Diapositive 1

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