207_Combined course Presentations

Kinase inhibitor binding sites

• Type I inhibitors – constitutes majority of ATP-competitive inhibitors and recognizes the so called active conformation of the kinase – e.g. sorafenib, dasatinib, sutent • Type II inhibitors – recognize the inactive conformation of the kinase – e.g. imatinib • Allosteric Inhibitors – bind outside of ATP-binding site; at an allosteric site – exhibit highest degree of kinase selectivity • Covalent inhibitors – require low concentrations – concern about potential toxicity by modification of unanticipated targets