The use of parallel peptide synthesizers in the manufacture of long and complex peptides and high throughput manufacture
Recorded Webinar from June 2, 2020. TIDES Digital Week
Reliance on Solid Phase Peptide Synthesis has increased dramatically over the decades to keep pace with the rise in the use of peptides in diagnostic and therapeutic research. In parallel, approaches to automated synthesis have evolved in order to be compatible with a diverse range of coupling chemistries, reaction conditions and synthesis monitoring. Automated peptide synthesises must be reliable, robust, fast, and easy to use.
Almac as a peptide CMO, has used parallel synthesisers for more than 15 years. In that time, we have developed methodology to manufacture very long and complex peptides, and we will present some examples in this filed. More recently, we have applied automated parallel synthesisers in a GMP setting in the manufacture of clinical grade peptides for use in vaccine products.
Alastair Hay, Account Manager
Peptides, Almac Group Ltd.
SPPS Tips for Success: Strategies for Minimizing Side-Reactions
Recorded Webinar from May 26, 2020
As peptide chemists strive to achieve new methods and techniques for solid phase peptide synthesis (SPPS), strategies must also be implemented to help reduce the occurrence of unwanted side reactions that inevitability take place during the chemical synthesis process. Attend this free webinar to learn how to implement preventative measures to help reduce or eliminate unwanted side products from forming.
Lukasz Frankiewicz PhD, Senior Product Specialist
Gyros Protein Technologies
Venom Peptides: Rethinking Voltage-Gated Sodium Channel Inhibition
Recorded Webinar from May 22, 2020
In this webinar, delineating the mechanism of action behind venom peptide inhibition of voltage-gated sodium channels will be presented. This will include discussion on engineering peptides to achieve subtype specificity and complete inhibition of specific sodium channels to unlock the potential of potent venom peptides as therapeutic leads for the treatment of pain.
Christina I. Schroeder, Stadtman Investigator,
National Cancer Institute, National Institutes of Health
Recorded Webinar from May 5, 2020
With the increasing chemical complexity of therapeutic peptides, how can you maximize the likelihood of success when developing a solid phase synthesis protocol to automate synthesis for a new peptide sequence? View this webinar to learn how to design SPPS synthesis protocols, analyze sequences and understand which factors influence decisions such as resin selection, choice of chemistry and coupling protocol.
Cyf Ramos-Colon PhD
Gyros Protein Technologies
Sequence-Specific “Peptoids” for Antifouling, Antibacterial and Self-Assembly Applications
Recorded Webinar from November 15, 2019
In this webinar, sponsored in partnership with Xtalks K.H Aron Lau will highlight recent efforts in exploring solid-phase synthesized peptoids for applications beyond their conventional use in combinatorial drug discovery.
K.H Aaron Lau, PhD
Senior Lecturer (Associate Professor),
Department of Pure and Applied Chemistry,
University of Strathclyde, Glasgow, Scotland, United Kingdom
Sustainability Considerations in Peptide Chemistry
Recorded Webinar from August 22, 2019
In this webinar, sponsored in partnership with Xtalks, Craig Jamieson will discuss current efforts in the peptide chemistry community towards pursuing more sustainable replacement solvents for peptide synthesis, as well as other considerations such as coupling chemistry.
Craig Jamieson, PhD
University of Strathclyde, Glasgow, UK
Innovation vs Application: Maximizing Efficiency in Peptide Drug Discovery from a Chemistry Perspective
Recorded Webinar from May 16, 2019
This presentation will discuss the discovery process used in the development and selection of a Glucagon agonist, including SAR studies and the positive impacts of integrating innovative technology. Faced with limited time and resources, flexible instrumentation has been used to efficiently incorporate molecular improvements that are critical for overcoming the inherent challenges of peptide drug discovery, including optimizing physical properties and receptor selectivity.
William Blackwell III,
Investigator, Intarcia Therapeutics
James Cain, Ph.D.,
Global Product Manager, Gyros Protein Technologies
Challenging SPPS: Difficult sequences and side reactions
Recorded Webinar from April 4, 2019
Peptide therapeutics have seen increased interest in the last decade, making peptide synthesis a critical step in the drug discovery and development process. One of the major drawbacks in peptide synthesis is that success largely depends on the peptide sequence being synthesized, so what do you do when you have a sequence with failed couplings at certain cycles? Do you extend the coupling time? Change reagents? Do multiple couplings? Here we’ll discuss our take on these questions using fast parallel synthesis optimization of a sterically hindered model peptide, Aib-ACP (VQ-Aib-Aib-IDYING-NH2) which saw improvements from 7.8% using HCTU to 91% using COMU and increasing the reaction temperature to 75 °C with short reaction times (2 x 3 min). What if your synthesis challenges aren’t difficult couplings but side reactions? We’ll discuss strategies for minimizing their occurrence during fast SPPS.
Cyf Ramos-Colón, Ph.D., Senior Scientist, Gyros Protein Technologies
Polar Hinges as Functionalized Conformational Constraints in (Bi)cyclic Peptides
Redorded webinar from November 8, 2018
Dr Alex Hoose
Post-Doctoral Research Associate
University of Glasgow
Strategies to Increase Robustness in the Optimization and CMC Production of Peptide Therapeutics with Parallel Peptide Synthesis
Recorded Webcast from TIDES 2018 Digital Week
With the advancement of personalized medicine and newer disease targets, peptide therapeutic development has greatly expanded. Its potential to achieve increased receptor specificity and decreased toxicity satisfies efficacy and safety regulatory requirements. Technology advances in automated SPPS enable screening and CMC production of peptides with greater structural complexity allows for the design of more physiologically stable products with increased target specificity and membrane permeability. Structural modification strategies for peptide lead optimization can include cyclization, stapling, and PEGylation, which can be difficult to synthesize and purify, requiring more efficient synthesis protocols and automation to ensure reproducible and efficient manufacturability.
Here we describe the process development and parallel optimization of SPPS relating to different biologically relevant peptides. Solid-support screening, reagent screening and temperature screening are demonstrated using an automated peptide synthesizer as part of the optimization process for difficult peptides such as Aib-Enkephalin (90% optimized crude purity vs 21% crude purity) and JR 10-mer (67% optimized crude purity vs 21% crude purity). In addition, the synthesis optimization in parallel of GLP-1 related peptides and dual GLP-1/glucagon receptor agonists will be shown, testing multiple resins and coupling reagents in search of optimal crude purities that may translate into ease of purification during the manufacturing process. Finally, the fully automated synthesis, from linear, on-resin cyclization, and resin cleavage, of NYAD-1 stapled peptide will be shared.
James Cain, Global Product Manager, Gyros Protein Technologies
Strategies for efficient, high throughput optimization of biopolymers and mimetic compounds
Peptide, peptidomimetic and oligonucleotide therapeutics are increasingly at the forefront of drug development programs for personalized medicine, cancer therapeutics, and genetic diseases among others. This has driven the search for faster and more efficient solid phase synthesis (SPS) protocols, making method development crucial in the discovery process towards scale-up. Automated synthesizers are part of the SPS toolbox that allows simultaneous optimization and high-throughput synthesis via parallel synthesis.
In this webinar, we describe the process development and parallel optimization of SPS of different biologically relevant compounds. Solid-support screening and reagent screening are demonstrated using automated peptide synthesis as part of the optimization process for peptide nucleic acids (PNA), peptoids, and cyclic peptides. For example, parallel synthesis condition scanning for the synthesis of SK-8mer PNA analog, H-Lys-AGTGGATC-Lys-NH2, led to an increase of 27% crude purity resulting in high purity product (73% crude pure) for biological analysis. Coupling reagents, resins and reaction time combinations for increased crude purity results will be discussed for biopolymers and mimetic compounds.
James Cain, Global Product Manager, Gyros Protein Technologies
Cyf Ramos-Colón, Senior Scientist, Peptide Applications, Gyros Protein Technologies
Cell Penetration Profiling using the Chloroalkane Penetration Assay for Peptides, Proteins and Nucleic Acids