Understanding Cell Penetration of Cyclic Peptides

Approximately 75% of all disease-relevant human proteins, including those involved in intracellular protein-protein interactions (PPIs), are undruggable with the current drug modalities (i.e., small molecules and biologics). Macrocyclic peptides provide a potential solution to these undruggable targets because their larger sizes (relative to conventional small molecules) endow them the capability of binding to flat PPI interfaces with antibody-like affinity and specificity. Powerful combinatorial library technologies have been developed to routinely identify cyclic peptides as potent, specific inhibitors against proteins including PPI targets. However, with the exception of a very small set of sequences, the…

• CF
  Cystic Fibrosis Foundation

  Award: PEI18G0
• OS
  Ohio State University
• NI
  National Institute of General Medical Sciences

  Award: GM122459
• NI
  National Institute of Allergy and Infectious Diseases

  Award: A139600