| 引用本文: | 李姗,盛荣,胡永洲.脯氨酸羟化酶抑制剂的研究进展[J].中国现代应用药学,2015,32(10):1277-1285. |
| LI Shan,SHENG Rong,HU Yongzhou.Recent Progress of Prolyl Hydroxylase Domain Inhibitors[J].Chin J Mod Appl Pharm(中国现代应用药学),2015,32(10):1277-1285. |
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| 摘要: |
| 低氧诱导因子(hypoxia-inducible factor，HIF)是细胞适应低氧环境的关键性转录因子，在组织贫(缺)血和炎症性疾病中稳定表达，对缓解病情具有重要作用。脯氨酸羟化酶(proline hydroxylase domain，PHD)能实现HIF的羟基化，是体内降解HIF的最主要蛋白酶。PHD抑制剂可以有效增加体内HIF蛋白含量，对于贫血及炎症性疾病治疗具有积极意义。本研究对小分子PHD抑制剂的最新进展进行综述。 |
| 关键词: 低氧 低氧诱导因子 脯氨酸羟化酶 脯氨酸羟化酶抑制剂 |
| DOI： |
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| 基金项目:国家自然科学基金面上项目(21072171) |
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| Recent Progress of Prolyl Hydroxylase Domain Inhibitors |
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LI Shan, SHENG Rong, HU Yongzhou
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College of Pharmaceutical Sciences, Zhejiang University, Hangzhou 310058, China
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| Abstract: |
| Hypoxia inducible factor(HIF) is the key transcriptional factor of cellular response to hypoxia and plays a critical role in hypoxia related diseases. When tissue ischemic and inflammation occured, HIF stabilization can be observed and beneficial to tissue stress and injury. Prolyl hydroxylase domain (PHD) selectively hydroxylate proline residues of HIF and act as the most important proteasomal degradation enzyme for HIF in vivo. Thus, PHD inhibition is effective in the treatment of ischemic and inflammatory events through HIF stabilization. In this short review, we will introduce the recent progress of PHD inhibitors. |
| Key words: hypoxia hypoxia-inducible factor prolyl hydroxylase domain prolyl hydroxylase domain inhibitors |
