蛋白激酶C抑制剂的研究新进展  

New progress in the study of protein kinase C(PKC)inhibitors

作　　者：吴静[1] 杨睿[2] 刘树业[1] 

机构地区：[1]天津市第三中心医院检验科,300170 [2]天津医科大学基础医学研究中心转化肿瘤学实验室

出　　处：《天津医药》2016年第1期114-117,共4页Tianjin Medical Journal

基　　金：国家自然科学基金资助项目(81301985);天津市应用基础与前沿技术研究计划青年项目(14JCQNJC14000)

摘　　要：蛋白激酶C(PKC)是一组磷脂依赖性的丝氨酸/苏氨酸蛋白激酶,与蛋白激酶A(PKA)和蛋白激酶G(PKG)共同构成丝氨酸/苏氨酸蛋白激酶AGC超家族。PKC包括传统型PKC、新型PKC、非典型PKC和与PKC相关的一些激酶(PRK)成员。PKC广泛分布于哺乳动物的组织和细胞中,对细胞的生长代谢、增殖分化等起着重要的生物学作用。研究表明,多种细胞的变异和疾病的发生发展都与PKC的异常表达有关。因此,设计和寻找高效的PKC抑制剂对于多种有效药物的合成和临床上包括肿瘤、心血管疾病、高血压等多种疾病的治疗都具有非常重要的意义。近年来,关于PKC抑制剂的研究已经成为国内外研究的焦点。大量文献报道了多种有效的PKC抑制剂,并对其作用位点、作用机制以及临床试验数据等进行了分析。这些PKC抑制剂的发现对于PKC的结构分析和疾病的治疗具有重要的意义。因此,本文对这些高效的PKC抑制剂进行综述。Protein kinase C （PKC） is a group of phospholipid-dependent serine/threonine protein kinases, which togeth- er with protein kinase A （PKA） and protein kinase G （PKG） constitute a superfamily of serine/threonine protein kinase AGC. PKC includes classic PKC, novel PKC, atypical PKC and some members of kinase associated with PKC （PRK）. PKC is widely distributed in mammalian tissues and ceils, which plays an important biological role in growth and metabolism, proliferation and differentiation of cells. A series of studies have demonstrated that variations of multiple cells, occurrence and devel- opment of diseases are related to the abnormal expression of PKC. Therefore, designing and searching for efficient PKC inhib- itors have very important implications for synthesis of many kinds of effective drugs and treatment of a variety of clinical dis- eases including cancer, cardiovascular, and hypertension, et al. In recent years, the research on PKC inhibitors has become the focus of domestic and foreign research. A large number of literatures have reported many kinds of effective PKC inhibi- tors, and analyzed their function site, mechanism, clinical trial data and so on. The discovery of these PKC inhibitors has im- portant implications for structural analysis of PKC and the treatment of diseases. So in this paper, the efficient PKC inhibi- tots are summarized.

关 键 词：蛋白激酶C 酶抑制剂 胰蛋白酶抑制剂 蛋白激酶抑制剂 肿瘤 综述 

分 类 号：R730.53[医药卫生—肿瘤]