Structure-Based Design of Novel Anti-Cancer Agents TargetingAurora Kinases

ISSN: 1875-5992 (Online)
ISSN: 1871-5206 (Print)


Volume 16, 12 Issues, 2016


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Anti-Cancer Agents in Medicinal Chemistry

Formerly: Current Medicinal Chemistry - Anti-Cancer Agents

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  • 27th of 59 in Chemistry, Medicinal

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Editor-in-Chief:
Michelle Prudhomme
Universite Blaise Pascal - C.N.R.S
Aubiere Cedex
France


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Structure-Based Design of Novel Anti-Cancer Agents TargetingAurora Kinases



Anti-Cancer Agents in Medicinal Chemistry, 3(1): 25-34.

Author(s): Daruka Mahadevan, David J. Bearss and Hariprasad Vankayalapati.

Affiliation: Arizona Cancer Center, University of Arizona, 1515, N. Campbell Ave., Tucson, AZ, 85724, USA.

Abstract

Aurora kinases are a family of mitotic serine-threonine kinases (S / T kinases), that functions as a class of novel oncogenes and are over-expressed in several solid tumors including breast, ovary, prostate, pancreas and colorectal cancer. To validate human ARK1 (Aurora2, STK15, HsAIRK1) as a drugable target in pancreatic cancer, we undertook a structure-based approach to design specific inhibitors utilizing homology modeling, affinity docking and an in vitro kinase assay in an iterative process. In this review, we discuss the biology, rationale for targeting and approaches taken to inhibit this family of protein kinases, implicated in dysregulated chromosome segregation and cytokinesis.

Keywords:

Anti-Cancer Agents, Novel, argetingAurora, chromosome segregation, cytokinesis.



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Article Details

Volume: 3
Issue Number: 1
First Page: 25
Last Page: 34
Page Count: 10
DOI: 10.2174/1568011033353524
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