Monday, May 15, 2000
Last week's eight-compound deal between Novartis Pharma AG
and Vertex Pharmaceuticals Inc. illustrates the building competition in the
kinase field, as a growing number of biotech and pharmaceutical companies are
pursuing the development of broad libraries of compounds that inhibit protein
kinase targets. While a few small molecule kinase inhibitors are in clinical
testing, the number of compounds and specific kinase targets is likely to increase
Kinases have become popular targets based on their involvement
in most cellular functions and hence most diseases. Kinases are cellular signaling
enzymes that catalyze the addition of a phosphorus group onto another protein
(phosphorylation), usually to regulate the activity of the substrate protein.
The kinase superfamily includes both receptors and cytoplasmic proteins that
phosphorylate either tyrosine residues or serine/threonine residues on their
targets. First identified as oncogenes activated by retroviruses, the kinase
superfamily is now estimated to contain more than 1,000 members involved in
a diverse array of signal transduction pathways.