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Selective inhibitors of a human prolyl hydroxylase (OGFOD1) involved in ribosomal decoding

Authors :
Thinnes, Cyrille C.
Lohans, Christopher T.
Abboud, Martine I.
Yeh, Tzu‐Lan
Tumber, Anthony
Nowak, Radosław P.
Attwood, Martin
Cockman, Matthew E.
Oppermann, Udo
Loenarz, Christoph
Schofield, Christopher J.
Source :
Chemistry (Weinheim an Der Bergstrasse, Germany)
Publication Year :
2018
Publisher :
Wiley, 2018.

Abstract

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.

Details

Database :
OpenAIRE
Journal :
Chemistry (Weinheim an Der Bergstrasse, Germany)
Accession number :
edsair.pmid.dedup....1325aa488e5f1ff15a8b42f960dc3e4d