2-oxoglutarate analogue inhibitors of HIF prolyl hydroxylase

被引：133

作者：

Mole, DR

Schlemminger, I

McNeill, LA

Hewitson, KS

Pugh, CW

Ratcliffe, PJ

Schofield, CJ

机构：

[1] Univ Oxford, Oxford Ctr Mol Sci, Dyson Perrins Lab, Oxford OX1 3QY, England

[2] Wellcome Trust Ctr Human Genet, Oxford OX3 7BN, England

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2003年 / 13卷 / 16期

基金：

英国惠康基金; 英国工程与自然科学研究理事会; 英国生物技术与生命科学研究理事会;

关键词：

D O I：

10.1016/S0960-894X(03)00539-0

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

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-la prolyl hydroxylases in cell-free extracts. (C) 2003 Published by Elsevier Ltd.

引用

收藏

页码：2677 / 2680

页数：4

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