Serine/threonine-protein kinases (EC 188.8.131.52) are enzyme or protein that has hydroxyl (OH) group in the side chain. Phosphorylation in serine or threonine residues may cause changes in the function of the target protein. Those drugs/ligands that inhibit phosphorylating activity of these kinases are called serine/threonine protein kinases inhibitors. Serine/threonine kinase receptors are a family of transmembrane receptors containing intracellular serine/threonine kinase domains that respond to a few cytokines including the transforming growth factor beta and bone morphogenic proteins families.
According to the enzyme classification system, E.C. 2.7.11 protein-serine/threonine kinases have subclasses such as B-RAF inhibitors, mitogen-activated protein kinase inhibitors, polo-like kinase 1 inhibitors, protein-kinase-b-alpha-inhibitors, and calmodulin-dependent-protein-kinase-III-inhibitors.
The serine/threonine protein kinase inhibitors pipeline has more than 40 drugs. In pipeline analysis, drugs are analyzed on the basis of route of administration and molecule type. The pipeline is also analyzed on the basis of monotherapy and combination therapy, and different clinical phases including phase III, phase II, phase I and preclinical stage.
ASN007, an under-development drug candidate of Asana BioSciences LLC, is in preclinical stage of development for the treatment of melanoma, colon and lung cancer. Preclinical study is also known as animal study. It is done before testing a drug in people to find out the toxicity profile of the drug. Preclinical study is of two types, including in vitro and in vivo. There are 9 serine/threonine-protein kinase inhibitor drugs in preclinical trial.
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Pipeline analysis provides description about the key companies which are developing serine/threonine-protein kinase inhibitors drugs. Some of the key players actively involved in the research and development are Bayer AG, AstraZeneca plc, F. Hoffmann-La Roche AG, Asana BioSciences, LLC, GlaxoSmithKline plc and Eli Lilly and Company.
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