Photoaffinity labeling (PAL) is a powerful technique in chemical biology and chemical
proteomics, and has been successfully demonstrated on a variety of non-covalent molecular …

Chronic myeloid leukaemia (CML) is a myeloproliferative disorder arising in the
haemopoietic stem cell (HSC) compartment. This disease is characterised by a reciprocal t …

We review insights from computational studies of affinities of ligands binding to proteins. The
power of structural biology is in translating knowledge of protein structures into insights …

Epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors gefitinib and erlotinib are
effective therapies for non–small cell lung cancer patients whose tumors harbor somatic …

Bosutinib, a dual Src/Abl tyrosine kinase inhibitor (TKI), has shown potent activity against
chronic myeloid leukemia (CML). This phase 1/2 study evaluated the efficacy and safety of …

In the treatment of chronic myeloid leukemia (CML) with BCR-ABL kinase inhibitors, the
T315I gatekeeper mutant has emerged as resistant to all currently approved agents. This …

Targeted therapies by means of compounds that inhibit a specific target molecule represent
a new perspective in the treatment of cancer. In contrast to conventional chemotherapy …

Raf are conserved, ubiquitous serine/protein kinases discovered as the cellular elements
hijacked by transforming retroviruses. The three mammalian RAF proteins (A, B and CRAF) …

Advances in our understanding of the intricate molecular mechanisms for transformation of a
normal cell to a cancer cell, and the aberrant control of complementary pathways, have …

The BCR‐ABL inhibitor imatinib has revolutionized the treatment of chronic myeloid
leukemia. However, drug resistance caused by kinase domain mutations has necessitated …