Owing to their crucial role in the modulation of cell pathways, protein kinases are important
targets for several human diseases, including but not limited to cancer. The classic approach …

Many members of the protein kinase family have emerged as key targets for
pharmacological intervention, most notably in cancer. However, the high sequence and …

Deregulation of protein kinase activity has been linked to many diseases ranging from
cancer to AIDS and neurodegenerative diseases. Not surprisingly, drugging the human …

The modulation of kinase function has become an important goal in modern drug discovery
and chemical biology research. In cancer-targeted therapies, kinase inhibitors have been …

Multidomain protein kinases, central controllers of signal transduction, use regulatory
domains to modulate catalytic activity in a complex cellular environment. Additionally, these …

Importance of the field: Protein kinases are important targets for drug discovery because
they possess critical roles in many human diseases. Several protein kinase inhibitors have …

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 …

Protein–protein interactions often regulate the activity of protein kinases by allosterically
modulating the conformation of the ATP-binding site. Bidirectional allostery implies that …

Background: The number of drugs in active clinical development or on the market that target
the unactivated conformational states of protein kinases is growing and represents a …

Protein kinases are involved in many essential cellular processes and their deregulation can
lead to a variety of diseases, including cancer. The pharmaceutical industry has invested …