Title : First-in-Class Inhibitors of the Ribosomal Oxygenase MINA53.

Pub. Date : 2021 Dec 9

PMID : 34843649






2 Functional Relationships(s)
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1 These assays enabled the identification of 2-(aryl)alkylthio-3,4-dihydro-4-oxoypyrimidine-5-carboxylic acids as potent MINA53 inhibitors, with selectivity over NO66 and other JmjC oxygenases. 2-(aryl)alkylthio-3,4-dihydro-4-oxoypyrimidine-5-carboxylic acids ribosomal oxygenase 2 Homo sapiens
2 Crystallographic studies with the JmjC demethylase KDM5B revealed active site binding but without direct metal chelation; however, molecular modeling investigations indicated that the inhibitors bind to MINA53 by directly interacting with the iron cofactor. Iron ribosomal oxygenase 2 Homo sapiens