2-oxoglutarate analogue inhibitors of HIF prolyl hydroxylase
DR Mole, I Schlemminger, LA McNeill… - Bioorganic & medicinal …, 2003 - Elsevier
DR Mole, I Schlemminger, LA McNeill, KS Hewitson, CW Pugh, PJ Ratcliffe, CJ Schofield
Bioorganic & medicinal chemistry letters, 2003•ElsevierHydroxylation 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-1α prolyl hydroxylases in cell-free extracts.
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-1α prolyl hydroxylases in cell-free extracts.
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-1α prolyl hydroxylases in cell-free extracts.
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