Progress on kinesin spindle protein inhibitors as anti-cancer agents.
The kinesin spindle protein (KSP, also known as Hs Eg5) plays an essential part in the proper separation of spindle poles and the correct formation of bipolar mitotic spindle during mitosis. Inhibition of this protein results in cells apoptosis followed by mitotic arrest and the formation of characteristic monoaster spindles. Compared with the traditional chemotherapeutic agents (taxanes, vinca alkaloids), KSP inhibitors (KSPi) will not lead to the neuropathic side effects, so KSP has become a novel and an attractive anticancer target. Accordingly, more and more interest has been focused on the development of high effective and selective KSPi. This review will focus on some kinds of KSPi on the basis of introducing structure and function of KSP.
Zhang
Yingjie
Y
Department of Medicinal Chemistry, School of Pharmaceutical Sciences, Shandong University, 44 West Culture Road, 250012 Ji'nan, Shandong, China.
Xu
Wenfang
W
D000255:Adenosine Triphosphate / Q000378:metabolism; D000970:Antineoplastic Agents / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use*; D001549:Benzamides / Q000138:chemical synthesis / Q000737:chemistry / Q000627:therapeutic use; D006801:Humans; D016547:Kinesins / Q000037:antagonists & inhibitors* / Q000737:chemistry / Q000502:physiology; D008954:Models, Biological; D008958:Models, Molecular; D009369:Neoplasms / Q000188:drug therapy*; D011743:Pyrimidines / Q000138:chemical synthesis / Q000737:chemistry / Q000627:therapeutic use; D011799:Quinazolines / Q000138:chemical synthesis / Q000737:chemistry / Q000627:therapeutic use; D008941:Spindle Apparatus / Q000187:drug effects*; D013871:Thiones / Q000138:chemical synthesis / Q000737:chemistry / Q000627:therapeutic use
D000970:Antineoplastic Agents; D001549:Benzamides; C470243:KIF11 protein, human; D011743:Pyrimidines; D011799:Quinazolines; D013871:Thiones; C400223:monastrol; D000255:Adenosine Triphosphate; C508757:ispinesib; D016547:Kinesins