Estimating the cooperativity of PROTAC-induced ternary complexes using 19F NMR displacement assay

RSC Med Chem. 2021 Aug 24;12(10):1765-1770. doi: 10.1039/d1md00215e. eCollection 2021 Oct 20.

Abstract

Cooperativity is an important parameter to understand the ternary complexes formed by protein degraders. We developed fluorine NMR competition binding experiments to determine cooperativity of PROTACs. We show applicability to estimate both positive and negative cooperativity, also with homo-dimerizers, and highlight key features and considerations for optimal assay development.