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Items: 1 to 20 of 128

1.

PLX4032, a selective BRAF(V600E) kinase inhibitor, activates the ERK pathway and enhances cell migration and proliferation of BRAF melanoma cells.

Halaban R, Zhang W, Bacchiocchi A, Cheng E, Parisi F, Ariyan S, Krauthammer M, McCusker JP, Kluger Y, Sznol M.

Pigment Cell Melanoma Res. 2010 Apr;23(2):190-200. doi: 10.1111/j.1755-148X.2010.00685.x. Epub 2010 Feb 10. Erratum in: Pigment Cell Melanoma Res. 2012 May;25(3):402.

2.

Melanomas acquire resistance to B-RAF(V600E) inhibition by RTK or N-RAS upregulation.

Nazarian R, Shi H, Wang Q, Kong X, Koya RC, Lee H, Chen Z, Lee MK, Attar N, Sazegar H, Chodon T, Nelson SF, McArthur G, Sosman JA, Ribas A, Lo RS.

Nature. 2010 Dec 16;468(7326):973-7. doi: 10.1038/nature09626. Epub 2010 Nov 24.

3.

p53 Reactivation by PRIMA-1(Met) (APR-246) sensitises (V600E/K)BRAF melanoma to vemurafenib.

Krayem M, Journe F, Wiedig M, Morandini R, Najem A, Sal├Ęs F, van Kempen LC, Sibille C, Awada A, Marine JC, Ghanem G.

Eur J Cancer. 2016 Mar;55:98-110. doi: 10.1016/j.ejca.2015.12.002. Epub 2016 Jan 17.

PMID:
26790143
4.

The oncogenic BRAF kinase inhibitor PLX4032/RG7204 does not affect the viability or function of human lymphocytes across a wide range of concentrations.

Comin-Anduix B, Chodon T, Sazegar H, Matsunaga D, Mock S, Jalil J, Escuin-Ordinas H, Chmielowski B, Koya RC, Ribas A.

Clin Cancer Res. 2010 Dec 15;16(24):6040-8. doi: 10.1158/1078-0432.CCR-10-1911.

5.

The RAF inhibitor PLX4032 inhibits ERK signaling and tumor cell proliferation in a V600E BRAF-selective manner.

Joseph EW, Pratilas CA, Poulikakos PI, Tadi M, Wang W, Taylor BS, Halilovic E, Persaud Y, Xing F, Viale A, Tsai J, Chapman PB, Bollag G, Solit DB, Rosen N.

Proc Natl Acad Sci U S A. 2010 Aug 17;107(33):14903-8. doi: 10.1073/pnas.1008990107. Epub 2010 Jul 28.

6.

RG7204 (PLX4032), a selective BRAFV600E inhibitor, displays potent antitumor activity in preclinical melanoma models.

Yang H, Higgins B, Kolinsky K, Packman K, Go Z, Iyer R, Kolis S, Zhao S, Lee R, Grippo JF, Schostack K, Simcox ME, Heimbrook D, Bollag G, Su F.

Cancer Res. 2010 Jul 1;70(13):5518-27. doi: 10.1158/0008-5472.CAN-10-0646. Epub 2010 Jun 15. Erratum in: Cancer Res. 2010 Nov 15;70(22):9527.

7.

The BRAF(V600E) inhibitor, PLX4032, increases type I collagen synthesis in melanoma cells.

Jenkins MH, Croteau W, Mullins DW, Brinckerhoff CE.

Matrix Biol. 2015 Oct;48:66-77. doi: 10.1016/j.matbio.2015.05.007. Epub 2015 May 16.

8.

Mitogen-activated protein kinase (MAPK) hyperactivation and enhanced NRAS expression drive acquired vemurafenib resistance in V600E BRAF melanoma cells.

Lidsky M, Antoun G, Speicher P, Adams B, Turley R, Augustine C, Tyler D, Ali-Osman F.

J Biol Chem. 2014 Oct 3;289(40):27714-26. doi: 10.1074/jbc.M113.532432. Epub 2014 Jul 25.

9.

SHOC2 and CRAF mediate ERK1/2 reactivation in mutant NRAS-mediated resistance to RAF inhibitor.

Kaplan FM, Kugel CH 3rd, Dadpey N, Shao Y, Abel EV, Aplin AE.

J Biol Chem. 2012 Dec 7;287(50):41797-807. doi: 10.1074/jbc.M112.390906. Epub 2012 Oct 17.

10.

Identification of MET and SRC activation in melanoma cell lines showing primary resistance to PLX4032.

Vergani E, Vallacchi V, Frigerio S, Deho P, Mondellini P, Perego P, Cassinelli G, Lanzi C, Testi MA, Rivoltini L, Bongarzone I, Rodolfo M.

Neoplasia. 2011 Dec;13(12):1132-42.

11.

The CSPG4-specific monoclonal antibody enhances and prolongs the effects of the BRAF inhibitor in melanoma cells.

Yu L, Favoino E, Wang Y, Ma Y, Deng X, Wang X.

Immunol Res. 2011 Aug;50(2-3):294-302. doi: 10.1007/s12026-011-8232-z.

PMID:
21717063
12.

Pharmacodynamic characterization of the efficacy signals due to selective BRAF inhibition with PLX4032 in malignant melanoma.

Tap WD, Gong KW, Dering J, Tseng Y, Ginther C, Pauletti G, Glaspy JA, Essner R, Bollag G, Hirth P, Zhang C, Slamon DJ.

Neoplasia. 2010 Aug;12(8):637-49.

13.

Involvement of superoxide and nitric oxide in BRAF(V600E) inhibitor PLX4032-induced growth inhibition of melanoma cells.

Yu L, Gao LX, Ma XQ, Hu FX, Li CM, Lu Z.

Integr Biol (Camb). 2014 Dec;6(12):1211-7. doi: 10.1039/c4ib00170b. Epub 2014 Nov 3.

PMID:
25363644
14.

Cytostatic activity of adenosine triphosphate-competitive kinase inhibitors in BRAF mutant thyroid carcinoma cells.

Salerno P, De Falco V, Tamburrino A, Nappi TC, Vecchio G, Schweppe RE, Bollag G, Santoro M, Salvatore G.

J Clin Endocrinol Metab. 2010 Jan;95(1):450-5. doi: 10.1210/jc.2009-0373. Epub 2009 Oct 30.

PMID:
19880792
15.

PLX4032: does it keep its promise for metastatic melanoma treatment?

Livingstone E, Zimmer L, Piel S, Schadendorf D.

Expert Opin Investig Drugs. 2010 Nov;19(11):1439-49. doi: 10.1517/13543784.2010.527945. Epub 2010 Oct 14. Review.

PMID:
20942773
16.

Clinical efficacy of a RAF inhibitor needs broad target blockade in BRAF-mutant melanoma.

Bollag G, Hirth P, Tsai J, Zhang J, Ibrahim PN, Cho H, Spevak W, Zhang C, Zhang Y, Habets G, Burton EA, Wong B, Tsang G, West BL, Powell B, Shellooe R, Marimuthu A, Nguyen H, Zhang KY, Artis DR, Schlessinger J, Su F, Higgins B, Iyer R, D'Andrea K, Koehler A, Stumm M, Lin PS, Lee RJ, Grippo J, Puzanov I, Kim KB, Ribas A, McArthur GA, Sosman JA, Chapman PB, Flaherty KT, Xu X, Nathanson KL, Nolop K.

Nature. 2010 Sep 30;467(7315):596-9. doi: 10.1038/nature09454.

17.

PI3'-kinase inhibition forestalls the onset of MEK1/2 inhibitor resistance in BRAF-mutated melanoma.

Deuker MM, Marsh Durban V, Phillips WA, McMahon M.

Cancer Discov. 2015 Feb;5(2):143-53. doi: 10.1158/2159-8290.CD-14-0856. Epub 2014 Dec 3.

18.

Identification of PLX4032-resistance mechanisms and implications for novel RAF inhibitors.

Choi J, Landrette SF, Wang T, Evans P, Bacchiocchi A, Bjornson R, Cheng E, Stiegler AL, Gathiaka S, Acevedo O, Boggon TJ, Krauthammer M, Halaban R, Xu T.

Pigment Cell Melanoma Res. 2014 Mar;27(2):253-62. doi: 10.1111/pcmr.12197. Epub 2014 Jan 6.

19.

Pan-erbB inhibition potentiates BRAF inhibitors for melanoma treatment.

Ng YK, Lee JY, Supko KM, Khan A, Torres SM, Berwick M, Ho J, Kirkwood JM, Siegfried JM, Stabile LP.

Melanoma Res. 2014 Jun;24(3):207-18. doi: 10.1097/CMR.0000000000000060.

20.

Specifically targeting ERK1 or ERK2 kills melanoma cells.

Qin J, Xin H, Nickoloff BJ.

J Transl Med. 2012 Jan 25;10:15. doi: 10.1186/1479-5876-10-15.

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