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Elucidation of an Allosteric Mode of Action for a Thienopyrazole RORγt Inverse Agonist

Authors
  • de Vries, Rens M. J. M.1
  • Doveston, Richard G.1, 2
  • Meijer, Femke A.1
  • Brunsveld, Luc1
  • 1 Eindhoven University of Technology, The Netherlands , (Netherlands)
  • 2 University of Leicester, UK , (United Kingdom)
Type
Published Article
Journal
ChemMedChem
Publisher
Wiley (John Wiley & Sons)
Publication Date
Mar 12, 2020
Volume
15
Issue
7
Pages
561–565
Identifiers
DOI: 10.1002/cmdc.202000044
PMID: 32053744
PMCID: PMC7187189
Source
PubMed Central
Keywords
License
Unknown
External links

Abstract

Example 13 : Inhibition of the RAR‐related orphan receptor gamma t (RORγt) nuclear receptor has proven to be a novel approach for targeting autoimmune diseases. Recently, RORγt was shown to feature an allosteric pocket. Using X‐ray crystallography, we now show that compound 13 , a promising thienopyrazole analogue of previously reported RORγt modulators, exerts its inverse agonism by binding to this allosteric pocket.

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