摘要
p21活化激酶4(p21-activated kinase 4,PAK4)是丝氨酸/苏氨酸蛋白激酶,参与体内多条信号通路,影响肿瘤细胞的增殖、存活、侵袭转移及凋亡,对肿瘤的发生发展起着重要作用。近年来,PAK4成为抗肿瘤药物研发的新靶点,多种类型的PAK4抑制剂已被发现。本文根据PAK4抑制剂的作用机制不同,分别对ATP竞争性抑制剂、变构抑制剂和miRNAs抑制剂进行综述,主要从结构特征、生物活性及其合成方法等研究进展进行了总结和探讨。
p21-activated kinase 4 (PAK4),the serine/threonine protein kinase, is able to affect the proliferation, survival, apoptosis, invasion and metastasis of tumor cells through multiform mechanisms. PAK4 plays a key role in the occurrence and development of tumor. In recent years, PAK4 is a promising anti-cancer drug target and multiple types of PAK4 inhibitors have been reported. According to the different mechanisms of PAK4 inhibitors, this review focused on the structural characteristics, biological activities and synthetic routes of ATP competitive inhibitors, allosteric inhibitors and miRNAs inhibitors from related literatures.
作者
李瑞娟
程卯生
王健
LI Rui-juan;CHENG Mao-sheng;WANG Jian(College of Pharmacy, Inner Mongolia Medical University, Huhhot 010110, China;Key Laboratory of Structure-Based Drug Design and Discovery, Ministry of Education, Shenyang Pharmaceutical University, Shenyang 110016, China)
出处
《合成化学》
CAS
北大核心
2019年第5期391-399,共9页
Chinese Journal of Synthetic Chemistry
基金
国家自然科学基金地区基金资助项目(81660587)
内蒙古自治区自然科学基金资助项目(2016BS0807)
内蒙古医科大学高层次人才引进项目(X206006)
