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Inhibition of JMJD6 by 2‐Oxoglutarate Mimics
Author(s) -
Islam Md. Sailful,
Thinnes Cyrille C.,
HoltMartyn James P.,
Chowdhury Rasheduzzaman,
McDonough Michael A.,
Schofield Christopher J.
Publication year - 2022
Publication title -
chemmedchem
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.817
H-Index - 100
eISSN - 1860-7187
pISSN - 1860-7179
DOI - 10.1002/cmdc.202100398
Subject(s) - chemistry , hydroxylation , oxygenase , enzyme , biochemistry , drug discovery , computational biology , stereochemistry , biology
Studies on the inhibition of the human 2‐oxoglutarate dependent oxygenase JMJD6, which is a cancer target, by 2‐oxoglutarate mimics / competitors, including human drugs, drug candidates, and metabolites relevant to cancer are described. JMJD6 assays employed NMR to monitor inhibitor binding and use of mass spectrometry to monitor JMJD6‐catalysed lysine hydroxylation. Notably, some clinically applied prolyl hydroxylase inhibitors also inhibit JMJD6. The results will help enable the development of inhibitors selective for human oxygenases, including JMJD6.