Picture of boy being examining by doctor at a tuberculosis sanatorium

Understanding our future through Open Access research about our past...

Strathprints makes available scholarly Open Access content by researchers in the Centre for the Social History of Health & Healthcare (CSHHH), based within the School of Humanities, and considered Scotland's leading centre for the history of health and medicine.

Research at CSHHH explores the modern world since 1800 in locations as diverse as the UK, Asia, Africa, North America, and Europe. Areas of specialism include contraception and sexuality; family health and medical services; occupational health and medicine; disability; the history of psychiatry; conflict and warfare; and, drugs, pharmaceuticals and intoxicants.

Explore the Open Access research of the Centre for the Social History of Health and Healthcare. Or explore all of Strathclyde's Open Access research...

Image: Heart of England NHS Foundation Trust. Wellcome Collection - CC-BY.

Strathprints

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

Full text not available in this repository. Request a copy from the Strathclyde author

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
Related URLs:
URI: https://strathprints.strath.ac.uk/id/eprint/54932
Export data:
CORE (COnnecting REpositories)