The FDA approval of imatinib in 2001 was a breakthrough in molecularly targeted cancer
therapy and heralded the emergence of kinase inhibitors as a key drug class in the oncology …

Protein kinases regulate nearly all aspects of cell life, and alterations in their expression, or
mutations in their genes, cause cancer and other diseases. Here, we review the remarkable …

Kinase inhibitor research is a comparatively recent branch of medicinal chemistry and
pharmacology and the first small‐molecule kinase inhibitor, imatinib, was approved for …

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 …

Highlights•A dramatic increase in the approval of small molecule kinase inhibitors
(SMKIs).•The molecular weight of most approved SMKIs is in the range of 400–600.•The …

The central role of dysregulated kinase activity in the etiology of progressive disorders,
including cancer, has fostered incremental efforts on drug discovery programs over the past …

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 …

Publicly available kinase inhibitors have been analyzed in detail. Nearly 19000 inhibitors
have been identified with activity against 266 different kinases. Thus, about half of the …

The success of the tyrosine kinase imatinib inhibitor (Gleevec, STI571) in treating chronic
myeloid leukemia as well as other selected cancers has greatly increased optimism for the …

Highlights•Summarized the diverse types of warheads across the human
kinome.•Highlighted facile covalent reactive functional groups which bind protein …