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

Guilherme Vieira de Castro; Alessio Ciulli

doi:10.1039/D1MD00215E

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

Guilherme Vieira de Castro ‡^a and Alessio Ciulli

*^a

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* Corresponding authors

^a Division of Biological Chemistry and Drug Discovery, School of Life Sciences, University of Dundee, Dow Street, Dundee, UK
E-mail: a.ciulli@dundee.ac.uk

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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Article information

DOI: https://doi.org/10.1039/D1MD00215E
Article type: Research Article
Submitted: 25 Jun 2021
Accepted: 17 Aug 2021
First published: 24 Aug 2021

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RSC Med. Chem., 2021,12, 1765-1770

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

G. V. de Castro and A. Ciulli, RSC Med. Chem., 2021, 12, 1765 DOI: 10.1039/D1MD00215E

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