Estimating the cooperativity of PROTAC-induced ternary complexes using 19F NMR displacement assay,RSC Medicinal Chemistry

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Estimating the cooperativity of PROTAC-induced ternary complexes using 19F NMR displacement assay
RSC Medicinal Chemistry ( IF 4.1 ) Pub Date : 2021-08-24 , DOI: 10.1039/d1md00215e
Guilherme Vieira de Castro ₁ , Alessio Ciulli ₁

Affiliation

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.

中文翻译：

使用 19F NMR 置换法估计 PROTAC 诱导的三元配合物的协同性

协同性是了解蛋白质降解剂形成的三元复合物的重要参数。我们开发了氟核磁共振竞争结合实验来确定 PROTAC 的协同性。我们展示了估计阳性和阴性协同性的适用性，也适用于同型二聚体，并强调了优化分析开发的关键特征和考虑因素。

更新日期：2021-09-07

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