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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. Joseph EW, et al. Among authors: poulikakos pi. Proc Natl Acad Sci U S A. 2010 Aug 17;107(33):14903-8. doi: 10.1073/pnas.1008990107. Epub 2010 Jul 28. Proc Natl Acad Sci U S A. 2010. PMID: 20668238 Free PMC article.
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. Poulikakos PI, et al. Nature. 2011 Nov 23;480(7377):387-90. doi: 10.1038/nature10662. Nature. 2011. PMID: 22113612 Free PMC article.
mTOR kinase inhibition causes feedback-dependent biphasic regulation of AKT signaling.
Rodrik-Outmezguine VS, Chandarlapaty S, Pagano NC, Poulikakos PI, Scaltriti M, Moskatel E, Baselga J, Guichard S, Rosen N. Rodrik-Outmezguine VS, et al. Among authors: poulikakos pi. Cancer Discov. 2011 Aug;1(3):248-59. doi: 10.1158/2159-8290.CD-11-0085. Epub 2011 Jun 17. Cancer Discov. 2011. PMID: 22140653 Free PMC article.
Relief of profound feedback inhibition of mitogenic signaling by RAF inhibitors attenuates their activity in BRAFV600E melanomas.
Lito P, Pratilas CA, Joseph EW, Tadi M, Halilovic E, Zubrowski M, Huang A, Wong WL, Callahan MK, Merghoub T, Wolchok JD, de Stanchina E, Chandarlapaty S, Poulikakos PI, Fagin JA, Rosen N. Lito P, et al. Among authors: poulikakos pi. Cancer Cell. 2012 Nov 13;22(5):668-82. doi: 10.1016/j.ccr.2012.10.009. Cancer Cell. 2012. PMID: 23153539 Free PMC article.
Enhanced inhibition of ERK signaling by a novel allosteric MEK inhibitor, CH5126766, that suppresses feedback reactivation of RAF activity.
Ishii N, Harada N, Joseph EW, Ohara K, Miura T, Sakamoto H, Matsuda Y, Tomii Y, Tachibana-Kondo Y, Iikura H, Aoki T, Shimma N, Arisawa M, Sowa Y, Poulikakos PI, Rosen N, Aoki Y, Sakai T. Ishii N, et al. Among authors: poulikakos pi. Cancer Res. 2013 Jul 1;73(13):4050-4060. doi: 10.1158/0008-5472.CAN-12-3937. Epub 2013 May 10. Cancer Res. 2013. PMID: 23667175 Free PMC article.
Mutually exclusive recurrent somatic mutations in MAP2K1 and BRAF support a central role for ERK activation in LCH pathogenesis.
Chakraborty R, Hampton OA, Shen X, Simko SJ, Shih A, Abhyankar H, Lim KP, Covington KR, Trevino L, Dewal N, Muzny DM, Doddapaneni H, Hu J, Wang L, Lupo PJ, Hicks MJ, Bonilla DL, Dwyer KC, Berres ML, Poulikakos PI, Merad M, McClain KL, Wheeler DA, Allen CE, Parsons DW. Chakraborty R, et al. Among authors: poulikakos pi. Blood. 2014 Nov 6;124(19):3007-15. doi: 10.1182/blood-2014-05-577825. Epub 2014 Sep 8. Blood. 2014. PMID: 25202140 Free PMC article.
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