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Comprehensive analysis of kinase inhibitor selectivity
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Journal Article
Comprehensive analysis of kinase inhibitor selectivity
2011
Overview
Davis
et al
. extend their previous efforts to use inhibitor-kinase interactions to understand kinase inhibitor selectivity by profiling the binding of 72 kinase inhibitors to 442 human kinase catalytic domains. The data reveal group-specific differences in selectivity and suggest the feasibility of developing reasonably specific inhibitors for most kinases.
We tested the interaction of 72 kinase inhibitors with 442 kinases covering >80% of the human catalytic protein kinome. Our data show that, as a class, type II inhibitors are more selective than type I inhibitors, but that there are important exceptions to this trend. The data further illustrate that selective inhibitors have been developed against the majority of kinases targeted by the compounds tested. Analysis of the interaction patterns reveals a class of 'group-selective' inhibitors broadly active against a single subfamily of kinases, but selective outside that subfamily. The data set suggests compounds to use as tools to study kinases for which no dedicated inhibitors exist. It also provides a foundation for further exploring kinase inhibitor biology and toxicity, as well as for studying the structural basis of the observed interaction patterns. Our findings will help to realize the direct enabling potential of genomics for drug development and basic research about cellular signaling.
Publisher
Nature Publishing Group US,Nature Publishing Group
Subject
/ Biological and medical sciences
/ Biomedical and Life Sciences
/ Biomedical Engineering/Biotechnology
/ Cellular signal transduction
/ Fundamental and applied biological sciences. Psychology
/ Genomics
/ Health. Pharmaceutical industry
/ High-Throughput Screening Assays
/ Humans
/ Industrial applications and implications. Economical aspects
/ Kinases
/ Molecular and cellular biology
/ Protein Kinase Inhibitors - chemistry
/ Protein Kinase Inhibitors - classification
/ Protein Kinases - classification
/ Proteins
/ resource
/ Toxicity
