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The Discovery and Development of Eg5 Inhibitors for the Clinic
Umeå universitet, Teknisk-naturvetenskapliga fakulteten, Kemiska institutionen. Umeå universitet, Medicinska fakulteten, Umeå Centre for Microbial Research (UCMR).ORCID-id: 0000-0003-2377-030X
2015 (Engelska)Ingår i: Kinesins and Cancer / [ed] Frank Kozielski, Springer, 2015, s. 27-52Kapitel i bok, del av antologi (Refereegranskat)
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.

Ort, förlag, år, upplaga, sidor
Springer, 2015. s. 27-52
Nyckelord [en]
Anti-mitotic, Drug discovery, Multiple myeloma, Kinesins, Eg5
Nationell ämneskategori
Kemi Cancer och onkologi
Identifikatorer
URN: urn:nbn:se:umu:diva-106758DOI: 10.1007/978-94-017-9732-0_2Scopus ID: 2-s2.0-84943196508ISBN: 978-94-017-9731-3 (tryckt)ISBN: 978-94-017-9732-0 (tryckt)OAI: oai:DiVA.org:umu-106758DiVA, id: diva2:844624
Tillgänglig från: 2015-08-07 Skapad: 2015-08-07 Senast uppdaterad: 2023-08-25Bibliografiskt granskad

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Good, James A. D.

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Good, James A. D.
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Kemiska institutionenUmeå Centre for Microbial Research (UCMR)
KemiCancer och onkologi

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Totalt: 252 träffar
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