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Title: Biology of Aurora A Kinase: Implications in Cancer Manifestation and Therapy
Authors: Karthigeyan, Dhanasekaran
Benaka Prasad, Sallekoppal B
Shandilya, Jayasha
Agrawal, Shipra
Kundu, Tapas K
Keywords: phosphorylation
centrosome dynamics
kinase inhibitors
Small-Molecule Inhibitor
I Dose-Escalation
A Kinase
Mitotic Spindle
B Kinase
Issue Date: 1-Mar-2010
Publisher: Wiley Blackwell
Citation: Medicinal Research Reviews 31(5), 757-793 (2010)
Abstract: The Aurora A kinase belongs to serine/threonine group of kinases, well known for its role in cell cycle, especially in the regulation of mitosis. Numerous substrates of Aurora A kinase have been identified, which are predominantly related to cell cycle progression while some of them are transcription factors. Aurora A-mediated phosphorylation can either directly or indirectly regulate the function of its substrates. There are overwhelming evidences which report overexpression and gene amplification of Aurora A in several human cancers, and suggest that Aurora A could be a bona fide oncogene involved in tumorigenesis. Hence, Aurora A plays wide-ranging roles in both mitosis and its deregulation manifests in cancer progression. These observations have favored the choice of Aurora kinases as a target for cancer therapy. Recently, numerous small molecules have been discovered against Aurora kinases and many have entered clinical trials. Most of these small-molecule modulators designed are specific against either Aurora A or Aurora B, but some are dual inhibitors targeting the ATP-binding site which is highly conserved among the three human homologues of Aurora kinase. In this review, we discuss the physiological functions of Aurora A, interactions between Aurora A kinase and its cellular substrates, tumorigenesis mediated by Aurora A kinase upon overexpression, and small-molecule modulators of Aurora kinase as targets for cancer therapy. © 2010 Wiley Periodicals, Inc. Med Res Rev
Description: Restricted Access
Other Identifiers: 1098-1128
Appears in Collections:Research Papers (Tapas K. Kundu)

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