Cambridge Healthtech Institute’s 7th Annual

Macrocyclics & Constrained Peptides
( 大环状肽及拘束性肽 )

Cell-Penetrating, Bigger Molecules for Oral-Based Therapeutics

2019年4月10日~11日

 

Synthetic macrocyclics and constrained peptides are of growing interest in the pharmaceutical industry because they are expanding the chemical space that can be explored for new therapies. This new class is considered ‘ideal’ because its medium size and ring structure are supposed to combine the best properties of biologics and small molecules. They are small enough to get in cells but large enough for specific interactions with more targets such as protein-protein interactions (PPIs) and their cyclic nature enhances their solubility. Some compounds are advancing in clinical trials. However, challenges still remain such as solubility and cell-penetration. Medicinal chemists continue to refine design ideas. Directed-evolution approaches to create libraries based on macrocyclics are also being applied. Join us at Cambridge Healthtech Institute's 7th Annual Macrocyclics & Constrained Peptides conference to stay abreast of progress and be part of the ground-laying efforts in this new field.

Coverage will include, but is not limited to:

  • Synthetic approaches for macrocyclic peptides
  • Methods for constraining peptides
  • Using natural products as starting points
  • Design strategies for cell-permeability and solubilization
  • Directed evolution approaches (e.g.: DNA-encoded libraries) for macrocyclic and constrained peptides
  • Designing desirable features that go beyond Lipinski’s ‘Rule of Five’
  • Examples of ‘middle-sized compounds’ progressing in development

* 活动内容有可能不事先告知作更动及调整。