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Items: 1 to 20 of 467

1.

Preclinical efficacy of a RAF inhibitor that evades paradoxical MAPK pathway activation in protein kinase BRAF-mutant lung cancer.

Okimoto RA, Lin L, Olivas V, Chan E, Markegard E, Rymar A, Neel D, Chen X, Hemmati G, Bollag G, Bivona TG.

Proc Natl Acad Sci U S A. 2016 Nov 22;113(47):13456-13461. Epub 2016 Nov 9.

2.

RAF inhibitors that evade paradoxical MAPK pathway activation.

Zhang C, Spevak W, Zhang Y, Burton EA, Ma Y, Habets G, Zhang J, Lin J, Ewing T, Matusow B, Tsang G, Marimuthu A, Cho H, Wu G, Wang W, Fong D, Nguyen H, Shi S, Womack P, Nespi M, Shellooe R, Carias H, Powell B, Light E, Sanftner L, Walters J, Tsai J, West BL, Visor G, Rezaei H, Lin PS, Nolop K, Ibrahim PN, Hirth P, Bollag G.

Nature. 2015 Oct 22;526(7574):583-6. doi: 10.1038/nature14982. Epub 2015 Oct 14.

PMID:
26466569
3.

PLX8394, a new generation BRAF inhibitor, selectively inhibits BRAF in colonic adenocarcinoma cells and prevents paradoxical MAPK pathway activation.

Tutuka CSA, Andrews MC, Mariadason JM, Ioannidis P, Hudson C, Cebon J, Behren A.

Mol Cancer. 2017 Jun 28;16(1):112. doi: 10.1186/s12943-017-0684-x.

4.

Clinical Acquired Resistance to RAF Inhibitor Combinations in BRAF-Mutant Colorectal Cancer through MAPK Pathway Alterations.

Ahronian LG, Sennott EM, Van Allen EM, Wagle N, Kwak EL, Faris JE, Godfrey JT, Nishimura K, Lynch KD, Mermel CH, Lockerman EL, Kalsy A, Gurski JM Jr, Bahl S, Anderka K, Green LM, Lennon NJ, Huynh TG, Mino-Kenudson M, Getz G, Dias-Santagata D, Iafrate AJ, Engelman JA, Garraway LA, Corcoran RB.

Cancer Discov. 2015 Apr;5(4):358-67. doi: 10.1158/2159-8290.CD-14-1518. Epub 2015 Feb 11.

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.

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.

Long-term vemurafenib treatment drives inhibitor resistance through a spontaneous KRAS G12D mutation in a BRAF V600E papillary thyroid carcinoma model.

Danysh BP, Rieger EY, Sinha DK, Evers CV, Cote GJ, Cabanillas ME, Hofmann MC.

Oncotarget. 2016 May 24;7(21):30907-23. doi: 10.18632/oncotarget.9023.

8.

Resistance to selective BRAF inhibition can be mediated by modest upstream pathway activation.

Su F, Bradley WD, Wang Q, Yang H, Xu L, Higgins B, Kolinsky K, Packman K, Kim MJ, Trunzer K, Lee RJ, Schostack K, Carter J, Albert T, Germer S, Rosinski J, Martin M, Simcox ME, Lestini B, Heimbrook D, Bollag G.

Cancer Res. 2012 Feb 15;72(4):969-78. doi: 10.1158/0008-5472.CAN-11-1875. Epub 2011 Dec 28.

9.

Overcoming acquired BRAF inhibitor resistance in melanoma via targeted inhibition of Hsp90 with ganetespib.

Acquaviva J, Smith DL, Jimenez JP, Zhang C, Sequeira M, He S, Sang J, Bates RC, Proia DA.

Mol Cancer Ther. 2014 Feb;13(2):353-63. doi: 10.1158/1535-7163.MCT-13-0481. Epub 2014 Jan 7.

10.

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.

11.

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.

12.

Discovery of a novel pan-RAF inhibitor with potent anti-tumor activity in preclinical models of BRAFV600E mutant cancer.

Hong SP, Ahn SK.

Life Sci. 2017 Aug 15;183:37-44. doi: 10.1016/j.lfs.2017.06.021. Epub 2017 Jun 21.

PMID:
28645859
13.

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
14.

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
15.

EGFR-Mediated Reactivation of MAPK Signaling Induces Acquired Resistance to GSK2118436 in BRAF V600E-Mutant NSCLC Cell Lines.

Kim SM, Kim H, Jang KW, Kim MH, Sohn J, Yun MR, Kang HN, Kang CW, Kim HR, Lim SM, Moon YW, Kim JH, Paik S, Cho BC.

Mol Cancer Ther. 2016 Jul;15(7):1627-36. doi: 10.1158/1535-7163.MCT-15-0375. Epub 2016 May 11. Retraction in: Mol Cancer Ther. 2017 Oct;16(10 ):2326.

16.

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.

17.

The MEK1/2 Inhibitor AZD6244 Sensitizes BRAF-Mutant Thyroid Cancer to Vemurafenib.

Song H, Zhang J, Ning L, Zhang H, Chen D, Jiao X, Zhang K.

Med Sci Monit. 2018 May 8 [revised 2018 Jan 1];24:3002-3010. doi: 10.12659/MSM.910084.

18.

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.

19.

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.

20.

Unresponsiveness of colon cancer to BRAF(V600E) inhibition through feedback activation of EGFR.

Prahallad A, Sun C, Huang S, Di Nicolantonio F, Salazar R, Zecchin D, Beijersbergen RL, Bardelli A, Bernards R.

Nature. 2012 Jan 26;483(7387):100-3. doi: 10.1038/nature10868.

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