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Items: 1 to 20 of 652

1.

RAF inhibitors transactivate RAF dimers and ERK signalling in cells with wild-type BRAF.

Poulikakos PI, Zhang C, Bollag G, Shokat KM, Rosen N.

Nature. 2010 Mar 18;464(7287):427-30. doi: 10.1038/nature08902.

2.

RAF inhibitors prime wild-type RAF to activate the MAPK pathway and enhance growth.

Hatzivassiliou G, Song K, Yen I, Brandhuber BJ, Anderson DJ, Alvarado R, Ludlam MJ, Stokoe D, Gloor SL, Vigers G, Morales T, Aliagas I, Liu B, Sideris S, Hoeflich KP, Jaiswal BS, Seshagiri S, Koeppen H, Belvin M, Friedman LS, Malek S.

Nature. 2010 Mar 18;464(7287):431-5. doi: 10.1038/nature08833. Epub 2010 Feb 3.

PMID:
20130576
3.

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.

4.

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.

5.

Drug discovery: inhibitors that activate.

Cichowski K, Jänne PA.

Nature. 2010 Mar 18;464(7287):358-9. doi: 10.1038/464358a. No abstract available.

PMID:
20237552
6.

Disruption of CRAF-mediated MEK activation is required for effective MEK inhibition in KRAS mutant tumors.

Lito P, Saborowski A, Yue J, Solomon M, Joseph E, Gadal S, Saborowski M, Kastenhuber E, Fellmann C, Ohara K, Morikami K, Miura T, Lukacs C, Ishii N, Lowe S, Rosen N.

Cancer Cell. 2014 May 12;25(5):697-710. doi: 10.1016/j.ccr.2014.03.011. Epub 2014 Apr 17.

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.

Tumours with class 3 BRAF mutants are sensitive to the inhibition of activated RAS.

Yao Z, Yaeger R, Rodrik-Outmezguine VS, Tao A, Torres NM, Chang MT, Drosten M, Zhao H, Cecchi F, Hembrough T, Michels J, Baumert H, Miles L, Campbell NM, de Stanchina E, Solit DB, Barbacid M, Taylor BS, Rosen N.

Nature. 2017 Aug 10;548(7666):234-238. doi: 10.1038/nature23291. Epub 2017 Aug 2.

9.

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.

10.

Inhibitors of Raf kinase activity block growth of thyroid cancer cells with RET/PTC or BRAF mutations in vitro and in vivo.

Ouyang B, Knauf JA, Smith EP, Zhang L, Ramsey T, Yusuff N, Batt D, Fagin JA.

Clin Cancer Res. 2006 Mar 15;12(6):1785-93.

11.

Inhibition of RAF Isoforms and Active Dimers by LY3009120 Leads to Anti-tumor Activities in RAS or BRAF Mutant Cancers.

Peng SB, Henry JR, Kaufman MD, Lu WP, Smith BD, Vogeti S, Rutkoski TJ, Wise S, Chun L, Zhang Y, Van Horn RD, Yin T, Zhang X, Yadav V, Chen SH, Gong X, Ma X, Webster Y, Buchanan S, Mochalkin I, Huber L, Kays L, Donoho GP, Walgren J, McCann D, Patel P, Conti I, Plowman GD, Starling JJ, Flynn DL.

Cancer Cell. 2015 Sep 14;28(3):384-98. doi: 10.1016/j.ccell.2015.08.002. Epub 2015 Sep 3.

12.

Mutation that blocks ATP binding creates a pseudokinase stabilizing the scaffolding function of kinase suppressor of Ras, CRAF and BRAF.

Hu J, Yu H, Kornev AP, Zhao J, Filbert EL, Taylor SS, Shaw AS.

Proc Natl Acad Sci U S A. 2011 Apr 12;108(15):6067-72. doi: 10.1073/pnas.1102554108. Epub 2011 Mar 25.

13.

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.

14.

ARAF acts as a scaffold to stabilize BRAF:CRAF heterodimers.

Rebocho AP, Marais R.

Oncogene. 2013 Jun 27;32(26):3207-12. doi: 10.1038/onc.2012.330. Epub 2012 Aug 27.

PMID:
22926515
15.

Resistance to MEK inhibitors: should we co-target upstream?

Poulikakos PI, Solit DB.

Sci Signal. 2011 Mar 29;4(166):pe16. doi: 10.1126/scisignal.2001948. Review.

PMID:
21447797
16.

A Raf-induced allosteric transition of KSR stimulates phosphorylation of MEK.

Brennan DF, Dar AC, Hertz NT, Chao WC, Burlingame AL, Shokat KM, Barford D.

Nature. 2011 Apr 21;472(7343):366-9. doi: 10.1038/nature09860. Epub 2011 Mar 27.

PMID:
21441910
17.

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.

18.
19.

RAF inhibitor-induced KSR1/B-RAF binding and its effects on ERK cascade signaling.

McKay MM, Ritt DA, Morrison DK.

Curr Biol. 2011 Apr 12;21(7):563-8. doi: 10.1016/j.cub.2011.02.033. Epub 2011 Mar 31.

20.

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

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