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The role of structure in kinase-targeted inhibitor design

Lookup NU author(s): Professor Jane Endicott, Professor Martin Noble

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Abstract

Protein kinases are attractive targets for rational drug design against a wide range of diseases. From detailed knowledge of the structure-function relationships underlying protein kinase activity and regulation, a number of methods for achieving kinase inhibition have been suggested and explored using structure-aided drug discovery. Attaining selective protein kinase inhibition in a cellular context, and converting the large number of known potent kinase inhibitors into effective drugs, are outstanding problems in this area and, from a structural perspective, the challenges presented by modulating pharmacokinetics and minimizing the incidence of resistant mutations in the target are of particular interest.


Publication metadata

Author(s): Noble MEM; Endicott JA; Pratt DJ

Publication type: Review

Publication status: Published

Journal: Current Opinion In Drug Discovery & Development

Year: 2004

Volume: 7

Issue: 4

Pages: 428-436

ISSN (print): 1367-6733

ISSN (electronic): 2040-3437

Publisher: THOMSON SCIENTIFIC

URL: http://www.ncbi.nlm.nih.gov/pubmed/15338952


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