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Spitz AZ, Zacharioudakis E, Reyna DE, Garner TP, Gavathiotis E. Eltrombopag directly inhibits BAX and prevents cell death. Nature Communications 2021 12:1134 | https://doi.org/10.1038/s41467-021-21224-1
Gadsden N, Fulcher C, Li D, Shrivastava N, Thomas C, Segall J, Prystowsky M, Schlecht N, Gavathiotis E, Ow T. Palbociclib renders human papilloma virus negative head and neck squamous cell carcinoma vulnerable to the senolytic agent navitoclax. Mol. Cancer Res. 2021 Jan 25 doi: 10.1158/1541-7786.MCR-20-0915
Dong S, Wang Q, Kao YK, Diaz A , Tasset I, Kaushik S, Thiruthuvanathan V, Zintiridou A, Nieves E, Dzieciatkowska M, Reisz JA, Gavathiotis E, D'Alessandro A, Will B, Cuervo AM. Chaperone-mediated autophagy sustains hematopoietic stem cell function. Nature 2021 Jan 13
Cotto-Rios X, Agianian B, Gitego, N, Zacharioudakis E, Giricz O, Wu Y, Yiyu, Z, Verma A, Poulikakos PI, Gavathiotis E. Inhibitors of BRAF dimers using an allosteric site. Nature Comms. (2020) 11:4370
Amgalan D, Garner TP, Pekson R, Jia XF, Yanamandala M, Paulino V, Liang FG, Corbalan JJ, Lee J, Chen Y, Karagiannis GS, Sanchez LS, Liang H, Narayanagari SR, Mitchell K, Lopez A, Margulets V, Scarlata M, Santulli G, Asnani A, Peterson RT, Hazan RB, Condeelis JS, Oktay MH, Steidl U, Kirshenbaum LA, Gavathiotis E.*, Kitsis RN* A small molecule allosteric inhibitor of BAX protects against doxorubicin-induced cardiomyopathy. Nature Cancer 2020. https://doi.org/10.1038/s43018-020-0039-1
Ow TJ, Thomas C, Fulcher CD, Chen J, Lopez A, Reyna, DE, Prystowsky MB, Smith RV, Schiff BA, Rosenblatt G, Belbin TJ, Harris JM, Childs GC, Kawachi N, Schlecht MF, Gavathiotis E. Apoptosis Signaling Molecules as Treatment Targets in Head and Neck Squamous Cell Carcinoma. The Laryngoscope. 2019 (in press) doi.10.1002/lary.28441
Chen X, Glytsou C, Zhou H, Narang S, Reyna DE, Lopez A, Sakellaropoulos T, Gong Y, Kloetgen A, Yap YS, Wang E, Gavathiotis E, Tsirigos A, Tibes R, Aifantis I. Targeting Mitochondrial Structure Sensitizes Acute Myeloid Leukemia to Venetoclax Treatment. Cancer Discov. 2019, 9:1-20
Garner TP, Amgalan D, Reyna DE, Li S, Kitsis RN, Gavathiotis E. Small Molecule Allosteric Inhibitors of BAX. Nat. Chem. Biol. 2019, 15: 1-12
Zhang J, He J, Johnson JL, Rahman F, Gavathiotis E, Cuervo AM, Catz SD. Chaperone-mediated autophagy upregulation rescues megalin expression and localization in cystinotic proximal tubule cells. Front. Endocrinol. 2019 doi: 10.3389/fendo.2019.00021
Ow TJ, Fulcher CD, Thomas C, O’Broin P, Lopez A, Reyna, DE, Smith RV, Sarta C, Prystowsky MB, Schlecht MF, Schiff BA, Rosenblatt G, Belbin TJ, Harris JM, Childs GC, Kawachi N, Guha C, Gavathiotis E. Optimal Targeting of BCL-family Proteins in Head and Neck Squamous Cell Carcinoma Requires Inhibition of Both BCL-xL and MCL-1. Oncotarget. 2019, 10:494-510.
Gavathiotis E. BCL-2 family proteins. Methods Mol. Biol. 2018, 1877: i-xi.
Reyna DE, Gavathiotis E. Liposomal parmeabilization assay to study functional interactions of BCL-2 family proteins. Methods Mol. Biol. 2018, 1877: 111-119.
Garner TP, Gavathiotis E. BCL-2 Protein Family Interaction Analysis by Nuclear Magnetic Resonance Spectroscopy. Methods Mol. Biol. 2018, 1877: 217-231.
Giricz O, Mo Y, Dahlman KB, Cotto-Rios XM, Vardabasso C, Nguyen H, Matusow B, Bartenstein M, Polishchuk V, Johnson DB, Bhagat TD, Shellooe R, Burton E, Tsai J, Zhang C, Habets G, Greally JM, Yu Y, Kenny PA, Fields GB, Pradhan K, Stanley ER, Bernstein E, Bollag G, Gavathiotis E, West BL, Sosman JA, Verma AK. The RUNX1/IL-34/CSF-1R axis is an autocrinally regulated modulator of resistance to BRAF-V600E inhibition in melanoma. JCI Insight. 2018, 3(14).
Zhang Q, Zhang J., Gavathiotis E. ICBS2017 in Shanghai-Illuminating Life with Chemical Innovation. ACS Chem. Biol. 2018. doi: 10.1021/acschembio.8b00220. PubMed PMID: 29677443.
Rocha GA, Franco F, Krezel A, Rumsey JM, Alberti JM, Knight WC, Biris N, Zacharioudakis E, Janetka JW, Baloh BH, Kitsis RN, Mochly-Rosen D, Townsend RR, Gavathiotis E, Dorn GW. Mfn2 agonists reverse mitochondrial defects in preclinical models of Charcot Marie Tooth disease type 2A. Science 2018, 360: 336-341.
Bogos A and Gavathiotis E. Current insights of BRAF inhibitors in cancer. J. Med. Chem. 2018, 61:5775-5793
Reyna DE and Gavathiotis E. Pulling the BAX trigger for tumor cell death . Oncotarget 2018, 9: 8204-8205
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Antony-Debré I, Paul A, Leite J, Mitchell K, Kim HM, Carvajal LA, Todorova TI, Huang K, Kumar A, Farahat AA, Bartholdy B, Narayanagari SR, Chen J, Ambesi-Impiombato A, Ferrando AA, Mantzaris I, Gavathiotis E, Verma A, Will B, Boykin DW, Wilson WD, Poon GM, Steidl U. Pharmacological inhibition of the transcription factor PU.1 in leukemia. J. Clin. Invest. 2017, Oct 30 doi: 10.1172/JCI92504
Reyna DE, Garner TP, Lopez A, Kopp F, Choudhary GS, Sridharan A, Narayanagari SR, Mitchell K, Dong B, Bartholdy BA, Walensky LD, Verma A, Steidl U, Gavathiotis E. Direct Activation of BAX by BTSA1 Ovecomes Apoptosis Resistance in Acute Meyloid Leukemia. Cancer Cell 2017, 32: 490–505
Karoulia Z. Gavathiotis E. Poulikakos PI. New perspectives for targeting RAF kinase in human cancer. Nat. Rev. Cancer 2017, Oct 6.
Garner TP, Lopez A, Reyna DE, Spitz AZ, Gavathiotis E. Progress in targeting the BCL-2 family of proteins. Curr. Opin. Chem. Biol. 2017, 39: 133-142
Gavathiotis E* and Zhou MM*. Chemical genetics and epigenetics. Curr. Opin. Chem. Biol. 2017, 39:1-3
Zhang J, Johnson JL, He J, Napolitano G, Ramadass M, Rocca C, Kiosses WB, Bucci C, Xin Q, Gavathiotis E, Cuervo AM, Cherqui S, Catz SD. Cystinosin, the small GTPase Rab11, and the Rab7 effector RILP regulate intracellular trafficking of the chaperone-mediated autophagy receptor LAMP2A. J. Biol. Chem. 2017, jbc.M116.764076
Franco A, Kitsis RN, Fleischer JA, Gavathiotis E, Kornfeld OS, Gong G, Biris N, Benz A, Qvit N, Donnelly SK, Chen Y, Mennerick S, Hodgson L, Mochly-Rosen D, Dorn GW 2nd. Correcting mitochondrial fusion by minipulating mitofusin conformations. Nature 2016, 540: 74-79
Johnson JL, Ramadass M, He J, Brown SJ, Zhang J, Abgaryan L, Biris N, Gavathiotis E, Rosen H, Catz SD. Identification of Nexinhibs, small-molecule inhibitors of neutrophil exocytosis and inflammation. Druggability of the small GTPase Rab27a. J. Biol. Chem. 2016, 291: 25965-25982
Reyna DE and Gavathiotis E. Self-regulation of BAX-induced cell death. Oncotarget 2016
Karoulia Z, Wu Y, Ahmed AA, Xin Q, Bollard J, Krepler C, Wu X, Zhang C, Bollag G, Herlyn M, Fagin JA, Lujambio A, Gavathiotis E*, Poulikakos P*. An Integrated Model of RAF inhibitor Action Predicts Inhibitor Activity against Oncogenic BRAF Signaling. Cancer Cell 2016, 30: 1-14.
Garner TP, Reyna DE, Priyadarshi A, Chen HC, Li S, Ganesan, YT, Malashkevich VN, Almo SS, Cheng EH, Gavathiotis E. An Autoinhibited Dimeric Form of BAX Regulates the BAX Activation Pathway. Mol. Cell 2016, 63: 485-497.
Cotto-Rios XM, Gavathiotis E. Unraveling cell death mysteries. Nat. Chem. Biol. 2016 12: 470-471
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Uchime O, Dai Z, Biris N, Lee D, Sidhu SS, Li S, Lai JR, Gavathiotis E. Synthetic Antibodies Inhibit Bcl-2-associated X Protein (BAX) through Blockade of the N-terminal Activation Site. J. Biol. Chem. 2015, 291: 89-102.
Chen HC, Kanai M, Inoue-Yamauchi A, Tu HC, Huang Y, Ren D, Kim H, Takeda S, Reyna DE, Chan PM, Ganesan YT, Liao CP, Gavathiotis E, Hsieh JJ, Cheng EH. An interconnected hierarchical model of cell death regulation by the BCL-2 family. Nat Cell Biol. 2015, 17: 1270-1281.
Barclay LA, Wales TE, Garner TP, Wachter F, Lee S, Guerra R, Stewart ML, Braun CR, Bird GH, Gavathiotis E, Engen JR, Walensky LD. Inhibition of Pro-apoptotic BAX by a noncanonical interaction mechanism. Mol. Cell 2015, 57: 1-14.
Li R, Cheng C, Balasis ME, Liu Y, Garner TP, Daniel KG, Li J, Qin Y, Gavathiotis E*, Sebti SM*. Design, synthesis and evaluation of Marinopyrrole derivatives as selective inhibitors of Mcl-1 binding to pro-apoptotic Bim and dual Mcl-1/Bcl-xL inhibitors.Eur. J. Med. Chem. 2015, 90: 315-331
Cheng C, Liu Y, Balasis ME, Garner TP, Li J, Simmons NL, Berndt N, Song H, Pan L, Qin Y, Nicolaou KC, Gavathiotis E, Sebti SM. Marinopyrrole Derivatives with Sulfide Spacers as Selective Disruptors of Mcl-1 Binding to Bim. Mar. Drugs 2014, 12: 4311-4325.
Papadopoulos E, Jenni S, Kabha E, Takrouri KJ, Yi T, Salvi N, Luna RE, Gavathiotis E, Mahalingam P, Arthanari H, Rodriguez-Mias R, Freedman RY, Aktas BA, Chorev M, Halperin JA, Wagner G. Structure of the translation initiation factor eIF4E in complex with 4EGI-1 reveals an allosteric mechanism for dissociating eIF4G, Proc. Natl. Acad. Sci. USA 2014, 111: E3187-E3195.
Bird GH, Gavathiotis E, Labelle JL, Katz SG, Walensky LD. Distinct BimBH3 (BimSAHB) Stapled Peptides for Structural and Cellular Studies. ACS Chem. Biol. 2014, 9: 831-837.
Gavathiotis E. Structural Perspectives on BCL-2 Family of Proteins. Cell Death - Mechanism and Disease. 2013 229-251.
Edwards EL, Gavathiotis E, LaBelle J, Braun GH, Opoku-Nsiah K, Bird GH, Walensky LD. Multimodal activation of apoptosis by a hydrocarbon stapled PUMA BH3 helix. Chem. & Biol. 2013; 20: 888-902.
Anguiano J. Garner T, Mahalingam M, Das BS*, Gavathiotis E* and Cuervo AM*. Chemical modulation of chaperone-mediated autophagy by novel retinoic acid derivatives. Nat. Chem. Biol. 2013, 374-382.
Cohen NA, Stewart ML, Gavathiotis E, Tepper JL, Opferman JT, Walensky LD. A competitive stapled peptide screen identified a selective small molecule that overcomes MCL-1 dependent leukemia cell survival. Chem & Biol. 2012, 19: 1175-1186.
Gavathiotis E*, Reyna DE, Bellairs JA, Leshchiner ES, Walensky LD*. Direct and selective small-molecule activation of proapoptotic BAX. Nature Chem. Bio. 2012, 8:639-645.
LaBelle JL, Katz SK, Bird GH, Gavathiotis E, Stewart ML, Lawrence C, Fisher JK, Godes M, Pitter K, Kung AL, Walensky LD. A stapled BIM peptide overcomes apoptotic resistance in hematologic cancers. J. Clin. Invest. 2012, 122:2018-2031.
Whelan RS, Konstantinidis K, Wei AC, Chen Y, Reyna DE, Jha S, Yang Y, Calvert JW, Lindsten T, Thompson CB, Crow MT, Gavathiotis E, Dorn GW 2nd, O'Rourke B, Kitsis RN. Bax regulates primary necrosis through mitochondrial dynamics. Proc Natl Acad Sci U S A. 2012, 109:6566-6571.
Walensky LD*. and Gavathiotis E*. BAX Unleashed: The Biochemical Transformation of an Inactive Cytosolic Monomer into a Toxic Mitochondrial Pore. Trends Biochem. Sci. 2011, 36:642:652
Gavathiotis E. and Walensky LD. Tracking BAX once the Trigger is Pulled. Cell Cycle 2011, 10:868-870.
Gavathiotis E, Reyna DR, Davis ML, Bird GH, Walensky LD. BH3-Triggered Structural Re-organization Drives the Activation of Pro-apoptotic BAX Mol. Cell 2010, 40:481-492.
Braun CR, Mintseris J, Gavathiotis E, Bird G, Gygi SP, Walensky LD. Photoreactive Stapled BH3 Peptides to Dissect the BCL-2 Family Interactome. Chem. Biol. 2010, 17:1325-1333.
Gavathiotis E, Suzuki M, Davis ML, Pitter K, Bird GH, Katz SG, Tu HC, Kim H, Cheng EH, Tjandra N, Walensky LD. BAX Activation is Initiated at a Novel Interaction Site. Nature 2008, 455:1076-1081.