Over the past two decades, elucidation of the genetic defects that underlie cancer has
resulted in a plethora of novel targeted cancer drugs. Although these agents can initially be …

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 …

Driver mutations promote initiation and progression of cancer. Pharmacological treatment
can inhibit the action of the mutant protein; however, drug resistance almost invariably …

Background Clinical trials of the KRAS inhibitors adagrasib and sotorasib have shown
promising activity in cancers harboring KRAS glycine-to-cysteine amino acid substitutions at …

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 …

Abstract Epidermal Growth Factor Receptor (EGFR) enacts major roles in the maintenance
of epithelial tissues. However, when EGFR signaling is altered, it becomes the grand …

Chronic myeloid leukemia (CML), caused by constitutively active BCR-ABL1 fusion tyrosine
kinase, has served as a paradigm for successful application of molecularly targeted cancer …

Mammalian target of rapamycin (mTOR) is a serine/threonine kinase that gets inputs from
the amino acids, nutrients, growth factor, and environmental cues to regulate varieties of …

The BCL2 inhibitor venetoclax induces high rates of durable remission in patients with
previously treated chronic lymphocytic leukemia (CLL). However, despite continuous daily …