High-throughput kinase profiling as a platform for drug discovery
- PMID: 18404149
- DOI: 10.1038/nrd2541
High-throughput kinase profiling as a platform for drug discovery
Abstract
To fully exploit the potential of kinases as drug targets, novel strategies for the efficient discovery of inhibitors are required. In contrast to the traditional, linear process of inhibitor discovery, high-throughput kinase profiling enables a parallel approach by interrogating compounds against hundreds of targets in a single screen. Compound potency and selectivity are determined simultaneously, providing a choice of targets to pursue that is guided by the quality of lead compounds available, rather than by target biology alone.
Similar articles
-
Doing more than just the structure-structural genomics in kinase drug discovery.Curr Opin Chem Biol. 2008 Feb;12(1):40-5. doi: 10.1016/j.cbpa.2008.01.042. Epub 2008 Feb 29. Curr Opin Chem Biol. 2008. PMID: 18267130 Review.
-
High-throughput screening for kinase inhibitors.Chembiochem. 2005 Mar;6(3):481-90. doi: 10.1002/cbic.200400211. Chembiochem. 2005. PMID: 15742384 Review.
-
High affinity targets of protein kinase inhibitors have similar residues at the positions energetically important for binding.J Mol Biol. 2005 Oct 7;352(5):1134-56. doi: 10.1016/j.jmb.2005.07.074. J Mol Biol. 2005. PMID: 16139843
-
Improved lead-finding for kinase targets using high-throughput docking.Curr Opin Drug Discov Devel. 2006 May;9(3):339-47. Curr Opin Drug Discov Devel. 2006. PMID: 16729730 Review.
-
Kinase-targeted libraries: the design and synthesis of novel, potent, and selective kinase inhibitors.Drug Discov Today. 2009 Mar;14(5-6):291-7. doi: 10.1016/j.drudis.2008.12.002. Epub 2009 Jan 21. Drug Discov Today. 2009. PMID: 19121409 Review.
Cited by
-
Comprehensive structural and functional characterization of the human kinome by protein structure modeling and ligand virtual screening.J Chem Inf Model. 2010 Oct 25;50(10):1839-54. doi: 10.1021/ci100235n. J Chem Inf Model. 2010. PMID: 20853887 Free PMC article.
-
Entering the 'big data' era in medicinal chemistry: molecular promiscuity analysis revisited.Future Sci OA. 2017 Mar 6;3(2):FSO179. doi: 10.4155/fsoa-2017-0001. eCollection 2017 Jun. Future Sci OA. 2017. PMID: 28670471 Free PMC article. Review.
-
Characterization of a selective inhibitor of the Parkinson's disease kinase LRRK2.Nat Chem Biol. 2011 Apr;7(4):203-5. doi: 10.1038/nchembio.538. Epub 2011 Mar 6. Nat Chem Biol. 2011. PMID: 21378983 Free PMC article.
-
Malaria biology and disease pathogenesis: insights for new treatments.Nat Med. 2013 Feb;19(2):156-67. doi: 10.1038/nm.3073. Epub 2013 Feb 6. Nat Med. 2013. PMID: 23389616 Free PMC article. Review.
-
Advances in exploring the therapeutic potential of marine natural products.Pharmacol Res. 2019 Sep;147:104373. doi: 10.1016/j.phrs.2019.104373. Epub 2019 Jul 25. Pharmacol Res. 2019. PMID: 31351913 Free PMC article. Review.
Publication types
MeSH terms
Substances
LinkOut - more resources
Full Text Sources
Other Literature Sources