System-based drug discovery within the human kinome.

摘要: Introduction: For well over a decade, significant effort has been devoted to the search for inhibitors of human protein kinase family. This is increasingly translating into success in clinic, with five new inhibitor drugs approved since 2011. However, despite encouraging signs other areas, largely restricted oncology. Areas covered: article reviews prospects drug discovery oncology and therapeutic areas. Major topics include application kinome profiling lessons learned from system-based research. With these fields nearing maturity, validation kinases as targets or their classification liabilities becoming pertinent. Other discussion properties required good small molecule probes. Expert opinion: The tractability through research excellent, adequate selectivity can often be achieved. With...