缺氧诱导因子脯氨酰羟化酶的2-氧代戊二酸类似物抑制剂
2-oxoglutarate analogue inhibitors of HIF prolyl hydroxylase.
作者信息
Mole David R, Schlemminger Imre, McNeill Luke A, Hewitson Kirsty S, Pugh Christopher W, Ratcliffe Peter J, Schofield Christopher J
机构信息
Wellcome Trust Centre for Human Genetics, Roosevelt Drive, Oxford OX3 7BN, UK.
出版信息
Bioorg Med Chem Lett. 2003 Aug 18;13(16):2677-80. doi: 10.1016/s0960-894x(03)00539-0.
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.
摘要
缺氧诱导因子是一种核转录因子，其羟基化由铁和2-氧代戊二酸依赖性羟化酶催化。合成了2-氧代戊二酸共底物的各种类似物，并显示它们在无细胞提取物中抑制人缺氧诱导因子-1α脯氨酰羟化酶的活性。
Zotero 插件