Importance of Rigidity in Designing Small Molecule Drugs To Tackle Protein–Protein Interactions (PPIs) through Stabilization of Desired Conformers

Abstract

Tackling PPIs, particularly by stabilizing clinically favored conformations of target proteins, with orally available, bona fide small molecules remains a significant but immensely worthwhile challenge for the pharmaceutical industry. Success may be more likely through the application of nature's learnings to build intrinsic rigidity into the design of clinical candidates.