 (2014): 2808-2816.2014

A peptide functionalized poly(ethylene glycol) (PEG) hydrogel for investigating the influence of biochemical and biophysical matrix properties on tumor cell migration.
Singh S. P. et al. Biomaterials Science, 2(7), 1024-1034.2014

Mechanical memory and dosing influence stem cell fate.
Yang C.  Nature Materials, 13(6), 645-652.2014

Measuring cellular forces using bis-aliphatic hydrazone crosslinked stress-relaxing hydrogels.
McKinnon D.D. et al. Soft Matter, 10(46), 9230-9236.2014

Origins of Structural Flexibility in Protein-Based Supramolecular Polymers Revealed by DEER Spectroscopy.
Tavenor N. A. et al. The Journal of Physical Chemistry. B, 118(33), 9881-9889.2014

The Role of Valvular Endothelial Cell Paracrine Signaling and Matrix Elasticity on Valvular Interstitial Cell Activation.
Gould S.T. et al. Biomaterials, 35(11), 3596-3606.2014

Secondary Photocrosslinking of Injectable Shear‐Thinning Dock‐and‐Lock Hydrogels
Lu H.D. et al.  Advanced healthcare materials 2.7 (2013): 1028-1036.2013

Diels–Alder mediated controlled release from a poly (ethylene glycol) based hydrogel.
Koehler K.C. et al. Biomacromolecules 14.2 (2013): 538-547.2013

Role of Cell-Matrix Interactions on VIC Phenotype and Tissue Deposition in 3D PEG Hydrogels.
Gould S.T. and Anseth K.S. Journal of Tissue Engineering and Regenerative Medicine, 10.1002/term.1836.2013

Direct measurement of matrix metalloproteinase activity in 3D cellular microenvironments using a fluorogenic peptide substrate.
Leight J.L. et al. Biomaterials, 34(30), 7344–7352.2013

Three-dimensional hMSC Motility within Peptide-Functionalized PEG-Based Hydrogel of Varying Adhesivity and Crosslinking Density.
Kyburz K.A. & Anseth K.S.  Acta Biomaterialia, 9(5), 6381–6392.2013

Disintegration and cancer immunotherapy efficacy of a squalane-in-water delivery system emulsified by bioresorbable poly (ethylene glycol)-block-polylactide.
Chen W.L. et al. Biomaterials. 2014 Feb;35(5):1686-95.2014

Phosphorylation-dependent mineral-type specificity for apatite-binding peptide sequences
Addison W.N. et al. Biomaterials. 2010 Dec;31(36):9422-30.2010

The adsorption of preferential binding peptides to apatite-based materials.
Segvich S.J. et al. Biomaterials Volume 30, Issue 7, March 2009, Pages 1287–1298.2009

High In Vitro Antibacterial Activity of Pac-525 against Porphyromonas gingivalis Biofilms Cultured on Titanium
Li J. et al BioMed Research International Volume 2015 (2015), Article ID 909870.2015

Self-sorting heterodimeric coiled coil peptides with defined and tuneable self-assembly properties.
Aronsson C. et al. Sci Rep. 2015; 5: 14063.2015

Anchoring a Cytoactive Factor in a Wound Bed Promotes Healing.
Chattopadhyay S. et al. J Tissue Eng Regen Med. 2016 Dec;10(12):1012-1020.2014

A photoclickable peptide microarray platform for facile and rapid screening of 3-D tissue microenvironments
Sharma al. Biomaterials, Volume 143, October 2017, Pages 17-28.2017

Rapid Bioorthogonal Chemistry Enables in Situ Modulation of the Stem Cell Behavior in 3D without External Triggers
Hao Y. et al. ACS Appl. Mater. Interfaces, 2018, 10 (31), pp 26016–26027.2018

Effect of Processing and End Groups on the Crystal Structure of Polypeptoids Studied by Cryogenic Electron Microscopy at Atomic Length Scales
Jiang X. et al. Soft Matter, 2019, Accepted Manuscript.2019

Sorafenib encapsulated in nanocarrier functionalized with glypican-3 specific peptide for targeted therapy of hepatocellular carcinoma
Shuoe Feng, et al. Colloids and Surfaces B: Biointerfaces2019

Peptides from diatoms and grasses harness phosphate ion binding to silica to help regulate biomaterial structure
Adiram-Filiba, N. et al. Acta Biomaterialia2020

Design, characterization and evaluation of ?-hairpin peptide hydrogels as a support for osteoblast cell growth and bovine lactoferrin delivery
De Leon-Rodrigues, L. et al. RSC Advances2020

Design, characterization and evaluation of ?-hairpin peptide hydrogels as a support for osteoblast cell growth and bovine lactoferrin delivery
De Leon-Rodriguez, L. et al. RSC Adv.

Design, characterization and evaluation of ?-hairpin peptide hydrogels as a support for osteoblast cell growth and bovine lactoferrin delivery
De Leon-Rodriguez, L. et al. RSC Adv.2020

Drug delivery


Directing the phase behavior of polyelectrolyte complexes using chiral patterned peptides.
Pacalin N.M. et al. EPJ ST October 2016, Volume 225, Issue 8, pp 1805-1815.2016

Endosomolytic Nano-Polyplex Platform Technology for Cytosolic Peptide Delivery To Inhibit Pathological Vasoconstriction.
Evans B.C. et al. ACS Nano, 9(6), 5893-5907. 2015

Intracellular Delivery System for Antibody Peptide Drug Conjugates.
Berguig G.Y. et al. Molecular Therapy, 23(5), 907-917. 2015

Multivalent display of pendant pro-apoptotic peptides increases cytotoxic activity.
Chu D.S.H. et al. Journal of Controlled Release: Official Journal of the Controlled Release Society, 205, 155-161. 2015

Dual MMP7-Proximity-Activated and Folate Receptor-Targeted Nanoparticles for siRNA Delivery.
Li H. et al.  Biomacromolecules, 16(1), 192-201.2015

Enhanced cellular uptake of short polyarginine peptides through fatty acylation and cyclization.
Oh D et al.  Molecular pharmaceutics 11.8 (2014): 2845-2854.2014

Enhanced efficacy of combination heat shock targeted polymer therapeutics with high intensity focused ultrasound.
Frazier N. et al. Biology and Medicine2016

Enhancing Endosomal Escape for Intracellular Delivery of Macromolecular Biologic Therapeutics
Lönn P. et al. Scientific Reports 6, Article number: 32301 (2016).2016

Re-directing an alkylating agent to mitochondria alters drug target and cell death mechanism.
Mourtada R. et al. PLoS One. 2013 Apr 9;8(4).2013

Evaluation of Doxorubicin-Loaded 3-Helix Micelles as Nanocarriers
Dube N. et al. Biomacromolecules. 2013 Oct 14;14(10):3697-705.2013

Targeted delivery of doxorubicin to mitochondria
Chamberlain G.R. et al. ACS Chem. Biol., 2013, 8 (7), pp 1389–1395.2013

Tuning Liposome Membrane Permeability by Competitive Peptide Dimerization and Partitioning-Folding Interactions Regulated by Proteolytic Activity
Lim S.K. et al. Scientific Reports 6, Article number: 21123 .2016

Optimization of the cyclotide framework to improve cell penetration properties.
Huang Y.-H. et al. Front Pharmacol. 2015; 6: 17.2015

Design of substrate-based BCR-ABL kinase inhibitors using the cyclotide scaffold
Huang Y.-H. et al. Scientific Reports 5, Article number: 12974.2015

A liposomal drug platform overrides peptide ligand targeting to a cancer biomarker, irrespective of ligand affinity or density.
Gray B.P. et al. PLoS One. 2013 Aug 23;8(8):e72938.2013

MRI-visible micellar nanomedicine for targeted drug delivery to lung cancer cells.
Guthi J.S. et al. Mol Pharm. 2010 Feb 1;7(1):32-40.2010

Peptide nanoparticle with pH-sensing cargo solubility enhances cancer drug efficiency
Choi H. et al. Nano Today, Available online 22 March 2017.2017

Self-assembly of Filamentous Cell Penetrating Peptides for Gene Delivery
Xu D. et al. Peptide Self-Assembly. Methods in Molecular Biology, vol 1777. Humana Press, New York, NY.2018

Cisplatin-loaded hollow gold nanoparticles for laser-triggered release
Xiong C. et al. Cancer Nano (2018) 9: 6.2018

Injectable Supramolecular Hydrogel/Microgel Composites for Therapeutic Delivery
Chen M.H. et al. Macromol. Biosci. 2018, 1800248. 2018

Solid-Phase Zincke Reaction for the Synthesis of Peptide-4,4′-bipyridinium Conjugates
Corton, P, et al. Synthesis2019

Cellular uptake and cytosolic delivery of a cyclic cystine knot scaffold
Huawu Yin, et al. ChemRxiv. 2020

Noninvasive Brain Delivery and Efficacy of BDNF to Stimulate Neuroregeneration and Suppression of Disease Relapse in EAE Mice
Brian M. Kopec, et al. Mol. Pharmaceutics2020

General Research

Application Notes

Peptoid Synthesis on the Symphony

Peptides are studied because of their range of biological activities in the body. As receptorbinding molecules, peptides have been investigated for therapeutic uses. Unfortunately, in the body peptides are easily broken down by proteases (enzymes that digest proteins and peptides) and have difficulty crossing cell membranes.


On-Resin Disulfide Bridge Formation

Many naturally occurring peptides contain intradisulfide bridges, which play an important role in biological activities.


Boc Synthesis of a Biotinylated Peptide Thioester on the Prelude™

YIYGSFK is a substrate for the protein tyrosine kinase. Tyrosine kinase activity is increased in several human tumors, so the study of its substrates may lead to a greater understanding of cancer. In this application, a tyrosine kinase substrate was synthesized and modified with a biotinylated lysine and a racemic amino acid thioester on a Prelude peptide synthesizer using Boc chemistry.


Synthesis of a Poly-Alanine Peptide Using Different Deprotection Reagents and the IntelliSynth UV-Monitoring and Feedback Control System on the Tribute™

The IntelliSynth™ UV-monitoring and Feedback Control System is a powerful tool that can be used to determine difficult cycles during a synthesis on the Tribute™ peptide synthesizer. It works by monitoring the extent of Fmoc removal during the deprotection reaction by measuring the concentration of removed Fmoc in the deprotection solution at 301 nm.


Synthesis of 65-74ACP and ABRF Using 4-Methylpiperidine as Deprotectant

In peptide synthesis and peptide library synthesis, piperidine is a common reagent for Fmoc removal. However, piperidine is a controlled substance, which requires special handling.


Fast Synthesis Study – Optimized Fmoc Chemistry Used to Rapidly Synthesize 32-mer C-Peptide in 8.7 Hours

Very fast synthesis times are achievable using optimized Fmoc conditions. Traditional peptide chemistry typically resorts to using extended reaction times to maintain synthesis yields, often resulting in deprotection times of 20-30 minutes and coupling times of an hour or more. It is accepted that speed is gained at the expense of purity.


On-Resin Head-To-Tail Peptide Cyclization on the Prelude

Cyclic peptides have interesting biological properties. They are increasingly being used as drug targets as they often are more metabolically stable and have greater affinity and selectivity to biological receptors than their linear counterparts.


Comparison of Alternative Deprotection Reagents to Piperidine for the Synthesis of a Poly-Alanine Peptide

In peptide synthesis, piperidine is a common agent for Fmoc removal. However, piperidine is a controlled substance which requires special handling and cannot be used in some countries. Therefore, it would be useful to identify alternative deprotection reagents to piperidine for Fmoc removal.


Synthesis of Fluorescently Labeled NDP-?-MSH on the Prelude®

The peptide hormone ?-melanocyte stimulating hormone, or ?-MSH, stimulates melanogenesis and plays a role in appetite, energy balance, and sexual function (1).


On-Resin Head-To-Tail Peptide Cyclization on the Symphony®

Cyclic peptides have interesting biological properties. They are increasingly being used as drug targets as they often are more metabolically stable and have greater affinity and selectivity to biological receptors than their linear counterparts.


Large-Scale Syntheses on the Symphony® and Prelude with No-Foam Beads

PTI has just developed No-Foam beads for large-scale syntheses on the Symphony® and PreludeTM.


Fully Automated Click Cyclization of a Cancer-Targeting Peptide on the Prelude®

The copper-catalyzed azide-alkyne cyclization (CuAAC), the most commonly recognized variant of “click chemistry,” has emerged as a powerful technique for ligation, conjugation, and cyclization reactions of peptides.


Low-Scale Automated Synthesis of a PNA-Peptide Conjugate on the Prelude

Peptide nucleic acid (PNA) is a DNA mimic in which the deoxyribose phosphate backbone is replaced with a neutral pseudopeptide backbone composed of 2-aminoethyl glycine linkages. The four natural nucleobases (adenine, guanine, cytosine and thymine) are retained as side chains.


N- and C-Terminal Biotinylation on the Prelude®

Biotinylation is the process of covalently binding biotin to a protein or other molecule. Due to the specificity and high binding affinity of biotin to the proteins avidin and streptavidin, biotinylation is commonly used in immunoanalytical techniques such as ELISA, ELISPOT and western blots.


Fully Automated Synthesis of a Stapled Peptide on the Prelude®

Cyclization is known to improve the stability, potency, and selectivity of many peptides. One method for peptide cyclization which has generated tremendous interest is the use of olefin metathesis to create “stapled” peptides.


Introduction to Fmoc Solid Phase Peptide Synthesis

Fully Automated Synthesis of Oxopiperazine Helix Mimics on Prelude® X

Download the application note and learn more about how oxopiperazine helix mimics (OHMs) have been successfully prepared using a fully automated method on Prelude X. Application of this method to the synthesis of diversified libraries will accelerate discovery of novel ligands for protein targets.



Comparison of Different Heating Protocols for the Cyclization of Melanotan II on the Prelude X

Heat-assisted synthesis has been shown to reduce the time necessary to produce high-purity linear peptides, and its application to the synthesis of cyclic peptides may provide similar advantages.


Parallel Synthesis and Rapid Heating on the Prelude X

Building upon the strength of the original Prelude platform, the Prelude X adds heating, oscillation shaking, and UV monitoring to deliver uncompromised speed, yield, reagent savings, and flexibility, creating the most complete peptide synthesis solution available.


Rapid synthesis of difficult peptide sequences using parallel heating and UV monitoring on the Prelude® X

Peptides have been recognized as highly selective and generally well tolerated drug candidates, increasing the demand for rapid access to different peptide sequences in order to accelerate the evaluation of potential therapeutics.


Simultaneous optimization of the synthesis of difficult peptides in the Prelude® X automated synthesizer using a novel reagent combination

The coupling reagent COMU has been demonstrated to be highly efficient in the synthesis of a variety of peptides.


Reduced Cycle Times & Solvent Consumption of 65-74ACP on Symphony X

New and optimized methods for rapid peptide synthesis, combined with instruments capable of parallel synthesis enable the production of peptide libraries with high throughput.


Ziconotide: high-throughput process optimization using automated parallel synthesis

The Symphony X™ multiple peptide synthesizer offers the most flexibility and independent protocols of any instrument on the market, making it an ideal platform for high-throughput process development.


Fast and efficient automated, on-resin synthesis of disulfide-bridged type-II diabetes-related peptide amylin

Type-II diabetes, caused by chronic insulin resistance and a progressive decline in pancreatic ?-cell function, affects over 150 million people worldwide [1]. The 37-mer human islet amyloid polypeptide (IAPP) (Figure 1) or amylin, is a major contributor to the amyloid deposits found in the pancreases of patients with typeII diabetes [2,3].


Investigating improved purity, yields of Alzheimer’s disease related peptide: human beta-amyloid (1-42)

Human ?-amyloid (1-42) (Figure 1) is a major component of the plaque deposits found in the brains of patients with Alzheimer’s disease (AD) [1]. b-amyloid is in constant demand for the continued research into the pathology, diagnostic tools, and potential therapeutics for AD.


Efficient synthesis of 84-mer human Parathyroid hormone for the study of osteoporosis and hypoparathyroidism

Human parathyroid hormone (1-84) (PTH) (Figure 1) is produced by the parathyroid glands and regulates calcium and phosphate metabolism. PTH acts on PTHR1 receptors to stimulate bone formation and is used as a treatment for osteoporosis and hypoparathyroidism, a rare deficiency of parathyroid hormone [1,2]


Optimized synthesis of therapeutic MK2 inhibitor cell penetrating peptide: reduction in synthesis time using parallel automated synthesis

Peptide based drug discovery and research is increasingly at the forefront in addressing new therapeutic challenges due to their high target selectivity and potency with low toxicity. Automated solid phase peptide synthesis (SPPS) increases reliability, efficiency and crude purity for peptides in drug discovery and development.


Synthesis of [des-Arg7]-Dynorphin A peptoid analogue: faster methods using parallel automated synthesis and induction heat

Therapeutic Peptides: Synthesis Optimization Using Parallel Automated SPPS

Poster presented at EPS2018



Design, synthesis of allosteric peptide activator for human SIRT1 and its biological evaluation in cellular model of Alzheimer's disease.
Kumar R. et al. European Journal of Medicinal Chemistry, November.2016

Hydrophobic Clusters Raise the Threshold Hydrophilicity for Insertion of Transmembrane Sequences in Vivo.
Stone T.A. et al. Biochemistry, 2016, 55 (40), pp 5772–5779.2016

Effects of Charged Cholesterol Derivatives on Aβ40 Amyloid Formation.
Elbassal E.A. et al. The Journal of Physical Chemistry. B, 120(1), 59-68.2016

Topical Delivery of Protein and Peptide Using Novel Cell Penetrating Peptide IMT-P8.
Gautam A. et al. Scientific Reports, 6, 26278.2016

Sequence, structure, and cooperativity in folding of elementary protein structural motifs.
Lai J.K. et al. Proceedings of the National Academy of Sciences of the United States of America, 112(32), 9890-9895. 2015

An Unprecedented alteration in mode of action of IsCT resulting its translocation into bacterial cytoplasm and inhibition of macromolecular syntheses.
Tripathi J.K. et al. Scientific Reports, 5, 9127. 2015

Identification and Functional Analysis of a Novel Tryptophyllin Peptide from the Skin of the Red-eye Leaf Frog, Agalychnis callidryas.
Wang R. et al. International Journal of Biological Sciences, 11(2), 209-219. 2015

Thermodynamic Switch in Binding of Adhesion/Growth Regulatory Human Galectin-3 to Tumor-Associated TF Antigen (CD176) and MUC1 Glycopeptides.
Rodriguez M.C. et al. Biochemistry, 54(29), 4462-4474. 2015

Phage display-guided nanocarrier targeting to atheroprone vasculature.
Hofmeister L.H. et al.  ACS Nano, 9(4), 4435-4446. 2015

Hydrophobic Blocks Facilitate Lipid Compatibility and Translocon Recognition of Transmembrane Protein Sequences.
Stone T. A. et al. Biochemistry, 54(7), 1465-1473. 2015

Monocyte-Targeting Supramolecular Micellar Assemblies: A Molecular Diagnostic Tool for Atherosclerosis.
Chung E.J. et al. Advanced Healthcare Materials, 4(3), 367-376. 2015

p-Cyanophenylalanine and Selenomethionine Constitute a Useful Fluorophore-Quencher Pair for Short Distance Measurements: Application to Polyproline Peptides.
Mintzer M.R. et al. Physical Chemistry Chemical Physics: PCCP, 17(12), 7881-7887.2015

Calorimetric Investigation of Copper Binding in the N-Terminal Region of the Prion Protein at Low Copper Loading: Evidence for an Entropically Favorable First Binding Event.
Gogineni D.P. et al. Inorganic Chemistry, 54(2), 441-447.2015

Efflux by Small Multidrug Resistance Proteins Is Inhibited by Membrane-interactive Helix-stapled Peptides.
Bellmann-Sickert K. et al.   The Journal of Biological Chemistry, 290(3), 1752-1759.2015

Optimization of peptide substrates for botulinum neurotoxin E improves detection sensitivity in the Endopep-MS assay.
Wang D. et al.  Analytical Biochemistry, 468, 15-21.2015

Synthetic Covalently Linked Dimeric Form of H2 Relaxin Retains Native RXFP1 Activity and Has Improved In Vitro Serum Stability.
Nair V. B. et al. BioMed Research International, 2015, 731852.2015

Cell-Penetrating Ability of Peptide Hormones: Key Role of Glycosaminoglycans Clustering.
Tchoumi Neree A. et al. International Journal of Molecular Sciences, 16(11), 27391-27400.2015

Targeting Bacteria via Iminoboronate Chemistry of Amine-Presenting Lipids.
Bandyopadhyay A. et al. Nature Communications, 6, 6561.2015

Global Shape and Ligand Binding Efficiency of the HIV-1-neutralizing Antibodies Differ from Those of Antibodies That Cannot Neutralize HIV-1.
Solanki A. K. et al. The Journal of Biological Chemistry, 289(50), 34780-34800. 2014

In Situ Synthesis of Peptide Nucleic Acids in Porous Silicon for Drug Delivery and Biosensing.
Beavers K. R. et al. Bioconjugate Chemistry, 25(7), 1192-1197.2014

The Role of Collagen Charge Clusters in the Modulation of Matrix Metalloproteinase Activity.
Lauer J. L. et al. The Journal of Biological Chemistry, 289(4), 1981-1992.2014

Fluorescence Detection of KRAS2 mRNA Hybridization in Lung Cancer Cells with PNA-Peptides Containing an Internal Thiazole Orange.
Sonar M.V. et al. Bioconjugate Chemistry, 25(9), 1697-1708.2014

Ester Carbonyl Vibration as a Sensitive Probe of Protein Local Electric Field.
Pazos I.M. et al. Angewandte Chemie (International Ed. in English), 53(24), 6080-6084.2014

Development of a fluorescence resonance energy transfer assay for monitoring bacterial collagenase triple-helical peptidase activity.
Tokmina-Roszyk, M. et al. Analytical Biochemistry, 453, 61-69.2014

Intersubunit communication in the dihydroorotase?aspartate transcarbamoylase complex of Aquifex aeolicus.
Evans H.G. et al. Protein Science: A Publication of the Protein Society, 23(1), 100-109.2014

Fibrin-binding, peptide amphiphile micelles for targeting glioblastoma.
Chung E.J. et al. Biomaterials, 35(4), 1249-1256.2014

Synthesis and folding of a mirror-image enzyme reveals ambidextrous chaperone activity.
Weinstock M.T. et al. Proceedings of the National Academy of Sciences 111.32 (2014): 11679-11684.2014

Regulation of s-adenosylhomocysteine hydrolase by lysine acetylation.
Wang Y et al.  Journal of Biological Chemistry 289.45 (2014): 31361-31372.2014

Radiolabeled novel peptide for imaging somatostatin-receptor expressing tumor: synthesis and radiobiological evaluation.
De K et al.  Journal of Radioanalytical and Nuclear Chemistry 301.3 (2014): 847-861.2014

Understanding Lipid Recognition by Protein-Mimicking Cyclic Peptides.
Hosseini A. S. et al. Tetrahedron, 70(42), 7632-7638.2014

The N-terminal Domain Allosterically Regulates Cleavage and Activation of the Epithelial Sodium Channel.
Kota P. et al. The Journal of Biological Chemistry, 289(33), 23029-23042.2014

Melittin-grafted HPMA-oligolysine based copolymers for gene delivery
Schellinger J.G. et al. Biomaterials 34.9 (2013): 2318-2326.2013

Synthesis and evaluation of cholecystokinin trimers: A multivalent approach to pancreatic cancer detection and treatment
Brabez N. et al. Bioorganic & Medicinal Chemistry Letters, 23(8), 2422–2425.2013

Enzyme-Free Translation of DNA into Sequence-Defined Synthetic Polymers Structurally Unrelated to Nucleic Acids
Niu J. et al. Nature Chemistry 5, 282–292.2013

Immunosuppression by Co-stimulatory Molecules: Inhibition of CD2-CD48/CD58 Interaction by Peptides from CD2 to Suppress Progression of Collagen-induced Arthritis in Mice.
Gohkale A. et al. Chemical Biology & Drug Design, 82(1), 106–118.2013

Pancreatic Cancer-Associated Cathepsin E as a Drug Activator.
Abd-Elgaliel W.R. et al. J Control Release. 2013 May 10;167(3):221-7.2013

Development of a protease-resistant reporter to quantify BCR–ABL activity in intact cells.
Proctor A. et al. Analyst, 2016, Oct 17;141(21):6008-6017.2016

Kinetic and structural basis for acyl-group selectivity and NAD+-dependence in Sirtuin-catalyzed deacylation
Feldman J.L. et al. Biochemistry, 54(19), 3037–3050.2015

Stability of an amphipathic helix-hairpin surfactant peptide in liposomes
Waring A.J. et al. Biochimica et Biophysica Acta (BBA) - Biomembranes Volume 1858, Issue 12, December 2016, Pages 3113–3119.2016

Mechanism of Four de novo designed antimicrobial peptides
Murray B. et al. Biol. Chem. 2016 291: 25706-25715.2016

Binding of Substrates to the Central Pore of the Vps4 ATPase Is Autoinhibited by the Microtubule Interacting and Trafficking (MIT) Domain and Activated by MIT Interacting Motifs (MIMs).
Han H. et al. The Journal of Biological Chemistry, 290(21), 13490–13499.2015

K Domain CR9 of Low Density Lipoprotein (LDL) Receptor-related Protein 1 (LRP1) Is Critical for Aggregated LDL-induced Foam Cell Formation from Human Vascular Smooth Muscle Cells
Costales P. et al. The Journal of Biological Chemistry, 290(24), 14852–14865.2015

KINATEST-ID: a pipeline to develop phosphorylation-dependent terbium sensitizing kinase assays.
Lipchik A.M. et al. Journal of the American Chemical Society, 137(7), 2484–2494.2015

Intrinsic site-selectivity of ubiquitin dimer formation.
Andersen K.A. et al. Protein Sci. 2015 Feb; 24(2): 182–189.2015

Cellular Uptake and Localization of Polymyxins in Renal Tubular Cells Using Rationally Designed Fluorescent Probes
Yun B. et al. Antimicrob Agents Chemother. 2015 Dec; 59(12): 7489–7496.2015

Structural Modifications of Mitochondria-Targeted Chlorambucil Alter Cell Death Mechanism but Preserve MDR Evasion.
Jean S.R. et al. Mol Pharm. 2014 Aug 4;11(8):2675-82.2014

Progression of Relapsing-Remitting Demyelinating Disease Does Not Require Increased TCR Affinity or Epitope Spread
Kersh A.E. et al. The Journal of Immunology November 1, 2014 vol. 193 no. 9 4429-4438.2014

A PWWP Domain-Containing Protein Targets the NuA3 Acetyltransferase Complex via Histone H3 Lysine 36 trimethylation to Coordinate Transcriptional Elongation at Coding Regions.
Gilbert T.M. et al. Mol Cell Proteomics. 2014 Nov; 13(11): 2883–2895.2014

Grape and Wine Sensory Attributes Correlate with Pattern-Based Discrimination of Cabernet Sauvignon Wines by a Peptidic Sensor Array.
Umali A.P. et al. Tetrahedron, Volume 71, Issue 20, 20 May 2015, Pages 3095–3099.2014

Electrophoretic study of peptide‐mediated quantum dot‐human immunoglobulin bioconjugation
Janu L. et al. Electrophoresis. 2013 Sep;34(18):2725-32.2013

Multiplexed MRM‐based quantitation of candidate cancer biomarker proteins in undepleted and non‐enriched human plasma.
Percy A.J. et al. Proteomics. 2013 Jul;13(14):2202-15.2013

Sequence-specific Ni (II)-dependent peptide bond hydrolysis for protein engineering: Active sequence optimization
Protas A.M. et al. J Inorg Biochem. 2013 Oct;127:99-106.2013

Selective control of Cu (II) complex stability in histidine peptides by β-alanine.
Nagaj J. et al. J Inorg Biochem. 2013 Feb;119:85-9.2013

Optimized templates for bottom-up growth of high-performance integrated biomolecular detectors
Lam B. et al. Lab Chip, 2013,13, 2569-2575.2013

Tuning the Bacterial Detection Sensitivity of Nanostructured Microelectrodes.
Das J. & Kelley S.O. Anal. Chem., 2013, 85 (15), pp 7333–7338.2013

Tethered Spectroscopic Probes Estimate Dynamic Distances with Subnanometer Resolution in Voltage-Dependent Potassium Channels.
Jarecki B.W. et al. Biophys J. 2013 Dec 17; 105(12): 2724–2732.2013

Time-resolved luminescence detection of spleen tyrosine kinase activity through terbium sensitization
Lipchik A.M. & Parker L.L. Anal Chem. 2013 Mar 5; 85(5): 2582–2588.2013

A Multiple Reaction Monitoring (MRM) Method to Detect Bcr-Abl Kinase Activity in CML Using a Peptide Biosensor
Yang T.Y. et al PLoS One. 2013;8(2):e56627.2013

Activity Assay of Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitors in Triple-Negative Breast Cancer Cells Using Peptide-Conjugated Magnetic Beads
Ghosh G. et al. Assay Drug Dev Technol. 2013 Feb;11(1):44-51.2013

Development and evaluation of an immuno-MALDI (iMALDI) assay for angiotensin I and the diagnosis of secondary hypertension
Camenzind A.G. et al. Clin Proteomics. 2013 Dec 20;10(1):20.2013

Improved design and screening of high bioactivity peptides for drug discovery
Giguère S. et al. arXiv:1311.3573v3 [q-bio.QM].2013

Proximal bacterial lysis and detection in nanoliter wells using electrochemistry
Besant J.D. et al. ACS Nano, 2013, 7 (9), pp 8183–8189.2013

Reversible blocking of antibodies using bivalent peptide–DNA conjugates allows protease-activatable targeting
Janssen B.M. et al. Chem. Sci., 2013,4, 1442-1450.2013

N‐Terminal pyroglutamate formation of Aβ38 and Aβ40 enforces oligomer formation and potency to disrupt hippocampal long‐term potentiatio
Schlenzig D. et al. J Neurochem. 2012 Jun;121(5):774-84.2012

Pyroglutamate formation influences solubility and amyloidogenicity of amyloid peptides
Schlenzig D. et al. Biochemistry. 2009 Jul 28;48(29):7072-8.2009

Polymerase Chain Reaction and Immunoassay− Matrix Assisted Laser Desorption Mass Spectrometry Using Tag-Mass Technology: New Tools to Break Down Quantification Limits and Multiplexes.
Stauber J. et al. Anal. Chem., 2009, 81 (22), pp 9512–9521.2009

The Trp cage motif as a scaffold for the display of a randomized peptide library on bacteriophage T7
Herman R.E. J Biol Chem. 2007 Mar 30;282(13):9813-24.2007

On the seeding and oligomerization of pGlu-amyloid peptides (in vitro)
Schilling S. et al. Biochemistry. 2006 Oct 17;45(41):12393-9.2006

Plasticity in the positive selection of T cells: affinity of the selecting antigen and IL-7 affect T cell responsiveness
Rubin R.L. & Hermanson T.M. Int Immunol. 2005 Jul;17(7):959-71.2005

tBid interaction with cardiolipin primarily orchestrates mitochondrial dysfunctions and subsequently activates Bax and Bak.
Gonzalvez F. et al. Cell Death Differ. 2005 Jun;12(6):614-26.2005

Activation of naive CD4 T cells by anti-CD3 reveals an important role for Fyn in Lck-mediated signaling
Sugie K. et al. Proc Natl Acad Sci U S A. 2004 Oct 12; 101(41): 14859–14864.2004

Distinct Recognition of OX1 and OX2 Receptors by Orexin Peptides
Ammoun S. et al. J Pharmacol Exp Ther. 2003 May;305(2):507-14.2003

Efficient internalization of the polo-box of polo-like kinase 1 fused to an Antennapedia peptide results in inhibition of cancer cell proliferation.
Yuan J. et al. Cancer Res. 2002 Aug 1;62(15):4186-90.2002

CD28 plays a critical role in the segregation of PKCθ within the immunologic synapse.
Huang J. et al. Proc Natl Acad Sci U S A. 2002 Jul 9; 99(14): 9369–9373.2002

T-cell receptor antagonists induce Vav phosphorylation by selective activation of Fyn kinase
Huang J. et al. Proc Natl Acad Sci U S A. 2000 Sep 26;97(20):10923-9.2000

Oxidation-reduction properties of disulfide-containing proteins of the Rhodobacter capsulatus cytochrome c biogenesis system
Setterdal A.T. et al. Biochemistry. 2000 Aug 22;39(33):10172-6.2000

Polar Hinges as Functionalized Conformational Constraints in (Bi)cyclic Peptides
Liskamp R.M.J. et al. ChemBioChem. Accepted Author Manuscript. doi:10.1002/cbic.201600612.2016

Singlet-singlet and triplet-triplet energy transfer in bichromophoric peptides
McGimpsey W.G. et al. J. Phys. Chem. A, 1999, 103 (31), pp 6082–6090.1999

Evidence for a neurotensin receptor in rat serosal mast cells.
Feldberg R.S. et al. Inflamm Res. 1998 Jun;47(6):245-50.1998

Sialic acid-modified antigens impose tolerance via inhibition of T-cell proliferation and de novo induction of regulatory T cells.
Perdicchio M. et al. Proc Natl Acad Sci U S A. 2016 Mar 22;113(12):3329-34.2016

Activity and biophysical inhibition resistance of a novel synthetic lung surfactant containing Super-Mini-B DATK peptide.
Notter R.H. et al. PeerJ, 4, e1528.2016

Avibirnavirus VP4 Protein Is a Phosphoprotein and Partially Contributes to the Cleavage of Intermediate Precursor VP4-VP3 Polyprotein.
Wang S. et al. PLoS ONE, 10(6), e0128828.2015

Dosimetry of [177Lu]-DO3A-VS-Cys40-Exendin-4 – impact on the feasibility of insulinoma internal radiotherapy.
Velikyan I. et al. Am J Nucl Med Mol Imaging. 2015 Jan 15;5(2):109-26. 2015

Synthetic lung surfactant reduces alveolar-capillary protein leakage in surfactant-deficient rabbits.
Gupta R. et al. Exp Lung Res. 2015 Jun; 41(5): 293–299.2015

A Cyclic Peptide Mimic of the β-Amyloid Binding Domain on Transthyretin.
Cho P.Y. et al. ACS Chem Neurosci. 2015 May 20;6(5):778-89.2015

Fine specificities of natural regulatory T cells after IVIG therapy in patients with Kawasaki disease
Burns J.C. et al Autoimmunity. 2015 May;48(3):181-8.2015

Synthesis and disaggregation of asparagine repeat‐containing peptides.
Lu X. & Murphy R.M.  J Pept Sci. 2014 Nov;20(11):860-7.2014

Peptide-conjugated glass slides for selective capture and purification of diagnostic cells: Applications in urine cytology.
Wronska D.B. et al. BioTechniques, 2014, 57(2):63-71.2014

Broad-Spectrum Allosteric Inhibition of Herpesvirus Proteases.
Gable J.E. et al. Biochemistry. 2014 Jul 22;53(28):4648-60.2014

Transthyretin-Derived Peptides as β-Amyloid Inhibitor
Cho P.Y. et al. ACS Chem Neurosci. 2014 Jul 16;5(7):542-51. 2014

DNA Nanoparticle-Mediated Thymulin Gene Therapy Prevents Airway Remodeling in Experimental Allergic Asthma
Da Silva A.L. et al. J Control Release. 2014 Apr 28;180:125-33.2014

Evaluation of Nanoparticle Tracking for Characterization of Fibrillar Protein Aggregates.
Yang D.T. et al. AIChE Journal. American Institute of Chemical Engineers, 60(4), 1236–1244.2014

Lung Gene Therapy with Highly Compacted DNA Nanoparticles that Overcome the Mucus Barrier.
Suk J.S. et al. J Control Release. 2014 Mar 28;178:8-17.2014

Highly compacted pH-responsive DNA nanoparticles mediate transgene silencing in experimental glioma.
Kim A.J. et al. J. Mater. Chem. B, 2014,2, 8165-8173.2014

Sensitive and Selective Plasmon Ruler Nanosensors for Monitoring the Apoptotic Drug Response in Leukemia.
Tajon C.A. et al. ACS Nano. 2014 Sep 23;8(9):9199-208.2014

From phage display to nanoparticle delivery: functionalizing liposomes with multivalent peptides improves targeting to a cancer biomarker.
Gray B.P., Li S. & Brown K.C. Bioconjug Chem. 2013 Jan 16;24(1):85-96. 2013

Peptide microarrays to interrogate the “histone code”
Rothbart S.B. et al. Methods Enzymol. 2012;512:107-35.2012

Generating Orally-Active Galanin Analogs with Analgesic Activities.
Robertson C.R. et al. ChemMedChem. 2012 May;7(5):903-9.2012

). Detection of β-amyloid peptide (1–16) and amyloid precursor protein (APP770) using spectroscopic ellipsometry and QCM techniques: A step forward towards Alzheimers disease diagnostics.
Mustafa M.K. et al. Biosens Bioelectron. 2010 Dec 15;26(4):1332-6.2010

A novel strategy for surface modification of superparamagnetic iron oxide nanoparticles for lung cancer imaging.
Huang G. etal J Mater Chem. 2009;19:6367-6372.2009

Biopanning of phage displayed peptide libraries for the isolation of cell-specific ligands.
McGuire M.J. et al. Methods Mol Biol. 2009;504:291-321.2009

Glycosylated neurotensin analogues exhibit sub-picomolar anticonvulsant potency in a pharmacoresistant model of epilepsy
Lee H.K. et al ChemMedChem. 2009 Mar;4(3):400-5.2009

Porcine β-defensin 2 displays broad antimicrobial activity against pathogenic intestinal bacteria.
Veldhuizen E.J. et al. Molecular immunology, 45(2), 386-394.2008

The different effects of structurally related sulfakinins on Drosophila melanogaster odor preference and locomotion suggest involvement of distinct mechanisms.
Nichols R. et al. Peptides. 2008 Dec; 29(12): 2128–2135.2008

A Combinatorial H4 Tail Library for Exploring the Histone Code.
Garske A.L. et al. Biochemistry. 2008 Aug 5; 47(31): 8094–8102.2008

Label-free, Water-soluble Fluorescent Peptide Probe for a Sensitive and Selective Determination of Copper Ions
Yang T. et al. Analytical Sciences, February 2017, Vol. 33.2017

Sperm gamma-aminobutyric acid type A receptor delta subunit (GABRD) and its interaction with purinergic P2X2 receptors in progesterone-induced acrosome reaction and male fertility
Wenming X. et al. Reproduction, Fertility and Development.Published online: 13 February 2017.2017

Emerging structural details of transient Amyloid-β oligomers suggest designs for effective small molecule modulators
Chandra B. et al. Chemical Physics Letters Available online 22 February 2017.2017

Bacterial Detection Using Peptide-Based Platform and Impedance Spectroscopy
Etayash H., Thundat T. & Kaur K. Protocol, Biosensors and Biodetection, Volume 1572 of the series Methods in Molecular Biology, pp 113-124.2017

A Structural and Functional Analogue of a Bowman Birk-type Protease Inhibitor from Odorrana Schmackeri
Wu Y. et al. Bioscience Reports, Accepted manuscript, DOI 10.1042/BSR20160593.2017

Epitopes rationally selected through computational analyses induce T-cell proliferation in mice and are recognized by serum from individuals infected with Schistosoma mansoni
Lopez M.D. et al. Biotechnol Progress. Accepted Author Manuscript. doi:10.1002/btpr.2463.2017

Matrix metalloproteinase processing of PTHrP yields a selective regulator of osteogenesis, PTHrP1–17
Frieling J.S. et al. Oncogene , (3 April 2017) | doi:10.1038/onc.2017.70.2017

An engineered cyclic peptide alleviates symptoms of inflammation in a murine model of inflammatory bowel disease
Cobos Caceres C. et al. Journal of Biological Chemistry,doi: 10.1074/jbc.M117.779215 jbc.M117.779215.2017

Antibacterial and Antibiofilm Activities of a Novel Synthetic Cyclic Lipopeptide Against Cariogenic Streptococcus mutans UA159
Min K.R. et al. Antimicrobial Agents and Chemotherapy, June 2017.2017

Measuring O-GlcNAc cleavage by OGA and cell lysates on a peptide microarray
Sharif S. et al. Analytical Biochemistry.Available online 29 May 2017.2017

Intracellular delivery of a catalytic organometallic complex
Indrigo E. et al. Chem. Commun., 2017, Advance Article.2017

Halogen Bonding: A Powerful Tool for Modulation of Peptide Conformation
Danelius E. et al. Biochemistry, Article ASAP DOI: 10.1021/acs.biochem.7b00429 Publication Date (Web): June 5, 2017.2017

Peptide Microarray Analysis of the Cross-talk Between O-GlcNAcylation and Tyrosine Phosphorylation
Shi J. et al. FEBS letters 2017.2017

Tunable Surface Repellency Maintains Stemness and Redox Capacity of Human Mesenchymal Stem Cells
Balikov B.A. et al. ACS Appl. Mater. Interfaces, Just Accepted Manuscript DOI: 10.1021/acsami.7b06103.2017

The N-terminus of hepcidin is a strong and potentially biologically relevant Cu(II) chelator
Plonka D. & Bal W. Inorganica Chimica Acta, 2017.2017

Lytic cell death induced by melittin bypasses pyroptosis but induces NLRP3 inflammasome activation and IL-1β release
Martín-Sánchez F. et al. Cell Death and Disease (2017) 8, e2984; doi:10.1038/cddis.2017.390; published online 10 August 2017.2017

Insights into Onchocerca volvulus population biology through multilocus immunophenotyping.
Norice-Tra C.T. et al. The Journal of Infectious Diseases,jix394.2017

Specific Histidine Residues Confer Histatin Peptides with Copper-Dependent Activity against Candida albicans
Conklin S.E. et al. Biochemistry, 2017, 56 (32), pp 4244–4255.2017

Peptide GC31 inhibits chemokines and ICAM-1 expression in corneal fibroblasts exposed to LPS or poly(I:C) by blocking the NF-κB and MAPK pathways
Zhu S. et al. Experimental Eye Research, Available online 2 August 2017.2017

Gold Nanoparticles as a Probe for Amyloid-β Oligomer and Amyloid Formation
Elbassal E.A. et al. J. Phys. Chem. C, Just Accepted Manuscript DOI: 10.1021/acs.jpcc.7b05169.2017

Evolution of mechanics in α-helical peptide conjugated linear- and star-block PEG
O'Neill S.C. et al. Soft Matter, 2017, Accepted Manuscript. DOI:10.1039/C7SM00968B.2017

Protein mimetic properties of monocyte-targeting peptide amphiphile micelles
Poon C. et al. ACS Biomater. Sci. Eng., Just Accepted Manuscript DOI: 10.1021/acsbiomaterials.7b00600.2017

Influence of hydrocarbon-stapling on membrane interactions of synthetic antimicrobial peptides
Stone T.A. et al. Bioorganic & Medicinal Chemistry, Available online 21 October 2017.2017

FRET Analysis of the Promiscuous yet Specific Interactions of the HIV-1 Vpu Transmembrane Domain
Cole G.B. et al. Biophysical Journal , Volume 113 , Issue 9 , 1992 - 2003.2017

Design, Synthesis and Biological Evaluation of 68Ga-DOTA-PA1 for Lung Cancer: A Novel PET Tracer for Multiple Somatostatin Receptors Imaging
Liu F. et al. Mol Pharm. 2017 Dec 27. doi: 10.1021/acs.molpharmaceut.7b00963. Epub ahead of print.2017

Identification and validation of FGFR2 peptide for detection of early Barrett's neoplasia
Zhou J. et al. Oncotarget. 2017 Oct 20; 8(50): 87095–87106.2017

An MD2-derived peptide promotes LPS aggregation, facilitates its internalization in THP-1 cells, and inhibits LPS-induced pro-inflammatory responses
Tandon A., Harioudh M., Ishrat N. et al. Cell. Mol. Life Sci. (2018).2018

Effects of Proline-Rich Peptides of the Innate Immune System on Drug-Resistant Bacterial Strains
Zharkova M.S. et al. Medical Immunology (Russia)/ Meditsinskaya Immunologiya 2018, Vol. 20, 1, pp. 107-114.2018

An MRM-Based Cytokeratin Marker Assay as a Tool for Cancer Studies: Application to Lung-Cancer Pleural Effusions
Perzanowska A. et al.  Prot. Clin. Appl., 1700084. Accepted Author Manuscript. doi:10.1002/prca.201700084.2018

Elucidation of the binding mode of the carboxyterminal region of peptide YY to the human Y2 receptor
Xu B. et al. Molecular Pharmacology January 24, 2018, mol.117.110627; DOI:

Development of a solid-phase traceless-Ugi multicomponent reaction for backbone anchoring and cyclic peptide synthesis
Jobin S., Beaumont C. & Biron E. Peptide Science, 2475-8817.DOI: 10.1002/pep2.24044.2018

Monoclonal antibody against the universal M2 epitope of influenza A virus
Feng M. et al. Appl Microbiol Biotechnol (2018)2018

Relative role(s) of leucine versus isoleucine in the folding of membrane proteins
Deber C.M. & Stone T.A. Peptide Science. 2018;e24075. 2018

Synthesis, antibacterial, and antibiofilm potential of human autophagy 16 polypeptide and analogues
Varnava K.G. et al. Peptide Science. 2018;e24076.2018

Cathelicidin Related Antimicrobial Peptide (CRAMP) Enhances Bone Marrow Cell Retention and Attenuates Cardiac Dysfunction in a Mouse Model of Myocardial Infarction
Klyachkin Y.M. et al. Stem Cell Rev and Rep (2018). 2018

Cyclic Hexapeptide Mimics of the LEDGF Integrase Recognition Loop in Complex with HIV‐1 Integrase
Northfield S. et al. ChemMedChem. Accepted Author Manuscript.2018

Quantification of hydrolyzed peptides and proteins by amino acid fluorescence
Allenspach M.D. et al.  Peptide Science (2018) 110, e3113.2018

Photoaffinity Cross-Linking and Unnatural Amino Acid Mutagenesis Reveal Insights into Calcitonin Gene-Related Peptide Binding to the Calcitonin Receptor-like Receptor/Receptor Activity-Modifying Protein 1 (CLR/RAMP1) Complex
Simms J. et al. iochemistry Article ASAP.2018

A liquid chromatography high-resolution mass spectrometry in vitro assay to assess metabolism at the injection site of subcutaneously administered therapeutic peptides
Esposito S. et al. Journal of Pharmaceutical and Biomedical Analysis Volume 159, 10 September 2018, Pages 449-458.2018

Peptide ligand-based ELISA reagents for antibody detection
Heyduk E. et al. Analytical Biochemistry, Available online 18 August 2018.2018

Lipophilicity prediction of peptides and peptide derivatives by consensus machine learning
Fuchs J-A. et al. Med. Chem. Commun., 2018, Advance Article.2018

Interaction of Insulin-Like Growth Factor-Binding protein 3 With Hyaluronan and Its Regulation by Humanin and CD44
Muterspaugh R. et al. Biochemistry, Just Accepted Manuscript, Publication Date (Web): September 5, 2018.2018

Engineered SH2 domains with tailored specificities and enhanced affinities for phosphoproteome analysis”
Veggiani G. et al. Protein Science. Accepted Author Manuscript.2018

Design of Y2 Receptor Selective and Proteolytically Stable PYY3–36 Analogues
Østergaard S. et al. J. Med. Chem. 2018, 61, 23, 10519-10530.2018

Optimized GIP analogs promote body weight lowering in mice through GIPR agonism not antagonism
Mroz P.A. et al. Molecular Metabolism Available online 5 December.2018

Structure-activity relationships of the bacteriocin bactofencin A and its interaction with bacterial membrane
Bedard F., Fliss I., and Biron E. ACS Infect. Dis., Just Accepted Manuscript,Publication Date (Web): December 12.2018

Combined Antibacterial Effect In Vitro of Human Salivary Prolinerich Peptide P-F (43-61) and Cationic Antimicrobial Peptides
Zharkova M.S. et al. UDC 616-092.19.2018

Aerosol delivery of dry powder synthetic lung surfactant to surfactant-deficient rabbits and preterm lambs on non-invasive respiratory support
Walther F.J. et al. Gates Open Research, (version 1; referees: awaiting peer review)2019

Specific inhibition of DPY30 activity by ASH2L-derived peptides suppresses blood cancer cell growth
Shah K.K. et al. bioRxiv, preprint first posted online Feb. 19.2019

Fluorescent analogues of BeKm-1 with high and specific activity against the hERG channel
Vasseur L. et al. Toxicon X. Available online 23 February 2019, 100010.2019

NMR Characterization of Conformational Fluctuations and Non‐covalent Interactions of SUMO protein from Drosophila melanogaster (dSmt3)
Kaur A. et al.  Proteins. Accepted Author Manuscript. 2019

Hydrophobic matching of HIV-1 Vpu transmembrane helix-helix interactions is optimized for subcellular location
Gregory B.Cole and Simon Sharpe Biochimica et Biophysica Acta (BBA) - Biomembranes2019

Affinity‐triggered assemblies based on a designed peptide‐peptide affinity pair
Claudia S. M. Fernandes et al. Biotechnology Journal2019

Peptide-based efflux pump inhibitors of the small multidrug resistance protein from Pseudomonas aeruginosa
Chloe J Mitchell, et al. Antimicrobial Agents and Chemotherapy2019

The aspartimide problem persists: Fluorenylmethyloxycarbonyl‐solid‐phase peptide synthesis (Fmoc‐SPPS) chain termination due to formation of N‐terminal piperazine‐2,5‐diones
Samson, D et al. Journal of Peptide Science2019

Peptide-based efflux pump inhibitors of the small multidrug resistance protein from Pseudomonas aeruginosa
Chloe J Mitchell, et al. Antimicrobial Agents and Chemotherapy2019

Design of N-Terminal Derivatives from a Novel Dermaseptin Exhibiting Broad-Spectrum Antimicrobial Activity against Isolates from Cystic Fibrosis Patients
Ying, Y, et al. biomolecules2019

Peptide-Assisted Design of Peptoid Sequences: One Small Step in Structure and Distinct Leaps in Functions
Eva Maron, et al. ACS Macro Lett.2020

Multifunctional Nanodelivery Platform for Maximizing Nucleic Acids Combination Therapy
Seung Koo Lee, et al. RNA Interference and CRISPR Technologies2020

Tandem Wittig-Diels Alder diversification of genetically encoded peptide libraries
Vivian Triana, et al. Organic & Biomolecular Chemistry2020

Computational Design of Biologically Active Anticancer Peptides and Their Interactions with Heterogeneous POPC/POPS Lipid Membranes
Maninder Singh, et al. J. Chem. Inf. Model2020

Synthesis and evaluation of zirconium-89 labelled and long-lived GLP-1 receptor agonists for PET imaging
Christian Borch Jacobsen, et al. Nuclear Medicine and Biology2020

A ClpS-based N-terminal amino acid binding reagent with improved thermostability and selectivity
Jennifer Tullman, et al. Biochemical Engineering Journal2020

Synthetic glucocorticoid-induced leucine zipper peptide inhibits lipopolysaccharide-induced ocular inflammation in rats
Guo Y., et al. Ophthalmic Research2020

Proline‐to‐cysteine cyclization for generating conformationally constrained cyclic peptides
Frost, J.R. et al. Peptide Science2020

Development of Novel 111-In-Labelled DOTA Urotensin II Analogues for Targeting the UT Receptor Overexpressed in Solid Tumours
Poret, B. et al. Biomolecules2020

Membrane affinity of individual toxic protein oligomers determined at the single-molecule level
Dey, S. et al. Physical Chemistry Chemical Physics2020

A Spectroscopic Marker for Structural Transitions Associated with Amyloid-? Aggregation
Das, A. et al. Biochemistry2020

Pharmacological activity and NMR solution structure of the leech peptide HSTX-I
McMahon, K. et al. Biochemical Pharmacology

Surface Chemical Functionalization of Wrinkled Thiol–Ene Elastomers for Promoting Cellular Alignment
Ma, S. et al. ACS Appl. Bio Mater.

Peptides from diatoms and grasses harness phosphate ion binding to silica to help regulate biomaterial structure
Adiram-Filiba, N. et al. Acta Biomaterialia

A Spectroscopic Marker for Structural Transitions Associated with Amyloid-? Aggregation
Das, A. et al. Biochemistry

Chain-End Modifications and Sequence Arrangements of Antimicrobial Peptoids for Mediating Activity and Nano-Assembly
Hasan, A. et al. Frontiers in Chemistry

Pharmacological activity and NMR solution structure of the leech peptide HSTX-I
McMahon, K. et al. Biochemical Pharmacology2020

Surface Chemical Functionalization of Wrinkled Thiol–Ene Elastomers for Promoting Cellular Alignment
Ma, S. et al. ACS Appl. Bio Mater.2020

Peptides from diatoms and grasses harness phosphate ion binding to silica to help regulate biomaterial structure
Adiram-Filiba, N. et al. Acta Biomaterialia2020

A Spectroscopic Marker for Structural Transitions Associated with Amyloid-? Aggregation
Das, A. et al. Biochemistry2020

Chain-End Modifications and Sequence Arrangements of Antimicrobial Peptoids for Mediating Activity and Nano-Assembly
Hasan, A. et al. Frontiers in Chemistry2020