The human genome comprises more than 500 protein kinases including serine/threonine,
tyrosine and dual specificity kinases. 1, 2 Because of the important physiological and …

Protein kinases are fascinating biological catalysts with a rapidly expanding knowledge
base, a growing appreciation in cell regulatory control, and an ascendant role in successful …

In an effort to find new pharmacological modalities to overcome resistance to ATP-binding-
site inhibitors of Bcr–Abl, we recently reported the discovery of GNF-2, a selective allosteric …

Protein kinases targeted by small-molecule inhibitors develop resistance through mutation
of the'gatekeeper'threonine residue of the active site. Here we show that the gatekeeper …

Ba/F3 cells are an increasingly popular tool in kinase drug discovery. The ability to test the
transforming capacity of newly identified kinase mutations, and to profile drug candidates …

The introduction of the BCR–ABL kinase inhibitor imatinib mesylate (Gleevec; Novartis)
revolutionized the treatment of chronic myeloid leukaemia (CML). However, most patients …

DNA-templated organic synthesis enables the translation of DNA sequences into synthetic
small-molecule libraries suitable for in vitro selection. Previously, we described the DNA …

Protein kinases are obvious drug targets against cancer, owing to their central role in
cellular regulation. Since the discovery of Gleevec, a potent and specific inhibitor of Abl …

Kinases have emerged as ubiquitous but highly challenging targets for drug discovery. The
human genome has 518 kinases1 and many of these play critical roles in cell growth and …

Myeloproliferative disorders (MPDs) constitute a group of hematopoietic malignancies that
feature enhanced proliferation and survival of one or more myeloid lineage cells. William …