Recent advances in research of colchicine binding site inhibitors and their interaction modes with tubulin

被引：28

作者：

Sun, Kewei ^{[1
]}

Sun, Zhonghao ^{[2
]}

Zhao, Fenglan ^{[1
]}

Shan, Guangzhi ^{[2
]}

Meng, Qingguo ^{[1
]}

机构：

[1] Yantai Univ, Collaborat Innovat Ctr Adv Drug Delivery Syst & B, Key Lab Mol Pharmacol & Drug Evaluat, Sch Pharm,Minist Educ, Yantai 264005, Peoples R China

[2] Chinese Acad Med Sci & Peking Union Med Coll, Inst Med Biotechnol, Beijing 100050, Peoples R China

来源：

FUTURE MEDICINAL CHEMISTRY | 2021年 / 13卷 / 09期

基金：

中国国家自然科学基金;

关键词：

antitumor; colchicine site inhibitors; crystal structure of complex; microtubule; tubulin; virtual screening; BIOLOGICAL EVALUATION; TARGETING TUBULIN; PHASE-I; ANTINEOPLASTIC AGENTS; ANTICANCER AGENTS; CANCER-CELLS; POLYMERIZATION INHIBITOR; CYTOTOXIC ACTIVITY; INDOLE MOLECULES; ANTITUMOR AGENTS;

D O I：

10.4155/fmc-2020-0376

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Microtubules have been a concerning target of cancer chemotherapeutics for decades, and several tubulin-targeted agents, such as paclitaxel, vincristine and vinorelbine, have been approved. The colchicine binding site is one of the primary targets on microtubules and possesses advantages compared with other tubulin-targeted agents, such as inhibitors of tumor vessels and overcoming P-glycoprotein overexpression-mediated multidrug resistance. This study reviews and summarizes colchicine binding site inhibitors reported in recent years with structural studies via the crystal structures of complexes or computer simulations to discover new lead compounds. We are attempting to resolve the challenge of colchicine site agent research.

引用

页码：839 / 858

页数：20

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