碳酸酐酶IX小分子抑制剂的研究进展  

Progress in the study of carbonic anhydrase inhibitors as potential anticancer drugs

作　　者：郭佳[1,2] 李凤然[1,2] 刘洋[1,2] 程卯生[1,2] 

机构地区：[1]沈阳药科大学基于靶点的药物设计与研究教育部重点实验室,辽宁沈阳110016 [2]沈阳药科大学制药工程学院,辽宁沈阳110016

出　　处：《药学学报》2013年第11期1637-1643,共7页Acta Pharmaceutica Sinica

摘　　要：碳酸酐酶IX(CA IX)是一个肿瘤相关蛋白,由于其在多种肿瘤组织中高度表达而在正常组织中几乎不表达,近年来成为一个潜在的抗癌靶点。寻找能够选择性抑制CA IX的小分子抑制剂将成为未来的焦点。本文对其在肿瘤生理活动中的作用、三维晶体结构的特征及小分子抑制剂研究进展进行综述。Carbonic anhydrase IX （CA IX） is a tumor associated protein which is able to be a potent anticancer target, since it is highly expressed in a multitude of carcinomas, while it is present in a limited number of normal tissues. This review focuses on its role in tumor physiology, the most recent three dimensional structure features of this enzyme which has recently been elucidated. In addition, we present recent advances in the development of small inhibitors able to target CA IX for therapeutic applications.

关 键 词：碳酸酐酶IX 抑制剂 缺氧 抗肿瘤 

分 类 号：R916[医药卫生—药学]