2013 Archived Content


Constrained Peptides and Macrocyclics Drug Discovery

Novel Peptide Therapeutics

April 16-17, 2013

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7:45 am Continental Breakfast Breakout Discussions

In this interactive session, several topics will be offered for discussions and delegates are invited to choose a topic of interest and join the moderated discussion at hand. In this informal setting, participants are encouraged to share examples from their work, vet ideas with peers and be part of a group problem-solving endeavor. We emphasize that this is an informal exchange amongst scientists and is not meant to be, in any way, a product promoting session.

Topic: Macrocycles in Hit to Lead Optimization: Specific Challenges and Possible Solutions

Moderator: Marc Thommen, Ph.D., Head Technology Platforms, Polyphor Ltd.

  • Chemical synthesis and optimization of macrocycle hits
  • Rapid synthesis of macrocyclic arrays
  • Analysis and prediction of conformations of semi-rigid macrocyclic molecules

Topic: Library Designs for Cyclic Molecules

Julio Camarero, Ph.D., Associate Professor, Pharmacology and Chemistry, University of Southern California

  • Chemical v. biological libraries
  • Designing the perfect library
  • How to screen and select your hits

Topic: Macrocycles Drug Development

Moderator: Ian Lewis, Ph.D., Research Chemist, Global Discovery Chemistry, Novartis

  • Hurdles in development of macrocyclic peptides
  • Technologies supporting delivery of peptide therapeutics
  • Establishing a peptide permeability and oral bioavailability road map



8:55 Chairperson’s Opening Remarks

Jan Hoflack, Ph.D., Head, Drug Discovery, ONCODESIGN Biotechnology


9:00 Direct Selection of Cyclomimetics™ from In Vitro Display Libraries

Douglas A. Treco, Ph.D., President and CEO, Ra Pharmaceuticals

Peptides offer high potency and target selectivity but display poor pharmacokinetics and bioavailability. Modifications aimed at improving these properties are typically added after a candidate sequence is identified, often reducing potency and rarely delivering high quality clinical leads. By incorporating non-natural side chains and N-substituted amino acids into cyclic peptide libraries through in vitro translation, Ra Pharma’s Extreme Diversity™ platform allows direct selection of cyclic peptidomimetics (Cyclomimetics) from libraries of up to 100 trillion members.

9:30 Successful Application of Novel Constrained Macrocycles in Drug Discovery

Daniel Obrecht, Ph.D., CSO, Polyphor, Ltd.

PEMfinder® (PEM=Protein Epitope Mimetics) and MacroFinder® are two complementary macrocycle-based platforms (MW= 400-2000) that have been developed by Polyphor as powerful tools to identify potent and selective modulators of intra- and extracellular protein-protein interactions (PPIs).This presentation will describe successful drug discovery case studies of applying PEMfinder®  and MacroFinder®  from discovery to the clinic.

10:00 Coffee Break in the Exhibit Hall with Poster Viewing

10:45 Targeting Protein-Protein Interactions with Engineered Cyclotides

Julio Camarero, Ph.D., Associate Professor, Pharmacology and Chemistry, University of Southern California

I will present new data on the biosynthesis of cyclotides using bacterial and yeast expression systems for the generation of large genetically-encoded cyclotide-based libraries for high throughput cell-based screening and selection of cyclotides with novel biological activities. We will also report the design and biosynthesis of a MCoTI-grafted cyclotide with the ability to target intracellular and extracellular protein-protein interactions.

11:15 Bi-Cyclic Peptides to Target Endopeptidases

Christophe Bonny, Ph.D., CSO, Bicycle Therapeutics Limited

The Bicycle technology is based on repertoires of peptides displayed on the surface of bacteriophages which can be modified with an organochemical scaffold to create a diverse array of constrained peptides. These repertoires have been extensively used for iterative selections to identify high affinity binding peptides for a wide array of proteases. Results will be presented that exemplify the potential of the technology and its application to animal models of diseases.

11:45 End of Conference

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