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The discovery and development of Eg5 inhibitors for the clinic

Good, James A. D. and Berretta, Giacomo and Anthony, Nahoum G. and Mackay, Simon P. (2015) The discovery and development of Eg5 inhibitors for the clinic. In: Kinesins and Cancer. Sense Publishers, pp. 27-52. ISBN 978-94-017-9731-3

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Abstract

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.

Item type: Book Section
ID code: 54932
Keywords: anti-mitotic, drug discovery, Eg5, kinesins, multiple myeloma, Neoplasms. Tumors. Oncology (including Cancer), Pharmacy and materia medica, Medicine(all), Biochemistry, Genetics and Molecular Biology(all), Chemistry(all), Pharmacology, Toxicology and Pharmaceutics(all)
Subjects: Medicine > Internal medicine > Neoplasms. Tumors. Oncology (including Cancer)
Medicine > Pharmacy and materia medica
Department: University of Strathclyde > University of Strathclyde
Faculty of Science > Strathclyde Institute of Pharmacy and Biomedical Sciences
Depositing user: Pure Administrator
Date deposited: 11 Dec 2015 04:25
Last modified: 22 Feb 2019 03:51
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URI: https://strathprints.strath.ac.uk/id/eprint/54932
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