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

Guilherme Vieira de Castro, Alessio Ciulli (Lead / Corresponding author)

Research output: Contribution to journalArticlepeer-review

8 Citations (Scopus)
71 Downloads (Pure)

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.
Original languageEnglish
Pages (from-to)1765-1770
Number of pages6
JournalRSC Medicinal Chemistry
Volume12
Early online date24 Aug 2021
DOIs
Publication statusPublished - Oct 2021

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Pharmacology
  • Pharmaceutical Science
  • Drug Discovery
  • Organic Chemistry

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