Members of the kinase superfamily are key regulators of pivotal cell signaling pathways. Genetic alterations in protein kinases compromise their biological functions resulting in deregulated cellular pathways such as apoptosis, cell cycle regulation, proliferation, angiogenesis, differentiation, cellular metabolism. Mutations in kinase-encoding genes have been observed in many pathological conditions, ranging from cancer, inflammatory disorders, cardiovascular diseases to neurodegeneration (1). Furthermore, mutations of certain kinases have been linked to acquired drug resistance. As a result, mutant kinases quickly established themselves as important drug targets and have been the focus of drug discovery and development efforts (2).
In an effort to support the advancement of next generation of kinase-targeted therapeutic programs, SignalChem has developed and manufactured over 250 clinically relevant active kinase mutants, representing the most comprehensive list of this class of proteins in the industry.
1. Kumar R et al., CancerDR: cancer drug resistance database. Sci Rep. 2013;3:1445. doi: 10.1038/srep01445.
2. Torkamani, A., Verkhivker, G., & Schork, N. J. (2009). Cancer driver mutations in protein kinase genes. Cancer Letters, 281(2), 117–127. http://doi.org/10.1016/j.canlet.2008.11.008