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Human prolyl hydroxylases are involved in the modification of transcription factors, procollagen, and ribosomal proteins, and are current medicinal chemistry targets. To date, there are few reports on inhibitors selective for the different types of prolyl hydroxylases. We report a structurally informed template-based strategy for the development of inhibitors selective for the human ribosomal prolyl hydroxylase OGFOD1. These inhibitors did not target the other human oxygenases tested, including the structurally similar hypoxia-inducible transcription factor prolyl hydroxylase, PHD2.

Original publication

DOI

10.1002/chem.201804790

Type

Journal article

Journal

Chemistry

Publication Date

06/02/2019

Volume

25

Pages

2019 - 2024

Keywords

2-oxoglutarate oxygenase, OGFOD1, barbiturate, epigenetics, histone demethylases, inhibitors, medicinal chemistry, Carrier Proteins, Drug Design, Humans, Nuclear Proteins, Prolyl Hydroxylases, Prolyl-Hydroxylase Inhibitors, Ribosomes, Structure-Activity Relationship, Substrate Specificity