Kinase inhibition is a major area for therapeutic intervention against a va
riety of diseases including cancer, inflammatory disorders and diabetes. Wh
ile this mode of action remains very promising at this time, it faces criti
cal challenges, such as drug safety, and biopharmaceutical profile. This re
view provides an update on kinase inhibitor pharmacophores from a structura
l standpoint. Advances in older inhibitor classes as well as new emerging l
ead structures will be presented.