207_Combined course Presentations
Mechanisms of small molecule action (TK-inhibitors) I
Initial concerns: well conserved ATP-binding sites in between the family of kinases: can we get specificity?
Using protein cristallography and NMR-spectroscopy sophisticated structure-based design of specific kinase-inhibitors are now feasible
Kinase inhibitors were developed with the goal of highest selectivity, however, several clinically approved kinases inhibitors are potent inhibitors of multiple kinases: reason for potency?
Potential to target multiple distinct processes (hallmarks) associated with tumor growth, but might be more toxic
Several preclinical studies demonstrate (supra-) additive effect by combined treatment modalities mAB plus TK-inhibitors (complementary effects)
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