Advances in Anticancer Agents in Medicinal Chemistry

Volume: 1

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Advances in Anticancer Agents in Medicinal Chemistry is an exciting eBook series comprising a selection of updated articles previously published in the peer-reviewed journal Anti-Cancer Agents in ...
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Progress Review on Kinesin Spindle Protein Inhibitors as Anti- Cancer Agents

Pp. 240-268 (29)

Yingjie Zhang and Wenfang Xu


The kinesin spindle protein (KSP, also known as Hs Eg5) plays an essential role 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.


Kinesin, KSP, uncompetitive inhibitor, competitive inhibitor, allosteric inhibitor.


Department of Medicinal Chemistry, School of Pharmaceutical Sciences, Shandong University, 44 West Culture Road, 250012 Ji’nan, Shandong, China