Xuewei Wu, Xiaobao Yang, Yan Xiong, Ruitong Li, Takahiro Ito, Tamer A. Ahmed, Zoi Karoulia, Christos Adamopoulos, Hong Wang, Li Wang, Ling Xie, Jing Liu, Beatrix Ueberheide, Stuart A. Aaronson, Xian Chen, Sean G. Buchanan, William R. Sellers, Jian Jin, Poulikos I. Poulikakos. Distinct CDK6 complexes determine tumor cell response to CDK4/6 inhibitors and degraders. Nat Cancer. 2021 2, 429–443 https://doi.org/10.1038/s43018-021-00174-z.

Adamopoulos C, Ahmed TA, Tucker MR, Ung PMU, Xiao M, Karoulia Z, Amabile A, Wu X, Aaronson SA, Ang C, Rebecca VW, Brown BD, Schlessinger A, Herlyn M, Wang Q, Shaw DE, Poulikakos PI. Exploiting allosteric properties of RAF and MEK inhibitors to target therapy-resistant tumors driven by oncogenic BRAF signaling. Cancer Discov. 2021 Feb 10:candisc.1351. 2020. doi: 10.1158/2159-8290.CD-20-1351. Online ahead of print. PMID: 33568355.

Cotto-Rios XM, Agianian B, Gitego N, Zacharioudakis E, Giricz O, Wu Y, Zou Y, Verma A, Poulikakos PI, Gavathiotis E. Inhibitors of BRAF dimers using an allosteric site. E. Nat Commun. 2020 Sep 1;11(1):4370. doi: 10.1038/s41467-020-18123-2. PMID: 32873792.

Santini CC, Longden J, Schoof EM, Simpson CD, Jeschke GR, Creixell P, Kim J, Wu X, Turk BE, Rosen N, Poulikakos PI, Linding R. Global view of the RAF-MEK-ERK module and its immediate downstream effectors. Sci Rep. 2019 Jul 26;9(1):10865. doi: 10.1038/s41598-019-47245-x. PMID: 31350469.

Ahmed TA, Adamopoulos C, Karoulia Z, Wu X, Sachidanandam R, Aaronson AA, Poulikakos PI. SHP2 Drives Adaptive Resistance to ERK Signaling Inhibition in Molecularly Defined Subsets of ERK-dependent Tumors. Cell Reports. 2019 Jan 2;26(1):65-78.e5. doi: 10.1016/j.celrep.2018.12.013. PMID: 30605687.

Stratikopoulos EE, Kiess N, Szabolcs M, Pegno S, Kakit C, Wu X, Poulikakos PI, Cheung P, Schmidt H, Parsons R. Mouse ER+/PIK3CAH1047R breast cancers caused by exogenous estrogen are heterogeneously dependent on estrogen and undergo BIM-dependent apoptosis with BH3 and PI3K agents. Oncogene. 2018 Aug 3. doi: 10.1038/s41388-018-0436-4. [Epub ahead of print]. PMID: 30076411.

Hogstad B, Berres ML, Chakraborty R, Tang J, Bigenwald C, Serasinghe M, Lim KPH, Lin H, Man TK, Remark R, Baxter S, Kana V, Jordan S, Karoulia Z, Kwan WH, Leboeuf M, Brandt E, Salmon H, McClain K, Poulikakos P, Chipuk J, Mulder WJM, Allen CE, Merad M. RAF/MEK/extracellular signal-related kinase pathway suppresses dendritic cell migration and traps dendritic cells in Langerhans cell histiocytosis lesions. The Journal of experimental medicine. 2018; Jan 2;215(1):319-336. PMID: 29263218. PMCID: PMC5748846.

Karoulia Z, Gavathiotis E, Poulikakos PI, New perspectives for targeting RAF kinase in human cancer. Nature Reviews Cancer. 2017 Nov; 17(11):676-691. Epub 2017 Oct 6. PMID: 28984291.

Chakraborty R, Hampton OA, Abhyankar H, Zinn DJ, Grimes A, Skull B, Eckstein O, Mahmood N, Wheeler DA, Lopez-Terrada D, Peters TL, Hicks JM, Elghetany T, Krance R, Poulikakos PI, Merad M, McClain KL, Allen CE, Parsons DW. Activating MAPK1 (ERK2) mutation in an aggressive case of disseminated juvenile xanthogranuloma. Oncotarget. 2017 Jul 11;8(28):46065-46070. PMID: 28512266.

Chakraborty R, Burke TM, Hampton OA, Zinn DJ, Lim KP, Abhyankar H, Scull B, Kumar V, Kakkar N, Wheeler DA, Roy A, Poulikakos PI, Merad M, McClain KL, Parsons DW, Allen CE.  Alternative genetic mechanisms of BRAF activation in Langerhans cell histiocytosis. Blood. 2016 Nov 24;128(21):2533-2537. PMID: 27729324.

Karoulia Z, Wu Y, Ahmed TA, Xin Q, Bollard J, Krepler C, Wu X, Zhang C, Bollag G, Herlyn M, Fagin JA, Lujambio A, Gavathiotis E, Poulikakos PI. An Integrated Model of RAF Inhibitor Activity Predicts Inhibitor Activity against Oncogenic BRAF Signaling. Cancer Cell. 2016 Sep 12;30(3):485-98. doi: 10.1016/j.ccell.2016.06.024. PMID: 27523909.

Krepler C, Xiao M, Sproesser K, Brafford PA, Shannan B, Beqiri M, Liu Q, Xu W, Garman B, Nathanson KL, Xu X, Karakousis GC, Mills GB, Lu Y, Ahmed TA, Poulikakos PI, Caponigro G, Boehm M, Peters M, Schuchter LM, Weeraratna AT, Herlyn M. Personalized Preclinical Trials in BRAF Inhibitor-Resistant Patient-Derived Xenograft Models Identify Second-Line Combination Therapy. Clin Cancer Res. 2016 Apr 1;22(7):1592-602. doi: 10.1158/1078-0432.CCR-15. PMID: 26673799.

Yao Z, Torres NM, Tao A, Gao Y, Luo L, Li Q, de Stanchina E, Abdel-Wahab O, Solit DB, Poulikakos PI, Rosen N.  BRAF Mutants Evade ERK-Dependent Feedback by Different Mechanisms that Determine Their Sensitivity to Pharmacologic Inhibition. Cancer Cell. 2015 Sep 14;28(3):370-83. doi: 10.1016/j.ccell.2015.08.001 PMID: 26343582. 

Salton M, Kasprzak WK, Voss T, Shapiro BA, Poulikakos PI, Misteli T. Inhibition of vemurafenib-resistant melanoma by interference with pre-mRNA splicing. Nat Commun. 2015 May 14;6:7103. doi: 10.1038/ncomms8103. PMID: 25971842.

Samatar AA, Poulikakos PI. Targeting RAS-ERK signaling in cancer: promises and challenges. Nat Rev Drug Discov. 2014 Dec 1;13(12):928-42. doi: 10.1038/nrd4281. PMID: 25435214.

Chakraborty R, Hampton OA, Shen X, Simko S, Shih A, Abhyankar H, Lim KP, Covington K, 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. Mutually exclusive recurrent somatic mutations in MAP2K1 and BRAF support a central role for ERK activation in LCH pathogenesis. Blood. 2014 Sep 8. pii: blood-2014-05-577825. PMID: 25202140.

Y, Tachibana-Kondo Y, Iikura H, Aoki T, Shimma N, Arisawa M, Sowa Y, Poulikakos PI, Rosen N, Aoki Y, Sakai T. Enhanced inhibition of ERK signaling by a novel allosteric MEK inhibitor, CH5126766, that suppresses feedback reactivation of RAF activity. Cancer Res. 2013 Jul 1;73(13):4050-60. Doi 10.1158/0008-5472.CAN-12-3937. Epub 2013 May 10. PMID: 23667175.

Chakravarty SD, Poulikakos PI, Ivashkiv LB, Salmon JE, Kalliolias GD. Kinase inhibitors: A new tool for the treatment of rheumatoid arthritis. Clin Immunol. 2013 Apr 17;148(1):66-78. doi: 10.1016/j.clim.2013.04.007. PMID 23651870.

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. Relief of Profound Feedback Inhibition of Mitogenic Signaling by RAF inhibitors Attenuates Their Activity in BRAFV600E Melanomas. Cancer Cell. 2012 Nov 13;22(5):668-82. doi: 10.1016/j.ccr.2012.10.009. PMID: 23153539.

Rodrik-Outmezguine VS, Chandarlapaty S, Pagano NC, Poulikakos PI, Scaltriti M, Moskatel E,Baselga J, Guichard S, Rosen N. mTOR kinase inhibition causes feedback-dependent biphasicregulation of AKT signaling. Cancer Discov. 2011 Aug;1(3):248-59. doi: 10.1158/2159 8290.CD-11- 0085. Epub 2011 Jun 17. PMID: 22140653.

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. RAF inhibitor resistance is mediated by dimerization of aberrantly spliced BRAF(V600E). Nature. 2011 Nov 23;480(7377):387-90. doi: 10.1038/nature10662. PMID: 22113612.

Poulikakos PI, Solit DB. Resistance to MEK inhibitors: should we co-target upstream? Sci Signal. 2011 Mar 29;4(166):pe16. doi: 10.1126/scisignal.2001948. Review. PMID: 21447797

Poulikakos PI, Rosen N. Mutant BRAF melanomas–dependence and resistance. Cancer Cell. 2011 Jan 18;19(1):11-5. doi: 10.1016/j.ccr.2011.01.008. Review. PMID: 21251612.

Joseph EW, Pratilas CA, Poulikakos PI, Tadi M, Wang W, Taylor BS, et al. The RAF inhibitor PLX4032 inhibits ERK signaling and tumor cell proliferation in a V600E BRAF-selective manner. Proc Natl Acad Sci U S A. 2010;107(33):14903-8. Epub 2010/07/30. doi: 1008990107 [pii] 10.1073/pnas.1008990107. PMID: 20668238.

Poulikakos PI, Zhang C, Bollag G, Shokat KM, Rosen N. RAF inhibitors transactivate RAF dimers and ERK signaling in cells with wild-type BRAF. Nature. 2010;464(7287):427-30. Epub 2010/02/25. doi: nature08902 [pii]10.1038/nature 08902. PMID: 20179705.

Mabuchi S, Altomare DA, Cheung M, Zhang L, Poulikakos PI, Hensley HH, Schilder RJ, Ozols RF, Testa JR. RAD001 inhibits human ovarian cancer cell proliferation, enhances cisplatin-induced apoptosis and prolongs survival in an ovarian cancer model. Clin Cancer Res. 2007 Jul 15;13(14):4261-70. PMID:17634556.

Li J, Poulikakos PI, Dai Z, Testa JR, Callaway DJ, Bu Z. Protein kinase C phosphorylation disrupts Na+/H+ exchanger regulatory factor 1 autoinhibition and promotes cystic fibrosis transmembrane conductance regulator macromolecular assembly. The Journal of Biological Chemistry. 2007;282(37):27086-99. Epub 2007/07/07. doi: 10.1074/jbc.M702019200. PMID: 17613530.

Poulikakos PI, Xiao GH, Gallagher R, Jablonski S, Jhanwar SC, Testa JR. Re-expression of the tumor suppressor NF2/merlin inhibits invasiveness in mesothelioma cells and negatively regulates FAK. Oncogene. 2006;25(44):5960-8. Epub 2006/05/03. doi: 10.1038/sj.onc.1209587. PMID: 16652148.

Wang HQ, Altomare DA, Skele KL, Poulikakos PI, Kuhajda FP, Di Cristofano A, et al. Positive feedback regulation between AKT activation and fatty acid synthase expression in ovarian carcinoma cells. Oncogene. 2005;24(22):3574-82. Epub 2005/04/05. doi:10.1038/sj.onc.1208463. PMID: 15806173.

Apostolou S, Klein JO, Mitsuuchi Y, Shetler JN, Poulikakos PI, Jhanwar SC, et al. Growth inhibition and induction of apoptosis in mesothelioma cells by selenium and dependence on selenoprotein SEP15 genotype. Oncogene. 2004;23(29):5032-40. Epub 2004/04/27. doi: 10.1038/sj.onc.1207683. PMID: 15107826.

Poulikakos P, Vassilacopoulou D, Fragoulis EG. L-DOPA decarboxylase association with membranes in mouse brain. Neurochem Res. 2001 May;26(5):479-85. PMID: 11513473.