2-oxoglutarate analogue inhibitors of HIF prolyl hydroxylase
- PMID: 12873492
- DOI: 10.1016/s0960-894x(03)00539-0
2-oxoglutarate analogue inhibitors of HIF prolyl hydroxylase
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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