The ins and outs of selective kinase inhibitor development

Protein kinases have emerged as one of the most successful families of drug targets. To date, most selective kinase inhibitors have been discovered serendipitously either through broad selectivity screening or through the discovery of unique binding modes. Here we discuss design strategies that coul...

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Bibliographic Details
Published inNature chemical biology Vol. 11; no. 11; pp. 818 - 821
Main Authors Müller, Susanne, Chaikuad, Apirat, Gray, Nathanael S, Knapp, Stefan
Format Journal Article
LanguageEnglish
Published New York Nature Publishing Group US 01.11.2015
Nature Publishing Group
Subjects
631/535/1266
631/67
631/92/275
631/92/613
Allosteric Site
Biochemical Engineering
Biochemistry
Bioorganic Chemistry
Catalytic Domain
Cell Biology
Chemistry
Chemistry/Food Science
commentary
Crystallography, X-Ray
Drug Approval
Drug Design
Drug Discovery
Drug therapy
Humans
Kinases
Protein Conformation
Protein Kinase Inhibitors - chemical synthesis
Protein Kinase Inhibitors - chemistry
Protein Kinases - chemistry
Proteins
Quantitative Structure-Activity Relationship
Small Molecule Libraries - chemical synthesis
Small Molecule Libraries - chemistry
United States
United States Food and Drug Administration
United States
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Summary:Protein kinases have emerged as one of the most successful families of drug targets. To date, most selective kinase inhibitors have been discovered serendipitously either through broad selectivity screening or through the discovery of unique binding modes. Here we discuss design strategies that could lead to a broader coverage of the kinome with selective inhibitors and to a more rational approach for developing them.
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ISSN:1552-4450
1552-4469
DOI:10.1038/nchembio.1938