Janus kinase drugs may also work well in rheumatoid arthritis a potentially even bigger market.
AstraZeneca itself is building an arsenal of anti-cancer pills known as tyrosine kinase inhibitors.
By then scientists had discovered hundreds of kinase genes scattered throughout the human DNA sequence.
The big sleeper is tasocitinib, a so-called janus kinase inhibitor, for rheumatoid arthritis and psoriasis.
Protein-kinase genes, whose products are involved in intracellular signalling, are similarly concentrated on chromosome 1.
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By 1999 Zeneca had devised a drug, Iressa, that interrupted the pathways between EGF and tyrosine kinase.
When EGF docks on a receptor, it signals to an enzyme called tyrosine kinase to regulate cell growth.
Blocking HMG CoA reductase not only prevents the formation of cholesterol, but also the creation of Rho kinase.
Recent examples: molecules to target drug-resistant bacteria and a kinase inhibitor to zap the enzyme responsible for tumor growth.
About this time Vertex biologist Michael Su became curious about a related kinase that plays a role in strokes.
The researchers found the enzyme, pyruvate kinase, switches between providing fuel for existing cells and forming material for new cells.
In the mid-1990s Vertex chemists crafted compounds that block a key kinase protein that unleashes toxic immune-system molecules in arthritic joints.
AstraZeneca is in midstage trials with 180 melanoma patients for a drug that hits a related target called mitogen-activated protein kinase kinase.
The compound targeted the protein kinase C-alpha, one of a family of 13 known proteins that relay information from one to another.
The researchers tripled the number of protein-kinase genes known from this chromosome.
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If it worked, Vertex would have a huge lead in kinase-blockers, but the firm lacked the money to mount a large-scale program alone.
The two kinases were so similar that Vertex researchers devised a prototype blocker for the second kinase in a year--half the normal time.
When this compound is present in sufficient amounts, the pyruvate kinase enzyme stops generating fuel for cells and instead pushes cells towards growing and dividing.
Inycte and Novartis are competing with numerous other drug companies including AstraZeneca, Eli Lilly, and Sanofi-Aventis (which is acquiring privately held Targegen and its janus kinase drug).
Today, AVEO (name was changed in 2005) has an interesting multi-kinase inhibitor tivozanib in Phase 3 for renal cell cancer, and their second program is an anti-HGF mAb.
He found they also activate an enzyme called Rho kinase, which negatively affects the way that arteries expand and contract and increasing the inflammation within cholesterol plaques in the artery wall.
AstraZeneca (nyse: AZN - news - people ) is in midstage trials with 180 melanoma patients for a drug that hits a related target called mitogen-activated protein kinase kinase.
The clincher: Once a prototype drug works against one kinase, Vertex figures it can easily tweak the compound to inhibit other siblings in the kinase family--and then attack other protein groups, as well.
Its scientific founders, all members of the prestigious National Academies of Science, include experts who helped discover the PI3 kinase mechanism that is a key drug target for companies like Merck and Pfizer.
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On the FDA's Fast Track and in phase III testing is the company's BAY 43-9006, a small molecule RAF kinase and VEGF inhibitor that inhibits tumor growth for patients with metastatic renal cell carcinoma (advanced kidney cancer).
Peroxynitrites contribute to the hyperphosphorylation of tau proteins by oxidating g-protein coupled receptors and trysoine kinase receptors preventing protein kinase C and AKT from inactivating the enzyme GSK3 which is necessary to prevent the hyperphosphorylation of tau proteins.
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Professor Seth Grant, an expert in the molecular mechanism of learning and memory at Edinburgh University, told BBC News Online that PKM was a particular version of an enzyme called protein kinase C (PKC) that had long been implicated in learning.
Separately, Pfizer said that the Food and Drug Administration has approved Xalkori capsules, which the company calls the first-ever drug targeting anaplastic lymphoma kinase, or ALK, for the treatment of locally advanced or metastatic non-small cell lung cancer that is ALK-positive.
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