Alizadeh AA, Staudt LM. Genomic-scale gene expression profiling of normal and malignant immune cells. Curr Opin Immunol. 2000;12(2):219–25.

Article  CAS  PubMed  Google Scholar 

Reddy A, Zhang J, Davis NS, Moffitt AB, Love CL, Waldrop A, Leppa S, Pasanen A, Meriranta L, Karjalainen-Lindsberg ML, Norgaard P, Pedersen M, Gang AO, Hogdall E, Heavican TB, Lone W, Iqbal J, Qin Q, Li G, Kim SY, Healy J, Richards KL, Fedoriw Y, Bernal-Mizrachi L, Koff JL, Staton AD, Flowers CR, Paltiel O, Goldschmidt N, Calaminici M, Clear A, Gribben J, Nguyen E, Czader MB, Ondrejka SL, Collie A, Hsi ED, Tse E, Au-Yeung RKH, Kwong YL, Srivastava G, Choi WWL, Evens AM, Pilichowska M, Sengar M, Reddy N, Li S, Chadburn A, Gordon LI, Jaffe ES, Levy S, Rempel R, Tzeng T, Happ LE, Dave T, Rajagopalan D, Datta J, Dunson DB, Dave SS. Genetic and functional drivers of diffuse large B cell lymphoma. Cell. 2017;171(2):481–e49415.

Article  CAS  PubMed  PubMed Central  Google Scholar 

Schmitz R, Wright GW, Huang DW, Johnson CA, Phelan JD, Wang JQ, Roulland S, Kasbekar M, Young RM, Shaffer AL, Hodson DJ, Xiao W, Yu X, Yang Y, Zhao H, Xu W, Liu X, Zhou B, Du W, Chan WC, Jaffe ES, Gascoyne RD, Connors JM, Campo E, Lopez-Guillermo A, Rosenwald A, Ott G, Delabie J, Rimsza LM, Tay Kuang Wei K, Zelenetz AD, Leonard JP, Bartlett NL, Tran B, Shetty J, Zhao Y, Soppet DR, Pittaluga S, Wilson WH, Staudt LM. Genetics and Pathogenesis of diffuse large B-Cell lymphoma. N Engl J Med. 2018;378(15):1396–407.

Article  CAS  PubMed  PubMed Central  Google Scholar 

Vogler M, Walter HS, Dyer MJS. Targeting anti-apoptotic BCL2 family proteins in haematological malignancies - from pathogenesis to treatment. Br J Haematol. 2017;178(3):364–79.

Article  CAS  PubMed  Google Scholar 

Davids MS, Roberts AW, Seymour JF, Pagel JM, Kahl BS, Wierda WG, Puvvada S, Kipps TJ, Anderson MA, Salem AH, Dunbar M, Zhu M, Peale F, Ross JA, Gressick L, Desai M, Kim SY, Verdugo M, Humerickhouse RA, Gordon GB, Gerecitano JF. Phase I first-in-human study of Venetoclax in patients with relapsed or refractory Non-hodgkin Lymphoma. J Clin Oncol. 2017;35(8):826–33.

Article  CAS  PubMed  PubMed Central  Google Scholar 

Rooswinkel RW, van de Kooij B, Verheij M, Borst J. Bcl-2 is a better ABT-737 target than Bcl-xL or Bcl-w and only Noxa overcomes resistance mediated by Mcl-1, Bfl-1, or Bcl-B. Cell Death Dis. 2012;3(8):e366.

Article  CAS  PubMed  PubMed Central  Google Scholar 

Boiko S, Proia T, San Martin M, Gregory GP, Wu MM, Aryal N, Hattersley M, Shao W, Saeh JC, Fawell SE, Johnstone RW, Drew L, Cidado J. Targeting Bfl-1 via acute CDK9 inhibition overcomes intrinsic BH3-mimetic resistance in lymphomas Blood, 2021. 137(21): pp. 2947–2957.

Wang G, Diepstraten ST, Herold MJ. Last but not least: BFL-1 as an emerging target for anti-cancer therapies. Biochem Soc Trans. 2022;50(4):1119–28.

Article  CAS  PubMed  PubMed Central  Google Scholar 

Vogler M. BCL2A1: the underdog in the BCL2 family. Cell Death Differ, 2012. 19.

Youle RJ, Strasser A. The BCL-2 protein family: opposing activities that mediate cell death. Nat Rev Mol Cell Biol. 2008;9(1):47–59.

Article  CAS  PubMed  Google Scholar 

Kehr S, Vogler M. It’s time to die: BH3 mimetics in solid tumors. Biochim Biophys Acta Mol Cell Res. 2021;1868(5):118987.

Article  CAS  PubMed  Google Scholar 

Bittker JA, Weiwer M, Wei G, Germain A, Brown E, Dandapani S, Munoz B, Palmer M, Golub T, Schreiber SL. Discovery of Inhibitors of Anti-Apoptotic Protein A1, in Probe Reports from the NIH Molecular Libraries Program. 2010: Bethesda (MD).

Smith VM, Dietz A, Henz K, Bruecher D, Jackson R, Kowald L, van Wijk SJL, Jayne S, Macip S, Fulda S, Dyer MJS, Vogler M. Specific interactions of BCL-2 family proteins mediate sensitivity to BH3-mimetics in diffuse large B-cell lymphoma. Haematologica. 2020;105(8):2150–63.

Article  CAS  PubMed  PubMed Central  Google Scholar 

Lou J, Zhou Q, Lyu X, Cen X, Liu C, Yan Z, Li Y, Tang H, Liu Q, Ding J, Lu Y, Huang H, Xie H, Zhao Y. Discovery of a covalent inhibitor that overcame resistance to Venetoclax in AML cells overexpressing BFL-1. J Med Chem, 2024.

Esteve-Arenys A, Valero JG, Chamorro-Jorganes A, Gonzalez D, Rodriguez V, Dlouhy I, Salaverria I, Campo E, Colomer D, Martinez A, Rymkiewicz G, Perez-Galan P, Lopez-Guillermo A, Roue G. The BET bromodomain inhibitor CPI203 overcomes resistance to ABT-199 (venetoclax) by downregulation of BFL-1/A1 in in vitro and in vivo models of MYC+/BCL2 + double hit lymphoma. Oncogene. 2018;37(14):1830–44.

Article  CAS  PubMed  Google Scholar 

Blum KA, Abramson J, Maris M, Flinn I, Goy A, Mertz J, Sims R, Garner F, Senderowicz A, Younes A. A phase I study of CPI-0610, a bromodomain and extra terminal protein (BET) inhibitor in patients with relapsed or refractory lymphoma. Ann Oncol. 2018;29:iii7.

Article  Google Scholar 

Moreno V, Vieito M, Sepulveda JM, Galvao V, Hernández-Guerrero T, Doger B, Saavedra O, Carlo-Stella C, Michot JM, Italiano A, Magagnoli M, Carpio C, Pinto A, Sarmiento R, Amoroso B, Aronchik I, Filvaroff E, Hanna B, Wei X, Nikolova Z, Braña I. BET inhibitor trotabresib in heavily pretreated patients with solid tumors and diffuse large B-cell lymphomas. Nat Commun. 2023;14(1):1359.

Article  CAS  PubMed  PubMed Central  Google Scholar 

Dickinson M, Briones J, Herrera AF, González-Barca E, Ghosh N, Cordoba R, Rutherford SC, Bournazou E, Labriola-Tompkins E, Franjkovic I, Chesne E, Brouwer-Visser J, Lechner K, Brennan B, Nüesch E, DeMario M, Rüttinger D, Kornacker M, Hutchings M. Phase 1b study of the BET protein inhibitor RO6870810 with venetoclax and rituximab in patients with diffuse large B-cell lymphoma. Blood Adv. 2021;5(22):4762–70.

Article  CAS  PubMed  PubMed Central  Google Scholar 

Bechter OS. P., Make your best BET: the emerging role of BEET inhibitor treatment in malignant tumors. Pharmacology and Therapeutics; 2020.

Bertoni F, Stathis A. Bromodomain and extra-terminal domain inhibitors for lymphoid malignancies. Curr Opin Hematol. 2019;26(4):273–80.

Article  PubMed  Google Scholar 

Letson C, Padron E. Non-canonical transcriptional consequences of BET inhibition in cancer. Pharmacol Res. 2019;150:104508.

Article  CAS  PubMed  Google Scholar 

Nemec V, Schwalm MP, Muller S, Knapp S. PROTAC degraders as chemical probes for studying target biology and target validation. Chem Soc Rev. 2022;51(18):7971–93.

Article  CAS  PubMed  Google Scholar 

Cummin TECC, Murray KL, Turaj TD, Dunning AH, English L, Fell VL, Packham R, Ma G, Powell Y, Johnson B, Cragg PWM, Carter MS. M. J., BET inhibitors synergize with venetoclax to induce apoptosis in MYC-driven lymphomas with high BCL-2 expression. Blood Adv, 2020. 4(14).

Boi M, Gaudio E, Bonetti P, Kwee I, Bernasconi E, Tarantelli C, Rinaldi A, Testoni M, Cascione L, Ponzoni M, Mensah AA, Stathis A, Stussi G, Riveiro ME, Herait P, Inghirami G, Cvitkovic E, Zucca E, Bertoni F. The BET bromodomain inhibitor OTX015 affects pathogenetic pathways in preclinical B-cell Tumor models and synergizes with targeted drugs. Clin Cancer Res. 2015;21(7):1628–38.

Article  CAS  PubMed  Google Scholar 

Chapuy B, McKeown MR, Lin CY, Monti S, Roemer MG, Qi J, Rahl PB, Sun HH, Yeda KT, Doench JG, Reichert E, Kung AL, Rodig SJ, Young RA, Shipp MA, Bradner JE. Discovery and characterization of super-enhancer-associated dependencies in diffuse large B cell lymphoma. Cancer Cell. 2013;24(6):777–90.

Article  CAS  PubMed  PubMed Central  Google Scholar 

Jost PJ, Ruland J. Aberrant NF-kappaB signaling in lymphoma: mechanisms, consequences, and therapeutic implications. Blood. 2007;109(7):2700–7.

Article  CAS  PubMed  Google Scholar 

Haselager MV, Thijssen R, Bax D, Both D, De Boer F, Mackay S, Dubois J, Mellink C, Kater AP, Eldering E. JAK-STAT signalling shapes the NF-kappaB response in CLL towards venetoclax sensitivity or resistance via Bcl-XL. Mol Oncol. 2023;17(6):1112–28.

Article  CAS  PubMed  PubMed Central  Google Scholar 

Liu FT, Jia L, Wang P, Wang H, Farren TW, Agrawal SG. STAT3 and NF-kappaB cooperatively control in vitro spontaneous apoptosis and poor chemo-responsiveness in patients with chronic lymphocytic leukemia. Oncotarget. 2016;7(22):32031–45.

Article  PubMed  PubMed Central  Google Scholar 

Scuto A, Kujawski M, Kowolik C, Krymskaya L, Wang L, Weiss LM, Digiusto D, Yu H, Forman S, Jove R. STAT3 inhibition is a therapeutic strategy for ABC-like diffuse large B-cell lymphoma. Cancer Res. 2011;71(9):3182–8.

Article  CAS  PubMed  PubMed Central  Google Scholar 

Lam LT, Wright G, Davis RE, Lenz G, Farinha P, Dang L, Chan JW, Rosenwald A, Gascoyne RD, Staudt LM. Cooperative signaling through the signal transducer and activator of transcription 3 and nuclear factor-kappab pathways in subtypes of diffuse large B-cell lymphoma. Blood. 2008;111(7):3701–13.

Article  CAS  PubMed  PubMed Central  Google Scholar 

Johnson DE, O’Keefe RA, Grandis JR. Targeting the IL-6/JAK/STAT3 signalling axis in cancer. Nat Rev Clin Oncol. 2018;15(4):234–48.

Article  CAS