Protein kinases are integrated into nearly every facet of the regulati
on of mammalian cellular proliferation. The identification of particul
ar kinase isoforms and tissue-specific expression affords the possibil
ity of precise targeting of specific regulatory pathways if potent, hi
ghly selective, cell-penetrable inhibitors can be developed. At the ve
ry least, such inhibitors would provide opportunities to dissect compl
ex interconnected regulatory pathways in intact cells, and sustain the
promise of the development of therapeutic leads, This paper reviews r
ecent developments in the identification of protein kinase targets for
the treatment of cancer, and in the design of selective inhibitors fo
r these enzymes.