Kinase Inhibitors

Kinases are a large class of enzymes that are crucial to the proper operation of many cellular processes including cell growth, metabolism and apoptosis. Protein kinases use ATP to phosphorylate proteins within a cell, modifying the target protein’s function in some manner. Since abnormally functioning protein kinases are involved in the pathogenesis of many diseases, these enzymes are often drug therapy targets. Protein kinase inhibitors are small molecules, polypeptides, or antibodies that block or diminish kinase function. In research, they are often used in kinase inhibition assays, ultimately leading to the identification of appropriate therapeutic targets and the development of effective treatments. There is a growing list of FDA-approved kinase inhibitor drugs that treat a myriad of diseases such as cancer, autoimmune disorders, inflammatory disorders, and glaucoma. Some examples include:

MEK Inhibitors - BRAF-V600E positive advanced melanoma (Trametinib)

JAK Inhibitors - myelofibrosis (Ruxolitinib)

PI3K Inhibitors - Chronic lymphocytic leukemia (Idelalisib)