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. 2003 Aug 18;13(16):2677-80.
doi: 10.1016/s0960-894x(03)00539-0.

2-oxoglutarate analogue inhibitors of HIF prolyl hydroxylase

David R Mole  1 , Imre Schlemminger, Luke A McNeill, Kirsty S Hewitson, Christopher W Pugh, Peter J Ratcliffe, Christopher J Schofield
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2-oxoglutarate analogue inhibitors of HIF prolyl hydroxylase

David R Mole et al. Bioorg Med Chem Lett. .

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.

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