Over the past decade, therapeutics that target subsets of the 518 human protein kinases
have played a vital role in the fight against cancer. Protein kinases are typically targeted at …

As described in the previous chapter, most kinase inhibitors that have been developed for
use in the clinic act by blocking ATP binding; however, there is growing interest in identifying …

Protein kinases are key players in a large number of cellular signaling pathways.
Dysregulated kinase activity has been implicated in a number of diseases, and members of …

c-Src and Bcr-Abl are two cytoplasmatic tyrosine kinases (TKs) involved in the development
of malignancies. In particular, Bcr-Abl is the etiologic agent of chronic myeloid leukemia …

Loss-of-function studies are valuable for elucidating kinase function and the validation of
new drug targets. While genetic techniques, such as RNAi and genetic knockouts, are highly …

We introduce a versatile approach for repurposing protein kinase chemosensors, containing
the phosphorylation-sensitive sulfonamido-oxine fluorophore termed Sox, for the specific …

The identification of potent and selective modulators of protein kinase function remains a
challenge, and new strategies are needed for generating these useful ligands. Here, we …

Src-family kinases (SFKs) play important roles in human biology and are key drug targets as
well. However, achieving selective inhibition of individual Src-family kinases is challenging …

Hematopoietic cell kinase (Hck) is a member of the Src-family of non-receptor tyrosine
kinases, which plays many roles in signalling pathways involved in the regulation of cell …

Chronic myeloid leukemia (CML) is a disease of bone marrow stem cells caused by
excessive growth and accumulation of granulocytes in the blood. Aberrant expression of the …