Protein kinases play important roles in regulating signal transduction in eukaryotic cells. Due to evolutionary conserved binding sites in the catalytic domain of the kinases, most inhibitors that target these sites promiscuously inhibit multiple kinases. Quantitative analysis can reveal complex and unexpected interactions between protein kinases and kinase inhibitors, providing opportunities for identifying multi-targeted inhibitors of specific diverse kinases for drug repurposing and development. We have developed K-Map - a novel and user-friendly web-based program that systematically connects a set of query kinases to kinase inhibitors based on quantitative profiles of the kinase inhibitor activities. Users can use K-Map to find kinase inhibitors for a set of query kinases (obtained from high-throughput 'omics' experiments) or to reveal new interactions between kinases and kinase inhibitors for rational drug combination studies.
Bibliographical noteFunding Information:
We gratefully thank Drs. Subhajyoti De and Tzu Phang, and the Tan Lab members for the constructive suggestions and discussion. We also like to thank the comments and suggestions from the two reviewers that have helped to improve the presentation of this manuscript. Part of this work was supported by the Cancer League of Colorado (JK and ACT), the Department of Defense Award W81XWH-11-1-0527 (ACT), and Institutional start-up fund (ACT).
ASJC Scopus subject areas
- Molecular Medicine
- Molecular Biology
- Drug Discovery