The problem of resistance to therapy in cancer is multifaceted. Here we take a reductionist
approach to define and separate the key determinants of drug resistance, which include …

Bcr-Abl inhibitors paved the way of targeted therapy epoch. Imatinib was the first tyrosine
kinase inhibitor to be discovered with high specificity for Bcr-Abl protein resulting from t (9 …

INTRODUCTION Protein kinases mediate many cell signaling processes. Central to their
physiological function is the regulation of their binding and enzymatic activities, which is …

Protein kinases play a predominant regulatory role in nearly every aspect of cell biology and
they can modify the function of a protein in almost every conceivable way. Protein …

The identification of mutationally activated BRAF in many cancers altered our conception of
the part played by the RAF family of protein kinases in oncogenesis. In this Review, we …

The physiological Src proto-oncogene is a protein-tyrosine kinase that plays key roles in cell
growth, division, migration, and survival signaling pathways. From the N-to C-terminus, Src …

Allostery is largely associated with conformational and functional transitions in individual
proteins. This concept can be extended to consider the impact of conformational …

Many human malignancies are associated with aberrant regulation of protein or lipid
kinases due to mutations, chromosomal rearrangements and/or gene amplification. Protein …

Lung cancer is the leading cause of death by cancer in North America. A decade ago,
genomic rearrangements in the anaplastic lymphoma kinase (ALK) receptor tyrosine kinase …

Eukayotic protein kinases evolved as a family of highly dynamic molecules with strictly
organized internal architecture. A single hydrophobic F-helix serves as a central scaffold for …