Design, synthesis and evaluation of an NLRP3 inhibitor diazirine photoaffinity probe

James R. Hill*, Rebecca C. Coll, Kate Schroder, Avril A.B. Robertson

*Corresponding author for this work

Research output: Contribution to journalArticle

1 Citation (Scopus)

Abstract

The NLRP3 inhibitor MCC950/CRID3 ameliorates a remarkable number of inflammatory disorders in animal models. Herein we describe a trifluoromethyl phenyl diazirine (TPD) photoaffinity probe, called TPD-950-Br, to probe the molecular interactions of MCC950. We show that TPD-950-Br covalently captures proximal species upon photo-activation and inhibits IL-1β production in an NLRP3 inhibitor assay.

Original languageEnglish
Article number151849
JournalTetrahedron Letters
Early online date16 Mar 2020
DOIs
Publication statusEarly online date - 16 Mar 2020

Keywords

  • Diazirine
  • NLRP3 inflammasome
  • Photoaffinity
  • Sandmeyer

ASJC Scopus subject areas

  • Biochemistry
  • Drug Discovery
  • Organic Chemistry

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