Covalent Targeting of Ras G12C by Rationally Designed Peptidomimetics.

ABSTRACT: Protein-protein interactions (PPIs) play a critical role in fundamental biological processes. Competitive inhibition of these interfaces requires compounds that can access discontinuous binding epitopes along a large, shallow binding surface area. Conformationally defined protein surface mimics present a viable route to target these interactions. However, the development of minimal protein mimics that engage intracellular targets with high affinity remains a major challenge because mimicry of a portion of the binding interface is often associated with the loss of critical binding interactions. Covalent targeting provides an attractive approach to overcome the loss of noncovalent contacts but have the inherent risk of dominating noncovalent contacts and increasing the likelihood of nonselec

SUBMITTER: Yoo DY 

PROVIDER: S-EPMC7739374 | biostudies-literature | 2020 Jun

REPOSITORIES: biostudies-literature