Bringing Kinases Into Focus: Efficient Drug Design Through the Use of Chemogenomic Toolkits

Author(s): Veronique Birault, C. J. Harris, Joelle Le, Mike Lipkin, Ravi Nerella, Adrian Stevens.

Journal Name: Current Medicinal Chemistry

Volume 13 , Issue 15 , 2006


The study of protein target families, as opposed to single targets, has become a very powerful tool in chemogenomics-led drug discovery. By integrating comprehensive chemoinformatics and bioinformatics databases with customised analytical tools, a Toolkit approach for the target family is possible, thus allowing predictions of the ligand class, affinity, selectivity and likely off-target issues to be made for the guidance of the medicinal chemist. In this review, we highlight the development and application of the Toolkit approach to the protein kinase superfamily, drawing on examples from lead optimisation studies and the design of focused libraries for lead discovery.

Keywords: Chemogenomics, kinases, Toolkit, 2D-roadmap™, Kinome Similarity Analysis™, KSA, cyclin-dependent, CDK2, CDK4, p38

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Article Details

Year: 2006
Page: [1735 - 1748]
Pages: 14
DOI: 10.2174/092986706777452452
Price: $58

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