Structure-based design of novel anti-cancer agents targeting Aurora kinases

Daruka Mahadevan, David J. Bearss, Hariprasad Vankayalapati

Research output: Contribution to journalReview articlepeer-review

24 Scopus citations

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.

Original languageEnglish (US)
Pages (from-to)25-34
Number of pages10
JournalCurrent Medicinal Chemistry - Anti-Cancer Agents
Volume3
Issue number1
DOIs
StatePublished - 2003
Externally publishedYes

ASJC Scopus subject areas

  • Molecular Medicine
  • Pharmacology
  • Cancer Research

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