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Items: 1 to 20 of 129

1.

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.

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.

Differential sensitivity of melanoma cell lines with BRAFV600E mutation to the specific Raf inhibitor PLX4032.

S√łndergaard JN, Nazarian R, Wang Q, Guo D, Hsueh T, Mok S, Sazegar H, MacConaill LE, Barretina JG, Kehoe SM, Attar N, von Euw E, Zuckerman JE, Chmielowski B, Comin-Anduix B, Koya RC, Mischel PS, Lo RS, Ribas A.

J Transl Med. 2010 Apr 20;8:39. doi: 10.1186/1479-5876-8-39.

4.

RAF inhibitor resistance is mediated by dimerization of aberrantly spliced BRAF(V600E).

Poulikakos PI, Persaud Y, Janakiraman M, Kong X, Ng C, Moriceau G, Shi H, Atefi M, Titz B, Gabay MT, Salton M, Dahlman KB, Tadi M, Wargo JA, Flaherty KT, Kelley MC, Misteli T, Chapman PB, Sosman JA, Graeber TG, Ribas A, Lo RS, Rosen N, Solit DB.

Nature. 2011 Nov 23;480(7377):387-90. doi: 10.1038/nature10662.

5.

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.

6.

Inhibition of mutant BRAF splice variant signaling by next-generation, selective RAF inhibitors.

Basile KJ, Le K, Hartsough EJ, Aplin AE.

Pigment Cell Melanoma Res. 2014 May;27(3):479-84. doi: 10.1111/pcmr.12218. Epub 2014 Feb 10.

7.

Reversing melanoma cross-resistance to BRAF and MEK inhibitors by co-targeting the AKT/mTOR pathway.

Atefi M, von Euw E, Attar N, Ng C, Chu C, Guo D, Nazarian R, Chmielowski B, Glaspy JA, Comin-Anduix B, Mischel PS, Lo RS, Ribas A.

PLoS One. 2011;6(12):e28973. doi: 10.1371/journal.pone.0028973. Epub 2011 Dec 14.

8.

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.

9.

The MEK1/2 inhibitor AS703026 circumvents resistance to the BRAF inhibitor PLX4032 in human malignant melanoma cells.

Park SJ, Hong SW, Moon JH, Jin DH, Kim JS, Lee CK, Kim KP, Hong YS, Choi EK, Lee JS, Lee JL, Kim TW.

Am J Med Sci. 2013 Dec;346(6):494-8. doi: 10.1097/MAJ.0b013e318298a185.

PMID:
24051957
10.

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.

11.

Adaptive upregulation of FOXD3 and resistance to PLX4032/4720-induced cell death in mutant B-RAF melanoma cells.

Basile KJ, Abel EV, Aplin AE.

Oncogene. 2012 May 10;31(19):2471-9. doi: 10.1038/onc.2011.424. Epub 2011 Sep 26.

12.

Reactivation of mitogen-activated protein kinase (MAPK) pathway by FGF receptor 3 (FGFR3)/Ras mediates resistance to vemurafenib in human B-RAF V600E mutant melanoma.

Yadav V, Zhang X, Liu J, Estrem S, Li S, Gong XQ, Buchanan S, Henry JR, Starling JJ, Peng SB.

J Biol Chem. 2012 Aug 10;287(33):28087-98. doi: 10.1074/jbc.M112.377218. Epub 2012 Jun 22.

13.

The BRAFT1799A mutation confers sensitivity of thyroid cancer cells to the BRAFV600E inhibitor PLX4032 (RG7204).

Xing J, Liu R, Xing M, Trink B.

Biochem Biophys Res Commun. 2011 Jan 28;404(4):958-62. doi: 10.1016/j.bbrc.2010.12.088. Epub 2010 Dec 23.

14.

Association between acquired resistance to PLX4032 (vemurafenib) and ATP-binding cassette transporter expression.

Michaelis M, Rothweiler F, Nerreter T, van Rikxoort M, Zehner R, Dirks WG, Wiese M, Cinatl J Jr.

BMC Res Notes. 2014 Oct 10;7:710. doi: 10.1186/1756-0500-7-710.

15.

A new water soluble MAPK activator exerts antitumor activity in melanoma cells resistant to the BRAF inhibitor vemurafenib.

Graziani G, Artuso S, De Luca A, Muzi A, Rotili D, Scimeca M, Atzori MG, Ceci C, Mai A, Leonetti C, Levati L, Bonanno E, Tentori L, Caccuri AM.

Biochem Pharmacol. 2015 May 1;95(1):16-27. doi: 10.1016/j.bcp.2015.03.004. Epub 2015 Mar 17.

PMID:
25795251
16.

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.

17.

Inhibiting EGF receptor or SRC family kinase signaling overcomes BRAF inhibitor resistance in melanoma.

Girotti MR, Pedersen M, Sanchez-Laorden B, Viros A, Turajlic S, Niculescu-Duvaz D, Zambon A, Sinclair J, Hayes A, Gore M, Lorigan P, Springer C, Larkin J, Jorgensen C, Marais R.

Cancer Discov. 2013 Feb;3(2):158-67. doi: 10.1158/2159-8290.CD-12-0386. Epub 2012 Dec 14.

18.

Incidence of the V600K mutation among melanoma patients with BRAF mutations, and potential therapeutic response to the specific BRAF inhibitor PLX4032.

Rubinstein JC, Sznol M, Pavlick AC, Ariyan S, Cheng E, Bacchiocchi A, Kluger HM, Narayan D, Halaban R.

J Transl Med. 2010 Jul 14;8:67. doi: 10.1186/1479-5876-8-67.

19.

AEBP1 upregulation confers acquired resistance to BRAF (V600E) inhibition in melanoma.

Hu W, Jin L, Jiang CC, Long GV, Scolyer RA, Wu Q, Zhang XD, Mei Y, Wu M.

Cell Death Dis. 2013 Nov 7;4:e914. doi: 10.1038/cddis.2013.441.

20.

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.

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