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Inhibition of a viral prolyl hydroxylase.

Authors :
Langley, Gareth W.
Abboud, Martine I.
Lohans, Christopher T.
Schofield, Christopher J.
Source :
Bioorganic & Medicinal Chemistry. Jun2019, Vol. 27 Issue 12, p2405-2412. 8p.
Publication Year :
2019

Abstract

The hydroxylation of prolyl-residues in eukaryotes is important in collagen biosynthesis and in hypoxic signalling. The hypoxia inducible factor (HIF) prolyl hydroxylases (PHDs) are drug targets for the treatment of anaemia, while the procollagen prolyl hydroxylases and other 2-oxoglutarate dependent oxygenases are potential therapeutic targets for treatment of cancer, fibrotic disease, and infection. We describe assay development and inhibition studies for a procollagen prolyl hydroxylase from Paramecium bursaria chlorella virus 1 (vCPH). The results reveal HIF PHD inhibitors in clinical trials also inhibit vCPH. Implications for the targeting of the human PHDs and microbial prolyl hydroxylases are discussed. [ABSTRACT FROM AUTHOR]

Details

Language :
English
ISSN :
09680896
Volume :
27
Issue :
12
Database :
Academic Search Index
Journal :
Bioorganic & Medicinal Chemistry
Publication Type :
Academic Journal
Accession number :
136646108
Full Text :
https://doi.org/10.1016/j.bmc.2019.01.018