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Bioorg Med Chem Lett. 2003 Aug 18;13(16):2677-80.

2-oxoglutarate analogue inhibitors of HIF prolyl hydroxylase.

Author information

1
Wellcome Trust Centre for Human Genetics, Roosevelt Drive, Oxford OX3 7BN, UK.

Abstract

Hydroxylation of hypoxia-inducible factor, a nuclear transcription factor, is catalysed by iron and 2-oxoglutarate dependent hydroxylases. Various analogues of the 2-oxoglutarate cosubstrate were synthesised and shown to inhibit the activity of human hypoxia-inducible factor-1alpha prolyl hydroxylases in cell-free extracts.

PMID:
12873492
DOI:
10.1016/s0960-894x(03)00539-0
[Indexed for MEDLINE]

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