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Current Medicinal Chemistry - Anti-Cancer Agents

Editor-in-Chief

ISSN (Print): 1568-0118
ISSN (Online): 1875-5968

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

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

Volume 3, Issue 1, 2003

Page: [25 - 34] Pages: 10

DOI: 10.2174/1568011033353524

Price: $65

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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