Protein posttranslational modifications (PTMs) refer to the breaking or generation of covalent
bonds on the backbones or amino acid side chains of proteins and expand the diversity of …

Over the past decade, whole genome sequencing and other'omics' technologies have
defined pathogenic driver mutations to which tumor cells are addicted. Such addictions …

For kinase inhibitors, intracellular target selectivity is fundamental to pharmacological
mechanism. Although a number of acellular techniques have been developed to measure …

Introduction: Because of their important roles in disease and excellent 'druggability', kinases
have become the second largest drug target family. The great success of the BCR-ABL …

The EGFRT790M mutant contributes approximately 50% to clinically acquired resistance
against gefitinib or erlotinib. However, almost all the single agent clinical trials of the second …

With the advent of the Type II kinase inhibitor imatinib (Gleevec) for treatment against
cancer, rational design of tailored molecules has brought a revolution in medicinal chemistry …

The Janus kinase (JAK) proteins are a family of intracellular nonreceptor tyrosine kinases
involved in cytokine signaling via the JAK–STAT (signal transducers and activators of …

Fibroblast growth factor receptors (FGFRs) are recognized therapeutic targets in cancer. We
here describe insights underpinning the impact of mutations on FGFR1 and FGFR3 kinase …

Kinases control a diverse set of cellular processes comprising of reversible phosphorylation
of proteins. Protein kinases play a pivotal role in human tumor cell proliferation, migration …

Activated Cdc42-associated kinase 1 (ACK1/TNK2) is a nonreceptor tyrosine kinase with a
unique structure. It not only can act as an activated transmembrane effector of receptor …