Inhibitors of PKA and Related Protein Kinases

摘要: The AGC group of protein kinases comprises a number pharmacologically important members—targets for small molecule inhibitors therapeutic value. Crystal structure data assist in the design new or improved inhibitory molecules. Protein kinase A (PKA), one longest and best-known members group, has been cocrystallized with many from highly diverse chemical groups, including isoquinoline derivatives, staurosporine bisindolylmaleimide cognates, balanol pyridine thus providing structural information about binding modes, selectivity cross selectivity. creation ‘ersatz’ by mutating inhibitor site PKA to resemble other fellow cocrystallization these ersatz molecules as well cocrystal structures like 3-phosphoinositide-dependent 1 (PDK1) derivatives helps identification exploration factors governing