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

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.

SUBMITTER: de Castro GV 

PROVIDER: S-EPMC8528210 | biostudies-literature | 2021 Oct

REPOSITORIES: biostudies-literature

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Estimating the cooperativity of PROTAC-induced ternary complexes using <sup>19</sup>F NMR displacement assay.

de Castro Guilherme Vieira GV   Ciulli Alessio A  

RSC medicinal chemistry 20210824 10

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. ...[more]

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