Toggle Main Menu Toggle Search

Open Access padlockePrints

The role of structure in kinase-targeted inhibitor design

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


Full text for this publication is not currently held within this repository. Alternative links are provided below where available.


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