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

Literature Information

Publication Date 2021-08-24
DOI 10.1039/D1MD00215E
Impact Factor 0
Authors

Guilherme Vieira de Castro, Alessio Ciulli


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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.

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