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Biomap#42

Title: List of MEK inhibitors
 
Legend: The RAS / RAF / MEK / ERK pathway is involved in several cell activities (including cell proliferation and survival) and is overactive (often through gain-of-function mutations of RAS and/or RAF family members) in many human cancers, including melanoma [1,2]: accordingly, it is a target for molecularly targeted agents (MTA). MEK1 (MAPK/ERK kinase 1, MAP2K1, MAPKK1) and MEK2 (MAPK/ERK kinase 2, MAP2K2, MAPKK2) are mitogen activated protein kinases (MAPK) that activate extracellular signal regulated kinase -1 (ERK1, MAPK3) and -2 (ERK2, MAPK1). The best characterized MEK inhibitors are AZD6244 (ARRY-142886), CI-1040, PD098059, PD0325901, PD184352 and U0126, with the first three of them having entered the clinical phase of experimentation [3,4]. REFERENCES: [1] Haluska FG et al, Curr Oncol Rep 2006, 8:400-5. [2] Fecher LA et al, J Clin Oncol 2007, 25:1606-20. [3] Kohno M et al, Ann Med 2006, 38:200-11. [4] Wang JY et al, Curr Top Med Chem 2007, 7:1364-78.
Author: The MMMP Team (updated: Jan 2008)

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