Lookup NU author(s): Professor Jane Endicott,
Professor Martin Noble
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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.
Author(s): Noble MEM; Endicott JA; Pratt DJ
Publication type: Review
Publication status: Published
Journal: Current Opinion In Drug Discovery & Development
ISSN (print): 1367-6733
ISSN (electronic): 2040-3437
Publisher: THOMSON SCIENTIFIC