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The Discovery and Development of Eg5 Inhibitors for the Clinic
Umeå University, Faculty of Science and Technology, Department of Chemistry. Umeå University, Faculty of Medicine, Umeå Centre for Microbial Research (UCMR).
2015 (English)In: Kinesins and Cancer / [ed] Frank Kozielski, Springer, 2015, 27-52 p.Chapter in book (Refereed)
Abstract [en]

The mitotic kinesin Eg5 (also known as kinesin spindle protein, KSP, Kif11, a member of the kinesin-5 family) represents an attractive oncology drug target in the ongoing development of anti-mitotic drugs that selectively block mitosis through disruption to the mitotic spindle. In this state-of-the-art review, we outline the progress that has been made in the development of Eg5 inhibitors for clinical use. We evaluate the preclinical development and attributes of key Eg5 inhibitors that have undergone clinical evaluation or extensive preclinical optimisation, and discuss the medicinal chemistry strategies utilised in their design to overcome the challenges encountered during lead optimisation. We critically analyse the progress that has been made towards delivering clinical benefits, and the wider implications this has in the utility of mitotic kinesin inhibitors as prospective oncology drugs.

Place, publisher, year, edition, pages
Springer, 2015. 27-52 p.
Keyword [en]
Anti-mitotic, Drug discovery, Multiple myeloma, Kinesins, Eg5
National Category
Chemical Sciences Cancer and Oncology
URN: urn:nbn:se:umu:diva-106758DOI: 10.1007/978-94-017-9732-0_2ISBN: 978-94-017-9731-3ISBN: 978-94-017-9732-0OAI: diva2:844624
Available from: 2015-08-07 Created: 2015-08-07 Last updated: 2016-01-15Bibliographically approved

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Good, James A. D.
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Department of ChemistryUmeå Centre for Microbial Research (UCMR)
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