The specificities of 65 compounds reported to be relatively specific inhibitors of protein
kinases have been profiled against a panel of 70–80 protein kinases. On the basis of this …

Protein kinase inhibitors represent an important and still emerging class of targeted
therapeutic agents. Drug discovery and development strategies have explored numerous …

Publisher Summary This chapter focuses on low-molecular-weight inhibitors that can be
used for studies with intact cells. As the specificity of these inhibitors is a major concern …

Protein kinases are fascinating biological catalysts with a rapidly expanding knowledge
base, a growing appreciation in cell regulatory control, and an ascendant role in successful …

Kinases have emerged as ubiquitous but highly challenging targets for drug discovery. The
human genome has 518 kinases1 and many of these play critical roles in cell growth and …

Kinases are highly regulated enzymes with diverse mechanisms controlling their catalytic
output. Over time, chemical discovery efforts for kinases have produced ATP-competitive …

The confluence of two distinct but related activities in the past 10 years has dramatically
accelerated efforts towards the discovery and development of novel drugs to treat cancer …

Protein-tyrosine kinases (PTKs) have been shown to induce the cascade of altered cell
parameters characteristic of transformed cells. This proposition provides an impor-tant …

Recent years have seen an explosion in the number of publicly available x-ray crystal
structures of protein kinases. These structures have provided a wealth of information on the …

Protein phosphorylation regulates most aspects of cell life, whereas abnormal
phosphorylation is a cause or consequence of disease. A growing interest in developing …