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Estimating the cooperativity of PROTAC-induced ternary complexes using 19F NMR displacement assay†
Guilherme Vieira de Castro,Alessio Ciulli
RSC Medicinal Chemistry Pub Date : 08/24/2021 00:00:00 , DOI:10.1039/D1MD00215E
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.

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