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Recent findings and future directions for interpolar mitotic kinesin inhibitors in cancer therapy

Myers, Stephanie and Collins, Ian (2016) Recent findings and future directions for interpolar mitotic kinesin inhibitors in cancer therapy. Future Medicinal Chemistry, 8 (4). pp. 463-489. ISSN 1756-8919

Item Type: Article

Abstract

The kinesin class of microtubule-associated motor proteins present attractive anticancer targets owing to their roles in key functions in dividing cells. Two interpolar mitotic kinesins Eg5 and HSET have opposing motor functions in mitotic spindle assembly with respect to microtubule movement, but both offer opportunities to develop cancer selective therapeutic agents. Here, we summarize the progress to date in developing inhibitors of Eg5 and HSET, with an emphasis on structural biology insights into the binding modes of allosteric inhibitors, compound selectivity and mechanisms of action of different chemical scaffolds. We discuss translation of preclinical studies to clinical experience with Eg5 inhibitors, recent findings on potential resistance mechanisms and explore the implications for future anticancer drug development against these targets.

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More Information

Depositing User: Stephanie Myers

Identifiers

Item ID: 9287
Identification Number: https://doi.org/10.4155/fmc.16.5
ISSN: 1756-8919
URI: http://sure.sunderland.ac.uk/id/eprint/9287
Official URL: https://doi.org/10.4155/fmc.16.5

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Catalogue record

Date Deposited: 09 May 2018 10:10
Last Modified: 18 Dec 2019 16:06

Contributors

Author: Stephanie Myers
Author: Ian Collins

University Divisions

Faculty of Health Sciences and Wellbeing
Faculty of Health Sciences and Wellbeing > School of Pharmacy and Pharmaceutical Sciences

Subjects

Sciences > Chemistry
Sciences > Pharmacy and Pharmacology

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