Protein Information

Name mitogen activated protein kinase (protein family or complex)
Synonyms MAPK; mitogen activated protein kinase; mitogen activated protein kinases

Compound Information

Name diphenylamine
CAS

Reference List

PubMed Abstract RScore(About this table)
16944149 Brown AP, Carlson TC, Loi CM, Graziano MJ: Pharmacodynamic and toxicokinetic evaluation of the novel MEK inhibitor, PD0325901, in the rat following oral and intravenous administration. Cancer Chemother Pharmacol. 2007 Apr;59(5):671-9. Epub 2006 Aug 31.


The MEK-mitogen-activated protein kinase (MAPK) signal transduction pathway is involved with numerous cellular processes including cell growth and differentiation.
2(0,0,0,2) Details
19929595 Huang W, Yang AH, Matsumoto D, Collette W, Marroquin L, Ko M, Aguirre S, Younis HS: PD0325901, a mitogen-activated protein kinase kinase inhibitor, produces ocular toxicity in a rabbit animal model of retinal vein occlusion. J Ocul Pharmacol Ther. 2009 Dec;25(6):519-30.

2(0,0,0,2) Details
18381570 Leboeuf R, Baumgartner JE, Benezra M, Malaguarnera R, Solit D, Pratilas CA, Rosen N, Knauf JA, Fagin JA: BRAFV600E mutation is associated with preferential sensitivity to mitogen-activated protein kinase kinase inhibition in thyroid cancer cell lines. J Clin Endocrinol Metab. 2008 Jun;93(6):2194-201. Epub 2008 Apr 1.

2(0,0,0,2) Details
18559577 Sebolt-Leopold JS: Advances in the development of cancer therapeutics directed against the RAS-mitogen-activated protein kinase pathway. Clin Cancer Res. 2008 Jun 15;14(12):3651-6.


Among mammalian mitogen-activated protein kinase (MAPK) signaling cascades, the extracellular signal-related kinase (ERK) pathway has received the most attention in the oncology drug discovery arena.
2(0,0,0,2) Details
19401449 Wee S, Jagani Z, Xiang KX, Loo A, Dorsch M, Yao YM, Sellers WR, Lengauer C, Stegmeier F: PI3K pathway activation mediates resistance to MEK inhibitors in KRAS mutant cancers. Cancer Res. 2009 May 15;69(10):4286-93. Epub 2009 Apr 28.


RAS signals through multiple effector pathways, including the RAF/mitogen-activated protein kinase (MAPK)/extracellular signal-regulated kinase (ERK) kinase (MEK)/ERK MAPK and phosphatidylinositol 3-kinase (PI3K)-AKT signaling cascades.
1(0,0,0,1) Details
19706763 Iverson C, Larson G, Lai C, Yeh LT, Dadson C, Weingarten P, Appleby T, Vo T, Maderna A, Vernier JM, Hamatake R, Miner JN, Quart B: RDEA119/BAY 869766: a potent, selective, allosteric inhibitor of MEK1/2 for the treatment of cancer. Cancer Res. 2009 Sep 1;69(17):6839-47. Epub 2009 Aug 25.


The RAS-RAF-mitogen-activated protein kinase/extracellular signal-regulated kinase (ERK) kinase (MEK)-ERK pathway provides numerous opportunities for targeted oncology therapeutics.
1(0,0,0,1) Details
16273091 Solit DB, Garraway LA, Pratilas CA, Sawai A, Getz G, Basso A, Ye Q, Lobo JM, She Y, Osman I, Golub TR, Sebolt-Leopold J, Sellers WR, Rosen N: BRAF mutation predicts sensitivity to MEK inhibition. . Nature. 2006 Jan 19;439(7074):358-62. Epub 2005 Nov 6.


The kinase pathway comprising RAS, RAF, mitogen-activated protein kinase kinase (MEK) and extracellular signal regulated kinase (ERK) is activated in most human tumours, often through gain-of-function mutations of RAS and RAF family members.
1(0,0,0,1) Details
18583568 Lunghi P, Giuliani N, Mazzera L, Lombardi G, Ricca M, Corradi A, Cantoni AM, Salvatore L, Riccioni R, Costanzo A, Testa U, Levrero M, Rizzoli V, Bonati A: Targeting MEK/MAPK signal transduction module potentiates ATO-induced apoptosis in multiple myeloma cells through multiple signaling pathways. Blood. 2008 Sep 15;112(6):2450-62. Epub 2008 Jun 26.

1(0,0,0,1) Details
18497825 Ying QL, Wray J, Nichols J, Batlle-Morera L, Doble B, Woodgett J, Cohen P, Smith A: The ground state of embryonic stem cell self-renewal. Nature. 2008 May 22;453(7194):519-23.


Self-renewal is enabled by the elimination of differentiation-inducing signalling from mitogen-activated protein kinase.
1(0,0,0,1) Details
18056475 Solit DB, Santos E, Pratilas CA, Lobo J, Moroz M, Cai S, Blasberg R, Sebolt-Leopold J, Larson S, Rosen N: 3'-deoxy-3'-[18F] fluorothymidine positron emission tomography is a sensitive method for imaging the response of BRAF-dependent tumors to MEK inhibition. Cancer Res. 2007 Dec 1;67(23):11463-9.


These tumors are very sensitive to pharmacologic inhibition of mitogen-activated protein kinase/extracellular signal-regulated kinase kinase (MEK), which causes loss of D-cyclin expression, hypophosphorylation of Rb, and G (1) arrest.
1(0,0,0,1) Details
17987349 Wentz SC, Wu H, Yip-Schneider MT, Hennig M, Klein PJ, Sebolt-Leopold J, Schmidt CM: Targeting MEK is effective chemoprevention of hepatocellular carcinoma in TGF-alpha-transgenic mice. J Gastrointest Surg. 2008 Jan;12(1):30-7. Epub 2007 Nov 7.


Previous studies from our lab provide evidence for altered mitogen-activated protein kinase and extracellular signal-regulated kinase kinase (MEK) signaling in HCC pathogenesis.
1(0,0,0,1) Details