  Research on kinase-targeting drugs has made great strides over the last 30
years and is attracting greater attention for the treatment of yet more
kinase-related diseases. Currently, 42 kinase drugs have been approved by the
FDA, most of which (39) are Type I/II inhibitors. Notwithstanding these
advances, it is desirable to target additional kinases for drug development as
more than 200 diseases, particularly cancers, are directly associated with
aberrant kinase regulation and signaling. Here, we review the extant Type I/II
drugs systematically to obtain insights into the binding pocket
characteristics, the associated features of Type I/II drugs, and the mechanism
of action to facilitate future kinase drug design and discovery. We conclude by
summarizing the main successes and limitations of targeting kinase for the
development of drugs.
