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Biomap#43

Title: List of PI3K inhibitors
 
Legend: Phosphatidyl inositol 3-kinases (PI3K) regulate different cell functions including survival, proliferation, metabolic control, cytoskeletal rearrangement and migration. Deregulation of the PI3K pathway occurs frequently in cancers (including melanoma) by activating mutations in growth factor receptors or the PIK3CA locus (coding for PI3K alpha), by loss of function mutations or hypermethylation of the PTEN gene (lipid phosphatase and tensin homolog deleted in chromosome ten), by the up-regulation of protein kinase B (PKB / Akt), or the impairment of the tuberous sclerosis complex (TSC1, TSC2). All these events can lead to cell growth and proliferation, and have thus prompted the development of agents targeting the PI3K pathway. Some PI3K inhibitors currently under development are the following: AS041164, Deguelin, Halenaquinone, IC486068, LY294002, PX-866, SF1126, WAY-266175, Wortmannin, ZSTK474. REFERENCES: [1] Marone R, Biochim Biophys Acta 2007, 1784:159-85. [2] Lopiccolo J, Drug Resist Updat 2008, 11:32-50. [3] Jiang BH, Biochim Biophys Acta 2007, 1784:150-8. [4] Haluska F, Semin Oncol 2007, 34:546-54.
Author: The MMMP Team (updated: Jan 2008)

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