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Items: 1 to 20 of 137

1.

Discovery of a selective inhibitor of oncogenic B-Raf kinase with potent antimelanoma activity.

Tsai J, Lee JT, Wang W, Zhang J, Cho H, Mamo S, Bremer R, Gillette S, Kong J, Haass NK, Sproesser K, Li L, Smalley KS, Fong D, Zhu YL, Marimuthu A, Nguyen H, Lam B, Liu J, Cheung I, Rice J, Suzuki Y, Luu C, Settachatgul C, Shellooe R, Cantwell J, Kim SH, Schlessinger J, Zhang KY, West BL, Powell B, Habets G, Zhang C, Ibrahim PN, Hirth P, Artis DR, Herlyn M, Bollag G.

Proc Natl Acad Sci U S A. 2008 Feb 26;105(8):3041-6. doi: 10.1073/pnas.0711741105. Epub 2008 Feb 19.

2.

Targeting BRAFV600E with PLX4720 displays potent antimigratory and anti-invasive activity in preclinical models of human thyroid cancer.

Nucera C, Nehs MA, Nagarkatti SS, Sadow PM, Mekel M, Fischer AH, Lin PS, Bollag GE, Lawler J, Hodin RA, Parangi S.

Oncologist. 2011;16(3):296-309. doi: 10.1634/theoncologist.2010-0317. Epub 2011 Feb 25.

3.

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.

4.

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.

5.

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.

6.

EBI-907, a novel BRAF(V600E) inhibitor, has potent oral anti-tumor activity and a broad kinase selectivity profile.

Zhang J, Lu B, Liu D, Shen R, Yan Y, Yang L, Zhang M, Zhang L, Cao G, Cao H, Fu B, Gong A, Sun Q, Wan H, Zhang L, Tao W, Cao J.

Cancer Biol Ther. 2016;17(2):199-207. doi: 10.1080/15384047.2016.1139231. Epub 2016 Jan 25.

7.

3'-Deoxy-3'-18F-fluorothymidine PET predicts response to (V600E)BRAF-targeted therapy in preclinical models of colorectal cancer.

McKinley ET, Smith RA, Zhao P, Fu A, Saleh SA, Uddin MI, Washington MK, Coffey RJ, Manning HC.

J Nucl Med. 2013 Mar;54(3):424-30. doi: 10.2967/jnumed.112.108456. Epub 2013 Jan 22.

8.

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.

9.

PLX4032, a potent inhibitor of the B-Raf V600E oncogene, selectively inhibits V600E-positive melanomas.

Lee JT, Li L, Brafford PA, van den Eijnden M, Halloran MB, Sproesser K, Haass NK, Smalley KS, Tsai J, Bollag G, Herlyn M.

Pigment Cell Melanoma Res. 2010 Dec;23(6):820-7. doi: 10.1111/j.1755-148X.2010.00763.x.

10.

Discovery of EBI-907: A highly potent and orally active B-Raf(V600E) inhibitor for the treatment of melanoma and associated cancers.

Lu B, Cao H, Cao J, Huang S, Hu Q, Liu D, Shen R, Shen X, Tao W, Wan H, Wang D, Yan Y, Yang L, Zhang J, Zhang L, Zhang L, Zhang M.

Bioorg Med Chem Lett. 2016 Feb 1;26(3):819-23. doi: 10.1016/j.bmcl.2015.12.086. Epub 2015 Dec 24.

PMID:
26739779
11.

Genotype-dependent cooperation of ionizing radiation with BRAF inhibition in BRAF V600E-mutated carcinomas.

Dasgupta T, Haas-Kogan DA, Yang X, Olow A, Yang DX, Gragg A, Orloff LA, Yom SS.

Invest New Drugs. 2013 Oct;31(5):1136-41. doi: 10.1007/s10637-013-9928-9. Epub 2013 Jan 26.

PMID:
23354848
12.

B-Raf(V600E) and thrombospondin-1 promote thyroid cancer progression.

Nucera C, Porrello A, Antonello ZA, Mekel M, Nehs MA, Giordano TJ, Gerald D, Benjamin LE, Priolo C, Puxeddu E, Finn S, Jarzab B, Hodin RA, Pontecorvi A, Nose V, Lawler J, Parangi S.

Proc Natl Acad Sci U S A. 2010 Jun 8;107(23):10649-54. doi: 10.1073/pnas.1004934107. Epub 2010 May 24.

13.

Apoptosis of human melanoma cells induced by inhibition of B-RAFV600E involves preferential splicing of bimS.

Jiang CC, Lai F, Tay KH, Croft A, Rizos H, Becker TM, Yang F, Liu H, Thorne RF, Hersey P, Zhang XD.

Cell Death Dis. 2010 Sep 2;1:e69. doi: 10.1038/cddis.2010.48.

14.

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.

15.

MEK-independent survival of B-RAFV600E melanoma cells selected for resistance to apoptosis induced by the RAF inhibitor PLX4720.

Jiang CC, Lai F, Thorne RF, Yang F, Liu H, Hersey P, Zhang XD.

Clin Cancer Res. 2011 Feb 15;17(4):721-30. doi: 10.1158/1078-0432.CCR-10-2225. Epub 2010 Nov 18.

16.

Glutamatergic pathway targeting in melanoma: single-agent and combinatorial therapies.

Lee HJ, Wall BA, Wangari-Talbot J, Shin SS, Rosenberg S, Chan JL, Namkoong J, Goydos JS, Chen S.

Clin Cancer Res. 2011 Nov 15;17(22):7080-92. doi: 10.1158/1078-0432.CCR-11-0098. Epub 2011 Aug 15. Erratum in: Clin Cancer Res. 2012 Mar 1;18(5):1484.

17.

Host immunity contributes to the anti-melanoma activity of BRAF inhibitors.

Knight DA, Ngiow SF, Li M, Parmenter T, Mok S, Cass A, Haynes NM, Kinross K, Yagita H, Koya RC, Graeber TG, Ribas A, McArthur GA, Smyth MJ.

J Clin Invest. 2013 Mar;123(3):1371-81. doi: 10.1172/JCI66236. Epub 2013 Feb 1. Erratum in: J Clin Invest. 2013 Jul 1;123(7):3182. J Clin Invest. 2016 Jan;126(1):402-3.

18.

COT drives resistance to RAF inhibition through MAP kinase pathway reactivation.

Johannessen CM, Boehm JS, Kim SY, Thomas SR, Wardwell L, Johnson LA, Emery CM, Stransky N, Cogdill AP, Barretina J, Caponigro G, Hieronymus H, Murray RR, Salehi-Ashtiani K, Hill DE, Vidal M, Zhao JJ, Yang X, Alkan O, Kim S, Harris JL, Wilson CJ, Myer VE, Finan PM, Root DE, Roberts TM, Golub T, Flaherty KT, Dummer R, Weber BL, Sellers WR, Schlegel R, Wargo JA, Hahn WC, Garraway LA.

Nature. 2010 Dec 16;468(7326):968-72. doi: 10.1038/nature09627. Epub 2010 Nov 24.

19.

BGB-283, a Novel RAF Kinase and EGFR Inhibitor, Displays Potent Antitumor Activity in BRAF-Mutated Colorectal Cancers.

Tang Z, Yuan X, Du R, Cheung SH, Zhang G, Wei J, Zhao Y, Feng Y, Peng H, Zhang Y, Du Y, Hu X, Gong W, Liu Y, Gao Y, Liu Y, Hao R, Li S, Wang S, Ji J, Zhang L, Li S, Sutton D, Wei M, Zhou C, Wang L, Luo L.

Mol Cancer Ther. 2015 Oct;14(10):2187-97. doi: 10.1158/1535-7163.MCT-15-0262. Epub 2015 Jul 24.

20.

Survival advantage combining a BRAF inhibitor and radiation in BRAF V600E-mutant glioma.

Dasgupta T, Olow AK, Yang X, Hashizume R, Nicolaides TP, Tom M, Aoki Y, Berger MS, Weiss WA, Stalpers LJ, Prados M, James CD, Mueller S, Haas-Kogan DA.

J Neurooncol. 2016 Feb;126(3):385-93. doi: 10.1007/s11060-015-1939-2. Epub 2015 Sep 18. Erratum in: J Neurooncol. 2016 Feb;126(3):395.

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