Antiapoptotic B cell leukemia/lymphoma 2 (BCL2) family proteins are expressed in many cancers, but the circumstances under which these proteins are necessary for tumor maintenance are poorly understood. We exploited a novel functional assay that uses BCL2 homology domain 3 (BH3) peptides to predict dependence on antiapoptotic proteins, a strategy we call BH3 profiling. BH3 profiling accurately predicts sensitivity to BCL2 antagonist ABT-737 in primary chronic lymphocytic leukemia (CLL) cells. BH3 profiling also accurately distinguishes myeloid cell leukemia sequence 1 (MCL1) from BCL2 dependence in myeloma cell lines. We show that the special sensitivity of CLL cells to BCL2 antagonism arises from the requirement that BCL2 tonically sequester proapoptotic BIM in CLL. ABT-737 displaced BIM from BCL2’s BH3-binding pocket, allowing BIM to activate BAX, induce mitochondrial permeabilization, and rapidly commit the CLL cell to death. Our experiments demonstrate that BCL2 expression alone does not dictate sensitivity to ABT-737. Instead, BCL2 complexed to BIM is the critical target for ABT-737 in CLL. An important implication is that in cancer, BCL2 may not effectively buffer chemotherapy death signals if it is already sequestering proapoptotic BH3-only proteins. Indeed, activator BH3-only occupation of BCL2 may prime cancer cells for death, offering a potential explanation for the marked chemosensitivity of certain cancers that express abundant BCL2, such as CLL and follicular lymphoma.
Victoria Del Gaizo Moore, Jennifer R. Brown, Michael Certo, Tara M. Love, Carl D. Novina, Anthony Letai
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P Casara, J Davidson, A Claperon, GL Toumelin-Braizat, M Vogler, A Bruno, M Chanrion, G Lysiak-Auvity, TL Diguarher, JB Starck, I Chen, N Whitehead, C Graham, N Matassova, P Dokurno, C Pedder, Y Wang, S Qiu, AM Girard, E Schneider, F Gravé, A Studeny, G Guasconi, F Rocchetti, S Maïga, JM Henlin, F Colland, L Kraus-Berthier, SL Gouill, MJ Dyer, R Hubbard, M Wood, M Amiot, GM Cohen, JA Hickman, E Morris, J Murray, O Geneste |
Oncotarget | 2018 |
BRD4 Profiling Identifies Critical Chronic Lymphocytic Leukemia Oncogenic Circuits and Reveals Sensitivity to PLX51107, a Novel Structurally Distinct BET Inhibitor
HG Ozer, D El-Gamal, B Powell, ZA Hing, JS Blachly, B Harrington, S Mitchell, NR Grieselhuber, K Williams, TH Lai, L Alinari, RA Baiocchi, L Brinton, E Baskin, M Cannon, L Beaver, VM Goettl, DM Lucas, JA Woyach, D Sampath, AM Lehman, L Yu, J Zhang, Y Ma, Y Zhang, W Spevak, S Shi, P Severson, R Shellooe, H Carias, G Tsang, K Dong, T Ewing, A Marimuthu, C Tantoy, J Walters, L Sanftner, H Rezaei, M Nespi, B Matusow, G Habets, P Ibrahim, C Zhang, EA Mathé, G Bollag, JC Byrd, R Lapalombella |
Cancer Discovery | 2018 |
DNA demethylation marks in chronic lymphocytic leukemia: it is time to let the cat out of the bag
C Bagacean, M Zdrenghea, CL Dantec, A Tempescul, C Berthou, Y Renaudineau |
Future Science OA | 2018 |
High PGAM5 expression induces chemoresistance by enhancing Bcl-xL-mediated anti-apoptotic signaling and predicts poor prognosis in hepatocellular carcinoma patients
J Cheng, D Qian, X Ding, T Song, M Cai, D Xie, Y Wang, J Zhao, Z Liu, Z Wu, Q Pang, L Zhu, P Wang, X Hao, Z Yuan |
Cell Death and Disease | 2018 |
Impaired immune surveillance accelerates accumulation of senescent cells and aging
Y Ovadya, T Landsberger, H Leins, E Vadai, H Gal, A Biran, R Yosef, A Sagiv, A Agrawal, A Shapira, J Windheim, M Tsoory, R Schirmbeck, I Amit, H Geiger, V Krizhanovsky |
Nature Communications | 2018 |
A Novel MCL1 Inhibitor Combined with Venetoclax Rescues Venetoclax-Resistant Acute Myelogenous Leukemia
HE Ramsey, MA Fischer, T Lee, AE Gorska, MP Arrate, L Fuller, KL Boyd, SA Strickland, J Sensintaffar, LJ Hogdal, GD Ayers, ET Olejniczak, SW Fesik, MR Savona |
Cancer Discovery | 2018 |
Bcl-w significantly contributes to B cell survival and lymphomagenesis
Clare Adams, Annette Kim, Ramkrishna Mitra, John Choi, Jerald Gong, Christine Eischen |
Journal of Clinical Investigation | 2017 |
Chronic lymphocytic leukaemia
TJ Kipps, FK Stevenson, CJ Wu, CM Croce, G Packham, WG Wierda, S O'Brien, J Gribben, K Rai |
Nature Reviews Disease Primers | 2017 |
Targeted activation of the SHP-1/PP2A signaling axis elicits apoptosis of chronic lymphocytic leukemia cells
E Tibaldi, MA Pagano, F Frezzato, V Trimarco, M Facco, G Zagotto, G Ribaudo, V Pavan, L Bordin, A Visentin, F Zonta, G Semenzato, AM Brunati, L Trentin |
Haematologica | 2017 |
Bruton’s tyrosine kinase inhibition increases BCL-2 dependence and enhances sensitivity to venetoclax in chronic lymphocytic leukemia
J Deng, E Isik, SM Fernandes, JR Brown, A Letai, MS Davids |
Leukemia | 2017 |
Genome-wide association analysis of chronic lymphocytic leukaemia, Hodgkin lymphoma and multiple myeloma identifies pleiotropic risk loci
PJ Law, A Sud, JS Mitchell, M Henrion, G Orlando, O Lenive, P Broderick, HE Speedy, DC Johnson, M Kaiser, N Weinhold, R Cooke, NJ Sunter, GH Jackson, G Summerfield, RJ Harris, AR Pettitt, DJ Allsup, J Carmichael, JR Bailey, G Pratt, T Rahman, C Pepper, C Fegan, EP von Strandmann, A Engert, A Försti, B Chen, MI da Filho, H Thomsen, P Hoffmann, MM Noethen, L Eisele, KH Jöckel, JM Allan, AJ Swerdlow, H Goldschmidt, D Catovsky, GJ Morgan, K Hemminki, RS Houlston |
Scientific Reports | 2017 |
The Development and Current Use of BCL-2 Inhibitors for the Treatment of Chronic Lymphocytic Leukemia
BL Lampson, MS Davids |
Current Hematologic Malignancy Reports | 2017 |
Pathways and mechanisms of venetoclax resistance
P Bose, V Gandhi, M Konopleva |
Leukemia & Lymphoma | 2017 |
Targeting BET proteins improves the therapeutic efficacy of BCL-2 inhibition in T-cell acute lymphoblastic leukemia
S Peirs, V Frismantas, F Matthijssens, WV Loocke, T Pieters, N Vandamme, B Lintermans, MP Dobay, G Berx, B Poppe, S Goossens, BC Bornhauser, JP Bourquin, PV Vlierberghe |
Leukemia | 2017 |
Pharmacotherapy of relapsed/refractory chronic lymphocytic leukemia
AA Zahr, P Bose, MJ Keating |
Expert Opinion on Pharmacotherapy | 2017 |
The Imipridone ONC201 Induces Apoptosis and Overcomes Chemotherapy Resistance by Up-Regulation of Bim in Multiple Myeloma
Y Tu, J He, H Liu, HC Lee, H Wang, J Ishizawa, JE Allen, M Andreeff, RZ Orlowski, RE Davis, J Yang |
Neoplasia (New York, N.Y.) | 2017 |
Complementary dynamic BH3 profiles predict co-operativity between the multi-kinase inhibitor TG02 and the BH3 mimetic ABT-199 in acute myeloid leukaemia cells
M Pallis, F Burrows, J Ryan, M Grundy, C Seedhouse, A Abdul-Aziz, J Montero, A Letai, N Russell |
Oncotarget | 2017 |
Why do BCL-2 inhibitors work and where should we use them in the clinic?
J Montero, A Letai |
Cell Death and Differentiation | 2017 |
Overcoming mutational complexity in acute myeloid leukemia by inhibition of critical pathways
Y Saito, Y Mochizuki, I Ogahara, T Watanabe, L Hogdal, S Takagi, K Sato, A Kaneko, H Kajita, N Uchida, T Fukami, LD Shultz, S Taniguchi, O Ohara, AG Letai, F Ishikawa |
Science Translational Medicine | 2017 |
Recent therapeutic advances in chronic lymphocytic leukemia
P Bose, V Gandhi |
F1000Research | 2017 |
The BCL-2 arbiters of apoptosis and their growing role as cancer targets
JM Adams, S Cory |
Cell Death and Differentiation | 2017 |
Bruton’s tyrosine kinase inhibitors: first and second generation agents for patients with Chronic Lymphocytic Leukemia (CLL)
PA Thompson, JA Burger |
Expert Opinion on Investigational Drugs | 2017 |
Found in Translation: How Preclinical Research Is Guiding the Clinical Development of the BCL2-Selective Inhibitor Venetoclax
JD Leverson, D Sampath, AJ Souers, SH Rosenberg, WJ Fairbrother, M Amiot, M Konopleva, A Letai |
Cancer Discovery | 2017 |
Targeted apoptosis of myofibroblasts with the BH3 mimetic ABT-263 reverses established fibrosis
D Lagares, A Santos, PE Grasberger, F Liu, CK Probst, RA Rahimi, N Sakai, T Kuehl, J Ryan, P Bhola, J Montero, M Kapoor, M Baron, X Varelas, DJ Tschumperlin, A Letai, AM Tager |
Science Translational Medicine | 2017 |
Bioluminescence Imaging Enhances Analysis of Drug Responses in a Patient-Derived Xenograft Model of Pediatric ALL
L Jones, J Richmond, K Evans, H Carol, D Jing, RT Kurmasheva, CA Billups, PJ Houghton, MA Smith, RB Lock |
Clinical cancer research | 2017 |
Control of cell death and mitochondrial fission by ERK1/2 MAP kinase signalling
SJ Cook, K Stuart, R Gilley, MJ Sale |
The FEBS journal | 2017 |
Functional precision cancer medicine—moving beyond pure genomics
A Letai |
Nature Medicine | 2017 |
Bcl-2 proteins and calcium signaling: complexity beneath the surface
T Vervliet, JB Parys, G Bultynck |
Oncogene | 2016 |
High-content screening identifies kinase inhibitors that overcome venetoclax resistance in activated CLL cells
S Oppermann, J Ylanko, Y Shi, S Hariharan, CC Oakes, PM Brauer, JC Zuniga-Pflucker, B Leber, DE Spaner, DW Andrews |
Blood | 2016 |
Select Bcl-2 antagonism restores chemotherapy sensitivity in high-risk neuroblastoma
R Tanos, D Karmali, S Nalluri, KC Goldsmith |
BMC Cancer | 2016 |
Targeting BCL2 with Venetoclax in Relapsed Chronic Lymphocytic Leukemia
AW Roberts, MS Davids, JM Pagel, BS Kahl, SD Puvvada, JF Gerecitano, TJ Kipps, MA Anderson, JR Brown, L Gressick, S Wong, M Dunbar, M Zhu, MB Desai, E Cerri, SH Enschede, RA Humerickhouse, WG Wierda, JF Seymour |
New England Journal of Medicine | 2016 |
The BH3 mimetic drug ABT-737 induces apoptosis and acts synergistically with chemotherapeutic drugs in thyroid carcinoma cells
M Broecker-Preuss, N Becher-Boveleth, S Müller, K Mann |
Cancer Cell International | 2016 |
The BCL2 selective inhibitor venetoclax induces rapid onset apoptosis of CLL cells in patients via a TP53-independent mechanism
MA Anderson, J Deng, JF Seymour, C Tam, SY Kim, J Fein, L Yu, JR Brown, D Westerman, EG Si, IJ Majewski, D Segal, SL Enschede, DC Huang, MS Davids, A Letai, AW Roberts |
Blood | 2016 |
BH3 profiling and a toolkit of BH3-mimetic drugs predict anti-apoptotic dependence of cancer cells
M Butterworth, A Pettitt, S Varadarajan, GM Cohen |
British Journal of Cancer | 2016 |
BIM mediates synergistic killing of B-cell acute lymphoblastic leukemia cells by BCL-2 and MEK inhibitors
K Korfi, M Smith, J Swan, TC Somervaille, N Dhomen, R Marais |
Cell Death and Disease | 2016 |
A fate worse than death: apoptosis as an oncogenic process
G Ichim, SW Tait |
Nature Reviews Cancer | 2016 |
Comparison of in vitro antileukemic activity of obatoclax and ABT-737
M Opydo-Chanek, L Mazur |
Tumor Biology | 2016 |
Chronic Lymphocytic Leukemia: Exploiting Vulnerabilities with Targeted Agents
J Maly, JS Blachly |
Current Hematologic Malignancy Reports | 2016 |
Directly targeting the mitochondrial pathway of apoptosis for cancer therapy using BH3 mimetics - recent successes, current challenges and future promise
KA Sarosiek, A Letai |
FEBS Journal | 2016 |
BCL2 Inhibitors as Anticancer Drugs: A Plethora of Misleading BH3 Mimetics
RS Soderquist, A Eastman |
Molecular cancer therapeutics | 2016 |
Microtubule destabilising agents: far more than just antimitotic anticancer drugs: MDA mechanisms of action
D Bates, A Eastman |
British Journal of Clinical Pharmacology | 2016 |
Duvelisib treatment is associated with altered expression of apoptotic regulators that helps in sensitization of chronic lymphocytic leukemia cells to venetoclax (ABT-199)
VM Patel, K Balakrishnan, M Douglas, T Tibbitts, EY Xu, JL Kutok, M Ayers, A Sarkar, R Guerrieri, WG Wierda, S O'Brien, N Jain, HM Stern, V Gandhi |
Leukemia | 2016 |
Targeting BCL2 With BH3 Mimetics: Basic Science and Clinical Application of Venetoclax in Chronic Lymphocytic Leukemia and Related B Cell Malignancies: Basic science and clinical application of venetoclax
AW Roberts, DC Huang |
Clinical Pharmacology & Therapeutics | 2016 |
Pharmacokinetic and pharmacodynamic evaluation of ibrutinib for the treatment of chronic lymphocytic leukemia: rationale for lower doses
P Bose, VV Gandhi, MJ Keating |
Expert Opinion on Drug Metabolism & Toxicology | 2016 |
Mitochondrial apoptosis and BH3 mimetics
H Dai, XW Meng, SH Kaufmann |
F1000Research | 2016 |
Acquired resistance to venetoclax (ABT-199) in t(14;18) positive lymphoma cells
J Bodo, X Zhao, L Durkin, AJ Souers, DC Phillips, MR Smith, ED Hsi |
Oncotarget | 2016 |
Efficacy and Biological Correlates of Response in a Phase II Study of Venetoclax Monotherapy in Patients with Acute Myelogenous Leukemia
M Konopleva, DA Pollyea, J Potluri, B Chyla, L Hogdal, T Busman, E McKeegan, AH Salem, M Zhu, JL Ricker, W Blum, CD DiNardo, T Kadia, M Dunbar, R Kirby, N Falotico, J Leverson, R Humerickhouse, M Mabry, R Stone, H Kantarjian, A Letai |
Cancer Discovery | 2016 |
Defining specificity and on-target activity of BH3-mimetics using engineered B-ALL cell lines
Koss B, Ryan J, Budhraja A, Szarama K, Yang X, Bathina M, Cardone MH, Nikolovska-Coleska Z, Letai A, Opferman JT |
Oncotarget | 2016 |
SLAMF1/CD150 regulates chemotaxis, autophagy and therapy responses in chronic lymphocytic leukemia patients
Cinzia Bologna, Roberta Buonincontri, Sara Serra, Tiziana Vaisitti, Valentina Audrito, Davide Brusa, Andrea Pagnani, Marta Coscia, Giovanni D'Arena, Elisabetta Mereu, Roberto Piva, Richard Furman, Davide Rossi, Gianluca Gaidano, Cox Terhorst, Silvia Deaglio |
Journal of Clinical Investigation | 2015 |
miR-377-dependent BCL-xL regulation drives chemotherapeutic resistance in B-cell lymphoid malignancies
S Al-harbi, GS Choudhary, JS Ebron, BT Hill, N Vivekanathan, AH Ting, T Radivoyevitch, MR Smith, GC Shukla, A Almasan |
Molecular Cancer | 2015 |
Emerging understanding of Bcl-2 biology: Implications for neoplastic progression and treatment
C Correia, SH Lee, XW Meng, ND Vincelette, KL Knorr, H Ding, GS Nowakowski, H Dai, SH Kaufmann |
Biochimica et Biophysica Acta (BBA) - Molecular Cell Research | 2015 |
The BCL2 Family: Key Mediators of the Apoptotic Response to Targeted Anticancer Therapeutics
AN Hata, JA Engelman, AC Faber |
Cancer Discovery | 2015 |
Metformin inhibits cell cycle progression of B-cell chronic lymphocytic leukemia cells
S Bruno, B Ledda, C Tenca, S Ravera, AM Orengo, AN Mazzarello, E Pesenti, S Casciaro, O Racchi, F Ghiotto, C Marini, G Sambuceti, A DeCensi, F Fais |
Oncotarget | 2015 |
Regulation of Bim in Health and Disease
RV Sionov, SA Vlahopoulos, Z Granot |
Oncotarget | 2015 |
How cell death shapes cancer
V Labi, M Erlacher |
Cell Death and Disease | 2015 |
The Evolving Role of Hematopoietic Cell Transplantation in Chronic Lymphocytic Leukemia
MS Davids, EP Alyea |
Current Hematologic Malignancy Reports | 2015 |
Potent and Specific Peptide Inhibitors of Human Pro-Survival Protein Bcl-xL
S Dutta, J Ryan, TS Chen, C Kougentakis, A Letai, AE Keating |
Journal of Molecular Biology | 2015 |
Mitochondrial Shape Governs BAX-Induced Membrane Permeabilization and Apoptosis
TT Renault, KV Floros, R Elkholi, KA Corrigan, Y Kushnareva, SY Wieder, C Lindtner, MN Serasinghe, JJ Asciolla, C Buettner, DD Newmeyer, JE Chipuk |
Molecular Cell | 2015 |
Assessment of ABT-263 activity across a cancer cell line collection leads to a potent combination therapy for small-cell lung cancer
AC Faber, AF Farago, C Costa, A Dastur, M Gomez-Caraballo, R Robbins, BL Wagner, WM Rideout, CT Jakubik, J Ham, EJ Edelman, H Ebi, AT Yeo, AN Hata, Y Song, NU Patel, RJ March, AT Tam, RJ Milano, JL Boisvert, MA Hicks, S Elmiligy, SE Malstrom, MN Rivera, H Harada, BE Windle, S Ramaswamy, CH Benes, T Jacks, JA Engelman |
Proceedings of the National Academy of Sciences | 2015 |
A phase 2 study of the BH3 mimetic BCL2 inhibitor navitoclax (ABT-263) with or without rituximab, in previously untreated B-cell chronic lymphocytic leukemia
TJ Kipps, H Eradat, S Grosicki, J Catalano, W Cosolo, I Dyagil, S Yalamanchili, A Chai, S Saharanaman, E Punnoose, D Hurst, H Pylypenko |
Leukemia & Lymphoma | 2015 |
Combining Paclitaxel with ABT-263 Has a Synergistic Effect on Paclitaxel Resistant Prostate Cancer Cells
C Wang, SB Huang, MC Yang, YT Lin, IH Chu, YN Shen, YH Chiu, SH Hung, L Kang, YR Hong, CH Chen, A Villunger |
PloS one | 2015 |
BH3 Inhibitor Sensitivity and Bcl-2 Dependence in Primary Acute Lymphoblastic Leukemia Cells
SE Alford, A Kothari, FC Loeff, JM Eichhorn, N Sakurikar, HM Goselink, RL Saylors, I Jedema, JH Falkenburg, TC Chambers |
Cancer research | 2015 |
BCL2 Inhibitor (ABT-737): A Restorer of Prednisolone Sensitivity in Early T-Cell Precursor-Acute Lymphoblastic Leukemia with High MEF2C Expression?
S Kawashima-Goto, T Imamura, C Tomoyasu, M Yano, H Yoshida, A Fujiki, S Tamura, S Osone, H Ishida, A Morimoto, H Kuroda, H Hosoi, F Bertolini |
PloS one | 2015 |
Pharmacological and Protein Profiling Suggests Venetoclax (ABT-199) as Optimal Partner with Ibrutinib in Chronic Lymphocytic Leukemia
F Cervantes-Gomez, B Lamothe, JA Woyach, WG Wierda, MJ Keating, K Balakrishnan, V Gandhi |
Clinical cancer research | 2015 |
A seven-gene expression panel distinguishing clonal expansions of pre-leukemic and chronic lymphocytic leukemia B cells from normal B lymphocytes
BA McCarthy, S Yancopoulos, M Tipping, X Yan, XP Wang, F Bennett, W Li, M Lesser, S Paul, E Boyle, C Moreno, R Catera, BT Messmer, G Cutrona, M Ferrarini, JE Kolitz, SL Allen, KR Rai, AC Rawstron, N Chiorazzi |
Immunologic Research | 2015 |
Dexamethasone treatment promotes Bcl-2 dependence in multiple myeloma resulting in sensitivity to venetoclax
SM Matulis, VA Gupta, AK Nooka, HV Hollen, JL Kaufman, S Lonial, LH Boise |
Leukemia | 2015 |
BCL-2 Antagonism to Target the Intrinsic Mitochondrial Pathway of Apoptosis
CJ Gibson, MS Davids |
Clinical cancer research | 2015 |
Clinical significance of bax/bcl-2 ratio in chronic lymphocytic leukemia
MI Principe, MD Bo, T Bittolo, F Buccisano, FM Rossi, A Zucchetto, D Rossi, R Bomben, L Maurillo, M Cefalo, GD Santis, A Venditti, G Gaidano, S Amadori, P Fabritiis, V Gattei, GD Poeta |
Haematologica | 2015 |
A synthetic peptide targeting the BH4 domain of Bcl-2 induces apoptosis in multiple myeloma and follicular lymphoma cells alone or in combination with agents targeting the BH3-binding pocket of Bcl-2
AR Lavik, F Zhong, MJ Chang, E Greenberg, Y Choudhary, MR Smith, KS McColl, J Pink, FJ Reu, S Matsuyama, CW Distelhorst |
Oncotarget | 2015 |
Isolation and Functional Analysis of Mitochondria from Cultured Cells and Mouse Tissue
T Lampl, JA Crum, TA Davis, C Milligan, VD Moore |
Journal of visualized experiments : JoVE | 2015 |
Knockdown of Peripheral Myelin Protein 22 Inhibits the Progression of Chronic Myeloid Leukemia
H Liu, H Cao, J Ta, W Zhang, Y Liu |
Oncology research | 2015 |
Co-targeting of Bcl-2 and mTOR pathway triggers synergistic apoptosis in BH3 mimetics resistant acute lymphoblastic leukemia.
Iacovelli S, Ricciardi MR, Allegretti M, Mirabilii S, Licchetta R, Bergamo P, Rinaldo C, Zeuner A, Foà R, Milella M, McCubrey JA, Martelli AM, Tafuri A |
Oncotarget | 2015 |
RPPA-based protein profiling reveals eIF4G overexpression and 4E-BP1 serine 65 phosphorylation as molecular events that correspond with a pro-survival phenotype in chronic lymphocytic leukemia
Shull AY, Noonepalle SK, Awan FT, Liu J, Pei L, Bollag RJ, Salman H, Ding Z, Shi H |
Oncotarget | 2015 |
Targeting ERK1/2-bim signaling cascades by BH3-mimetic ABT-737 as an alternative therapeutic strategy for oral cancer
Shin JA, Kim LH, Lee SJ, Jeong JH, Jung JY, Lee HN, Hong IS, Cho SD |
Oncotarget | 2015 |
The outcome of B-cell receptor signaling in chronic lymphocytic leukemia: proliferation or anergy
G Packham, S Krysov, A Allen, N Savelyeva, AJ Steele, F Forconi, FK Stevenson |
Haematologica | 2014 |
Both leukaemic and normal peripheral B lymphoid cells are highly sensitive to the selective pharmacological inhibition of prosurvival Bcl-2 with ABT-199
SL Khaw, D Mérino, MA Anderson, SP Glaser, P Bouillet, AW Roberts, DC Huang |
Leukemia | 2014 |
Cell death and the mitochondria: therapeutic targeting of the BCL-2 family-driven pathway: Therapeutic targeting of the BCL-2 family proteins
MJ Roy, A Vom, PE Czabotar, G Lessene |
British Journal of Pharmacology | 2014 |
Drp1 is dispensable for apoptotic cytochrome c release in primed MCF10A and fibroblast cells but affects Bcl-2 antagonist-induced respiratory changes: Drp1 is not required for ABT-737-induced apoptosis
P Clerc, SX Ge, H Hwang, J Waddell, BA Roelofs, M Karbowski, H Sesaki, BM Polster |
British Journal of Pharmacology | 2014 |
Radiosensitization by a novel Bcl-2 and Bcl-XL inhibitor S44563 in small-cell lung cancer
Y Loriot, P Mordant, D Dugue, O Geneste, A Gombos, P Opolon, J Guegan, JL Perfettini, A Pierre, LK Berthier, G Kroemer, JC Soria, S Depil, E Deutsch |
Cell Death and Disease | 2014 |
Putting the pieces together: How is the mitochondrial pathway of apoptosis regulated in cancer and chemotherapy?
R Elkholi, TT Renault, MN Serasinghe, JE Chipuk |
Cancer & Metabolism | 2014 |
An antiapoptotic role for telomerase RNA in human immune cells independent of telomere integrity or telomerase enzymatic activity
FS Gazzaniga, EH Blackburn |
Blood | 2014 |
A Bim-targeting strategy overcomes adaptive bortezomib resistance in myeloma through a novel link between autophagy and apoptosis
S Chen, Y Zhang, L Zhou, Y Leng, H Lin, M Kmieciak, XY Pei, R Jones, RZ Orlowski, Y Dai, S Grant |
Blood | 2014 |
Maturation Stage of T-cell Acute Lymphoblastic Leukemia Determines BCL-2 versus BCL-XL Dependence and Sensitivity to ABT-199
TN Chonghaile, JE Roderick, C Glenfield, J Ryan, SE Sallan, LB Silverman, ML Loh, SP Hunger, B Wood, DJ DeAngelo, R Stone, M Harris, A Gutierrez, MA Kelliher, A Letai |
Cancer Discovery | 2014 |
B Cell Lymphoma-2 (BCL-2) Homology Domain 3 (BH3) Mimetics Demonstrate Differential Activities Dependent upon the Functional Repertoire of Pro- and Anti-apoptotic BCL-2 Family Proteins
TT Renault, R Elkholi, A Bharti, JE Chipuk |
The Journal of biological chemistry | 2014 |
Rational combination of dual PI3K/mTOR blockade and Bcl-2/-xL inhibition in AML
P Vachhani, P Bose, M Rahmani, S Grant |
Physiological genomics | 2014 |
Inhibition of Phosphatidylinositol 3-Kinase/AKT Signaling by NVP-BKM120 Promotes ABT-737-Induced Toxicity in a Caspase-Dependent Manner through Mitochondrial Dysfunction and DNA Damage Response in Established and Primary Cultured Glioblastoma Cells
EP Jane, DR Premkumar, A Morales, KA Foster, IF Pollack |
The Journal of pharmacology and experimental therapeutics | 2014 |
Apoptosis inducers in chronic lymphocytic leukemia.
Billard C |
Oncotarget | 2014 |
PUMA and BIM Are Required for Oncogene Inactivation–Induced Apoptosis
GR Bean, YT Ganesan, Y Dong, S Takeda, H Liu, PM Chan, Y Huang, LA Chodosh, GP Zambetti, JJ Hsieh, EH Cheng |
Science signaling | 2013 |
MicroRNAs and Glucocorticoid-Induced Apoptosis in Lymphoid Malignancies
RV Sionov |
ISRN Hematology | 2013 |
ABT-199, a new Bcl-2-specific BH3 mimetic, has in vivo efficacy against aggressive Myc-driven mouse lymphomas without provoking thrombocytopenia
CJ Vandenberg, S Cory |
Blood | 2013 |
Emerging Drug Profile: Cyclin-Dependent Kinase Inhibitors
JS Blachly, JC Byrd |
Leukemia & Lymphoma | 2013 |
pRb/E2F-1-mediated caspase-dependent induction of Noxa amplifies the apoptotic effects of the Bcl-2/Bcl-xL inhibitor ABT-737
J Bertin-Ciftci, B Barré, JL Pen, L Maillet, C Couriaud, P Juin, F Braun |
Cell Death and Differentiation | 2013 |
Impact of bone marrow stromal cells on Bcl-2 family members in chronic lymphocytic leukemia
V Patel, K Balakrishnan, WG Wierda, V Gandhi |
Leukemia & Lymphoma | 2013 |
Decoding and unlocking the BCL-2 dependency of cancer cells
P Juin, O Geneste, F Gautier, S Depil, M Campone |
Nature Reviews Cancer | 2013 |
Bcl-2 antagonists: a proof of concept for CLL therapy
K Balakrishnan, V Gandhi |
Investigational New Drugs | 2013 |
Evaluation and critical assessment of putative MCL-1 inhibitors
S Varadarajan, M Vogler, M Butterworth, D Dinsdale, LD Walensky, GM Cohen |
Cell Death and Differentiation | 2013 |
Control of apoptosis by the BCL-2 protein family: implications for physiology and therapy
PE Czabotar, G Lessene, A Strasser, JM Adams |
Nature Reviews Molecular Cell Biology | 2013 |
Mantle cell lymphoma in cyclin D1 transgenic mice with Bim-deficient B cells
SG Katz, JL LaBelle, H Meng, RP Valeriano, JK Fisher, H Sun, SJ Rodig, SH Kleinstein, LD Walensky |
Blood | 2013 |
Requirement for antiapoptotic MCL-1 in the survival of BCR-ABL B-lineage acute lymphoblastic leukemia
B Koss, J Morrison, RM Perciavalle, H Singh, JE Rehg, RT Williams, JT Opferman |
Blood | 2013 |
Priming BCL-2 to kill: the combination therapy of tamoxifen and ABT-199 in ER+ breast cancer
J Deng, A Letai |
Breast Cancer Research | 2013 |
BH3 profiling discriminates response to cytarabine-based treatment of acute myelogenous leukemia
WE Pierceall, SM Kornblau, NE Carlson, X Huang, N Blake, R Lena, M Elashoff, M Konopleva, MH Cardone, M Andreeff |
Molecular cancer therapeutics | 2013 |
Metastatic SW620 colon cancer cells are primed for death when detached and can be sensitized to anoikis by the BH3-mimetic ABT-737
A Maamer-Azzabi, O Ndozangue-Touriguine, J Bréard |
Cell Death and Disease | 2013 |
Modifying chemotherapy response by targeted inhibition of eukaryotic initiation factor 4A
R Cencic, F Robert, G Galicia-Vázquez, A Malina, K Ravindar, R Somaiah, P Pierre, J Tanaka, P Deslongchamps, J Pelletier |
Blood Cancer Journal | 2013 |
IP3R2 levels dictate the apoptotic sensitivity of diffuse large B-cell lymphoma cells to an IP3R-derived peptide targeting the BH4 domain of Bcl-2
H Akl, G Monaco, RL Rovere, K Welkenhuyzen, S Kiviluoto, T Vervliet, J Molgó, CW Distelhorst, L Missiaen, K Mikoshiba, JB Parys, HD Smedt, G Bultynck |
Cell Death and Disease | 2013 |
The sensitivity of diffuse large B-cell lymphoma cell lines to histone deacetylase inhibitor-induced apoptosis is modulated by BCL-2 family protein activity
RC Thompson, I Vardinogiannis, TD Gilmore |
PloS one | 2013 |
An evidence-based review of obatoclax mesylate in the treatment of hematological malignancies
CA Goard, AD Schimmer |
Core evidence | 2013 |
HA14-1, but not the BH3 mimetic ABT-737, causes Ca2+ dysregulation in platelets and human cell lines
H Akl, I Vandecaetsbeek, G Monaco, A Kauskot, T Luyten, K Welkenhuyzen, M Hoylaerts, HD Smedt, JB Parys, G Bultynck |
Haematologica | 2013 |
Selective BCL-2 inhibition by ABT-199 causes on-target cell death in acute myeloid leukemia
R Pan, LJ Hogdal, JM Benito, D Bucci, L Han, G Borthakur, J Cortes, DJ DeAngelo, L Debose, H Mu, H Döhner, VI Gaidzik, I Galinsky, LS Golfman, T Haferlach, KG Harutyunyan, J Hu, JD Leverson, G Marcucci, M Müschen, R Newman, E Park, PP Ruvolo, V Ruvolo, J Ryan, S Schindela, P Zweidler-McKay, RM Stone, H Kantarjian, M Andreeff, M Konopleva, AG Letai |
Cancer Discovery | 2013 |
Vinblastine rapidly induces NOXA and acutely sensitizes primary chronic lymphocytic leukemia cells to ABT-737
DJ Bates, AV Danilov, CH Lowrey, A Eastman |
Molecular cancer therapeutics | 2013 |
That which does not kill me makes me stronger; combining ERK1/2 pathway inhibitors and BH3 mimetics to kill tumour cells and prevent acquired resistance
MJ Sale, SJ Cook |
British Journal of Pharmacology | 2013 |
RNAi screening uncovers Dhx9 as a modifier of ABT-737 resistance in an Eμ-myc/Bcl-2 mouse model
JR Mills, A Malina, T Lee, DD Paola, O Larsson, C Miething, F Grosse, H Tang, M Zannis-Hadjopoulos, SW Lowe, J Pelletier |
Blood | 2013 |
ABT-199: A New Hope for Selective BCL-2 Inhibition
MS Davids, A Letai |
Cancer Cell | 2013 |
Customized chemotherapy in metastatic non-small cell lung cancer (NSCLC)
Jia Wei, Teresa Moran, Zhengyun Zou, Xiaoping Qian, Lifeng Wang, Carlos Camps, Wenjing Hu, Imane Chaib, Belén Sanchez, Lixia Xu, Niki Karachaliou, María Sanchez-Ronco, Baorui Liu, Rafael Rosell |
Translational Lung Cancer Research | 2013 |
TYK2–STAT1–BCL2 Pathway Dependence in T-cell Acute Lymphoblastic Leukemia
T Sanda, JW Tyner, A Gutierrez, VN Ngo, J Glover, BH Chang, A Yost, W Ma, AG Fleischman, W Zhou, Y Yang, M Kleppe, Y Ahn, J Tatarek, MA Kelliher, DS Neuberg, RL Levine, R Moriggl, M Müller, NS Gray, CH Jamieson, AP Weng, LM Staudt, BJ Druker, AT Look |
Cancer Discovery | 2013 |
mTOR Inhibition Specifically Sensitizes Colorectal Cancers with KRAS or BRAF Mutations to BCL-2/BCL-XL Inhibition by Suppressing MCL-1
AC Faber, EM Coffee, C Costa, A Dastur, H Ebi, AN Hata, AT Yeo, EJ Edelman, Y Song, AT Tam, JL Boisvert, RJ Milano, J Roper, DP Kodack, RK Jain, RB Corcoran, MN Rivera, S Ramaswamy, KE Hung, CH Benes, JA Engelman |
Cancer Discovery | 2013 |
Mitochondrial Bcl-2 family dynamics define therapy response and resistance in neuroblastoma
KC Goldsmith, M Gross, S Peirce, D Luyindula, X Liu, A Vu, M Sliozberg, R Guo, H Zhao, CP Reynolds, MD Hogarty |
Cancer research | 2012 |
Bcl-2, Bcl-x(L), and Bcl-w are not equivalent targets of ABT-737 and navitoclax (ABT-263) in lymphoid and leukemic cells
D Mérino, SL Khaw, SP Glaser, DJ Anderson, LD Belmont, C Wong, P Yue, M Robati, B Phipson, WD Fairlie, EF Lee, KJ Campbell, CJ Vandenberg, S Cory, AW Roberts, MJ Ludlam, DC Huang, P Bouillet |
Blood | 2012 |
Decreased mitochondrial apoptotic priming underlies stroma-mediated treatment resistance in chronic lymphocytic leukemia
MS Davids, J Deng, A Wiestner, BJ Lannutti, L Wang, CJ Wu, WH Wilson, JR Brown, A Letai |
Blood | 2012 |
Targeting the B-Cell Lymphoma/Leukemia 2 Family in Cancer
MS Davids, A Letai |
Journal of Clinical Oncology | 2012 |
Glucocorticoid resistance in chronic lymphocytic leukaemia is associated with a failure of upregulated Bim/Bcl-2 complexes to activate Bax and Bak
T Melarangi, J Zhuang, K Lin, N Rockliffe, AG Bosanquet, M Oates, JR Slupsky, AR Pettitt |
Cell Death and Disease | 2012 |
Rapid Detection of an ABT-737-Sensitive Primed for Death State in Cells Using Microplate-Based Respirometry
P Clerc, GB Carey, Z Mehrabian, M Wei, H Hwang, GD Girnun, H Chen, SS Martin, BM Polster |
PloS one | 2012 |
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
RW Rooswinkel, B de Kooij, M Verheij, J Borst |
Cell Death and Disease | 2012 |
The selective BH4-domain biology of Bcl-2-family members: IP3Rs and beyond
G Monaco, T Vervliet, H Akl, G Bultynck |
Cellular and Molecular Life Sciences | 2012 |
A Competitive Stapled Peptide Screen Identifies a Selective Small Molecule that Overcomes MCL-1-Dependent Leukemia Cell Survival
NA Cohen, ML Stewart, E Gavathiotis, JL Tepper, SR Bruekner, B Koss, JT Opferman, LD Walensky |
Chemistry & Biology | 2012 |
Biomarkers of Therapeutic Response to BCL2 Antagonists in Cancer
LT Lam, H Zhang, B Chyla |
Molecular diagnosis & therapy | 2012 |
Targeting the Bcl-2 family for cancer therapy
S Thomas, BA Quinn, SK Das, R Dash, L Emdad, S Dasgupta, XY Wang, P Dent, JC Reed, M Pellecchia, D Sarkar, PB Fisher |
Expert Opinion on Therapeutic Targets | 2012 |
Therapeutic effects of deleting cancer-associated fibroblasts in cholangiocarcinoma
JC Mertens, CD Fingas, JD Christensen, RL Smoot, SF Bronk, NW Werneburg, MP Gustafson, AB Dietz, LR Roberts, AE Sirica, GJ Gores |
Cancer research | 2012 |
Structural biology of the intrinsic cell death pathway: what do we know and what is missing?
EF Lee, WD Fairlie |
Computational and Structural Biotechnology Journal | 2012 |
ABT-737 induces Bim expression via JNK signaling pathway and its effect on the radiation sensitivity of HeLa cells
H Wang, YB Yang, HM Shen, J Gu, T Li, XM Li |
PloS one | 2012 |
Dual inhibition of Bcl-2 and Bcl-xL strikingly enhances PI3K inhibition-induced apoptosis in human myeloid leukemia cells through a GSK3- and Bim-dependent mechanism
M Rahmani, MM Aust, E Attkisson, DC Williams, A Ferreira-Gonzalez, S Grant |
Cancer research | 2012 |
B-lymphopoiesis is stopped by mobilizing doses of G-CSF and is rescued by overexpression of the anti-apoptotic protein Bcl2
IG Winkler, LJ Bendall, CE Forristal, F Helwani, B Nowlan, V Barbier, Y Shen, A Cisterne, LM Sedger, JP Levesque |
Haematologica | 2012 |
Understanding sensitivity to BH3 mimetics: ABT-737 as a case study to foresee the complexities of personalized medicine
VA Stamelos, CW Redman, A Richardson |
Journal of molecular signaling | 2012 |
BH3-only proteins in apoptosis at a glance
L Happo, A Strasser, S Cory |
Journal of cell science | 2012 |
ABT-737 synergizes with bortezomib to induce apoptosis, mediated by Bid cleavage, Bax activation, and mitochondrial dysfunction in an Akt-dependent context in malignant human glioma cell lines
DR Premkumar, EP Jane, JD DiDomenico, NA Vukmer, NR Agostino, IF Pollack |
The Journal of pharmacology and experimental therapeutics | 2012 |
BH3 profiling--measuring integrated function of the mitochondrial apoptotic pathway to predict cell fate decisions
VD Moore, A Letai |
Cancer Letters | 2012 |
BCL2 suppresses PARP1 function and nonapoptotic cell death
C Dutta, T Day, N Kopp, D Bodegom, MS Davids, J Ryan, L Bird, N Kommajosyula, O Weigert, A Yoda, H Fung, JR Brown, GI Shapiro, A Letai, DM Weinstock |
Cancer research | 2012 |
The Role of BCL2 Family of Apoptosis Regulator Proteins in Acute and Chronic Leukemias
F Tzifi, C Economopoulou, D Gourgiotis, A Ardavanis, S Papageorgiou, A Scorilas |
Advances in Hematology | 2012 |
Phosphoinositide 3-kinase/AKT/mTORC1/2 Signaling Determines Sensitivity of Burkitt's Lymphoma Cells to BH3 mimetics
LC Spender, GJ Inman |
Molecular cancer research : MCR | 2012 |
Targeting the regulatory machinery of BIM for cancer therapy.
Harada H, Grant S |
Critical reviews in eukaryotic gene expression | 2012 |
Sensitization of BCL-2–expressing breast tumors to chemotherapy by the BH3 mimetic ABT-737
SR Oakes, F Vaillant, E Lim, L Lee, K Breslin, F Feleppa, S Deb, ME Ritchie, E Takano, T Ward, SB Fox, D Generali, GK Smyth, A Strasser, DC Huang, JE Visvader, GJ Lindeman |
Proceedings of the National Academy of Sciences | 2011 |
Bcl-x(L) blocks a mitochondrial inner membrane channel and prevents Ca2+ overload-mediated cell death
D Tornero, I Posadas, V Ceña |
PloS one | 2011 |
Emerging Bcl-2 inhibitors for the treatment of cancer
AS Azmi, Z Wang, PA Philip, RM Mohammad, FH Sarkar |
Expert Opinion on Emerging Drugs | 2011 |
An antiapoptotic BCL-2 family expression index predicts the response of chronic lymphocytic leukemia to ABT-737
S Al-harbi, BT Hill, S Mazumder, K Singh, J DeVecchio, G Choudhary, LA Rybicki, M Kalaycio, JP Maciejewski, JA Houghton, A Almasan |
Blood | 2011 |
Inhibitors of the anti-apoptotic Bcl-2 proteins: a patent review
N Bajwa, C Liao, Z Nikolovska-Coleska |
Expert Opinion on Therapeutic Patents | 2011 |
Histone deacetylases mediate the silencing of miR-15a, miR-16, and miR-29b in chronic lymphocytic leukemia
D Sampath, C Liu, K Vasan, M Sulda, VK Puduvalli, WG Wierda, MJ Keating |
Blood | 2011 |
Multiple BH3 Mimetics Antagonize Antiapoptotic MCL1 Protein by Inducing the Endoplasmic Reticulum Stress Response and Up-regulating BH3-only Protein NOXA*
TC Albershardt, BL Salerni, RS Soderquist, DJ Bates, AA Pletnev, AF Kisselev, A Eastman |
The Journal of biological chemistry | 2011 |
Homoharringtonine reduced Mcl-1 expression and induced apoptosis in chronic lymphocytic leukemia
R Chen, L Guo, Y Chen, Y Jiang, WG Wierda, W Plunkett |
Blood | 2011 |
Distribution of Bim determines Mcl-1 dependence or codependence with Bcl-xL/Bcl-2 in Mcl-1–expressing myeloma cells
AA Morales, M Kurtoglu, SM Matulis, J Liu, D Siefker, DM Gutman, JL Kaufman, KP Lee, S Lonial, LH Boise |
Blood | 2011 |
Pretreatment Mitochondrial Priming Correlates with Clinical Response to Cytotoxic Chemotherapy
TN Chonghaile, KA Sarosiek, TT Vo, JA Ryan, A Tammareddi, VD Moore, J Deng, KC Anderson, P Richardson, YT Tai, CS Mitsiades, UA Matulonis, R Drapkin, R Stone, DJ Deangelo, DJ McConkey, SE Sallan, L Silverman, MS Hirsch, DR Carrasco, A Letai |
Science (New York, N.Y.) | 2011 |
SAR by Inter-Ligand nuclear Overhauser Effects (ILOEs) based discovery of acylsulfonamide compounds active against Bcl-xL and Mcl-1
MF Rega, B Wu, J Wei, Z Zhang, JF Cellitti, M Pellecchia |
Journal of Medicinal Chemistry | 2011 |
Decreased sensitivity of 17p-deleted chronic lymphocytic leukemia cells to a small molecule BCL-2 antagonist ABT-737
K Kojima, S Duvvuri, V Ruvolo, F Samaniego, A Younes, M Andreeff |
Cancer | 2011 |
Synergistic Activity of Fenretinide and the Bcl-2 Family Protein Inhibitor ABT-737 against Human Neuroblastoma
H Fang, TM Harned, O Kalous, V Maldonado, YA DeClerck, CP Reynolds |
Clinical cancer research | 2011 |
Substantial Susceptibility of Chronic Lymphocytic Leukemia to BCL2 Inhibition: Results of a Phase I Study of Navitoclax in Patients With Relapsed or Refractory Disease
AW Roberts, JF Seymour, JR Brown, WG Wierda, TJ Kipps, SL Khaw, DA Carney, SZ He, DC Huang, H Xiong, Y Cui, TA Busman, EM McKeegan, AP Krivoshik, SH Enschede, R Humerickhouse |
Journal of Clinical Oncology | 2011 |
Induction of Ca2+-driven apoptosis in chronic lymphocytic leukemia cells by peptide-mediated disruption of Bcl-2–IP3 receptor interaction
F Zhong, MW Harr, G Bultynck, G Monaco, JB Parys, HD Smedt, YP Rong, JK Molitoris, M Lam, C Ryder, S Matsuyama, CW Distelhorst |
Blood | 2010 |
The Beclin 1 interactome
C He, B Levine |
Current Opinion in Cell Biology | 2010 |
Bim-Bcl-2 homology 3 mimetic therapy is effective at suppressing inflammatory arthritis through the activation of myeloid cell apoptosis
JC Scatizzi, J Hutcheson, RM Pope, GS Firestein, AE Koch, M Mavers, A Smason, H Agrawal, GK 3rd, NS Chandel, RS Hotchkiss, H Perlman |
Arthritis & Rheumatism | 2010 |
Bax activation by engagement with, then release from, the BH3 binding site of Bcl-xL
F Gautier, Y Guillemin, PF Cartron, T Gallenne, N Cauquil, TL Diguarher, P Casara, FM Vallette, S Manon, JA Hickman, O Geneste, P Juin |
Molecular and cellular biology | 2010 |
Heightened mitochondrial priming is the basis for apoptotic hypersensitivity of CD4+ CD8+ thymocytes
JA Ryan, JK Brunelle, A Letai |
Proceedings of the National Academy of Sciences | 2010 |
Diminished sensitivity of chronic lymphocytic leukemia cells to ABT-737 and ABT-263 due to albumin binding in blood
M Vogler, SD Furdas, M Jung, T Kuwana, MJ Dyer, GM Cohen |
Clinical cancer research | 2010 |
Displacement of Bim by Bmf and Puma rather than increase in Bim level mediates paclitaxel-induced apoptosis in breast cancer cells
O Kutuk, A Letai |
Cell Death and Differentiation | 2010 |
Acquired resistance to ABT-737 in lymphoma cells that up-regulate MCL-1 and BFL-1
D Yecies, NE Carlson, J Deng, A Letai |
Blood | 2010 |
Mitochondrial control of caspase-dependent and -independent cell death
LA Pradelli, M Bénéteau, JE Ricci |
Cellular and Molecular Life Sciences | 2010 |
Safety, Pharmacokinetics, Pharmacodynamics, and Activity of Navitoclax, a Targeted High Affinity Inhibitor of BCL-2, in Lymphoid Malignancies
WH Wilson, OA O'Connor, MS Czuczman, AS LaCasce, JF Gerecitano, JP Leonard, A Tulpule, K Dunleavy, H Xiong, YL Chiu, Y Cui, T Busman, SW Elmore, SH Rosenberg, AP Krivoshik, SH Enschede, RA Humerickhouse |
The Lancet Oncology | 2010 |
BH3 Domains other than Bim and Bid Can Directly Activate Bax/Bak*
H Du, J Wolf, B Schafer, T Moldoveanu, JE Chipuk, T Kuwana |
The Journal of biological chemistry | 2010 |
Inflammation and survival pathways: chronic lymphocytic leukemia as a model system
LS Chen, K Balakrishnan, V Gandhi |
Biochemical Pharmacology | 2010 |
The BH3 mimetic ABT-737 induces cancer cell senescence
JH Song, K Kandasamy, M Zemskova, YW Lin, AS Kraft |
Cancer research | 2010 |
The BCL-2 Family Reunion
JE Chipuk, T Moldoveanu, F Llambi, MJ Parsons, DR Green |
Molecular Cell | 2010 |
Phase I and Pharmacologic Study of SNS-032, a Potent and Selective Cdk2, 7, and 9 Inhibitor, in Patients With Advanced Chronic Lymphocytic Leukemia and Multiple Myeloma
WG Tong, R Chen, W Plunkett, D Siegel, R Sinha, RD Harvey, AZ Badros, L Popplewell, S Coutre, JA Fox, K Mahadocon, T Chen, P Kegley, U Hoch, WG Wierda |
Journal of Clinical Oncology | 2010 |
Small-Molecule Inhibitors of Protein-Protein Interactions
L Vassilev, D Fry |
2010 | |
A Bax-Mediated Mechanism for Obatoclax-Induced Apoptosis of Cholangiocarcinoma Cells
RL Smoot, BR Blechacz, NW Werneburg, SF Bronk, FA Sinicrope, AE Sirica, GJ Gores |
Cancer research | 2010 |
BH3-only proteins and their effects on cancer.
Vo TT, Letai A |
Advances in experimental medicine and biology | 2010 |
MCL-1-dependent leukemia cells are more sensitive to chemotherapy than BCL-2-dependent counterparts
JK Brunelle, J Ryan, D Yecies, JT Opferman, A Letai |
The Journal of Cell Biology | 2009 |
Pulmonary surfactant: an immunological perspective
ZC Chroneos, Z Sever-Chroneos, VL Shepherd |
Cellular physiology and biochemistry : international journal of experimental cellular physiology, biochemistry, and pharmacology | 2009 |
The liver's dance with death: two Bcl-2 guardian proteins from the abyss
SC Cazanave, GJ Gores |
Hepatology | 2009 |
Combination of novel proteasome inhibitor NPI-0052 and lenalidomide trigger in vitro and in vivo synergistic cytotoxicity in multiple myeloma
D Chauhan, AV Singh, B Ciccarelli, PG Richardson, MA Palladino, KC Anderson |
Blood | 2009 |
Bax activation by the BH3-only protein Puma promotes cell dependence on antiapoptotic Bcl-2 family members
T Gallenne, F Gautier, L Oliver, E Hervouet, B Noël, JA Hickman, O Geneste, PF Cartron, FM Vallette, S Manon, P Juin |
The Journal of Cell Biology | 2009 |
ABT-737 synergizes with chemotherapy to kill head and neck squamous cell carcinoma cells via a Noxa-mediated pathway
R Li, Y Zang, C Li, NS Patel, JR Grandis, DE Johnson |
Molecular pharmacology | 2009 |
Mechanism of action of SNS-032, a novel cyclin-dependent kinase inhibitor, in chronic lymphocytic leukemia
R Chen, WG Wierda, S Chubb, RE Hawtin, JA Fox, MJ Keating, V Gandhi, W Plunkett |
Blood | 2009 |
Unleashing the power of inhibitors of oncogenic kinases through BH3 mimetics
MS Cragg, C Harris, A Strasser, CL Scott |
Nature Reviews Cancer | 2009 |
BH3 response profiles from neuroblastoma mitochondria predict activity of small molecule Bcl-2 family antagonists
KC Goldsmith, BJ Lestini, M Gross, L Ip, A Bhumbla, X Zhang, H Zhao, X Liu, MD Hogarty |
Cell Death and Differentiation | 2009 |
Bcl2 family proteins in carcinogenesis and the treatment of cancer
A Frenzel, F Grespi, W Chmelewskij, A Villunger |
Apoptosis | 2009 |
Bcl-2 Inhibitors: Targeting Mitochondrial Apoptotic Pathways in Cancer Therapy
MH Kang, CP Reynolds |
Clinical cancer research | 2009 |
Chronic Lymphocytic Leukemia and B and T Cells Differ in Their Response to Cyclic Nucleotide Phosphodiesterase Inhibitors
JA Meyers, DW Su, A Lerner |
Journal of immunology (Baltimore, Md. : 1950) | 2009 |
Bim Upregulation by Histone Deacetylase Inhibitors Mediates Interactions with the Bcl-2 Antagonist ABT-737: Evidence for Distinct Roles for Bcl-2, Bcl-xL, and Mcl-1
S Chen, Y Dai, XY Pei, S Grant |
Molecular and cellular biology | 2009 |
Control of mitochondrial apoptosis by the Bcl-2 family
JK Brunelle, A Letai |
Journal of cell science | 2009 |
PUMA cooperates with direct activator proteins to promote mitochondrial outer membrane permeabilization and apoptosis.
Chipuk JE, Green DR |
Cell cycle (Georgetown, Tex.) | 2009 |
EPO receptor circuits for primary erythroblast survival
P Sathyanarayana, A Dev, J Fang, E Houde, O Bogacheva, O Bogachev, M Menon, S Browne, A Pradeep, C Emerson, DM Wojchowski |
Blood | 2008 |
Bim and Bmf in tissue homeostasis and malignant disease
JD Piñon, V Labi, A Egle, A Villunger |
Oncogene | 2008 |
ABT-737 induces expression of the death receptor 5 and sensitizes human cancer cells to TRAIL-induced apoptosis
JH Song, K Kandasamy, AS Kraft |
The Journal of biological chemistry | 2008 |
Mechanism of apoptosis induction by inhibition of the anti-apoptotic BCL-2 proteins
JE Chipuk, JC Fisher, CP Dillon, RW Kriwacki, T Kuwana, DR Green |
Proceedings of the National Academy of Sciences | 2008 |
In vivo efficacy of the Bcl-2 antagonist ABT-737 against aggressive Myc-driven lymphomas
KD Mason, CJ Vandenberg, CL Scott, AH Wei, S Cory, DC Huang, AW Roberts |
Proceedings of the National Academy of Sciences | 2008 |
AT-101 induces apoptosis in CLL B cells and overcomes stromal cell-mediated Mcl-1 induction and drug resistance
K Balakrishnan, JA Burger, WG Wierda, V Gandhi |
Blood | 2008 |
Surface expression of Bcl-2 in chronic lymphocytic leukemia and other B-cell leukemias and lymphomas without a breakpoint t(14;18)
BA McCarthy, E Boyle, XP Wang, D Guzowski, S Paul, R Catera, J Trott, X Yan, CM Croce, R Damle, S Yancopoulos, BT Messmer, M Lesser, SL Allen, KR Rai, N Chiorazzi |
Molecular Medicine | 2008 |
Gossypol, a BH3 mimetic, induces apoptosis in chronic lymphocytic leukemia cells
K Balakrishnan, WG Wierda, MJ Keating, V Gandhi |
Blood | 2008 |
BH3 mimetic ABT-737 potentiates TRAIL-mediated apoptotic signaling by unsequestering Bim and Bak in human pancreatic cancer cells
S Huang, FA Sinicrope |
Cancer research | 2008 |
Preclinical studies of Apogossypolone: a new nonpeptidic pan small-molecule inhibitor of Bcl-2, Bcl-XL and Mcl-1 proteins in Follicular Small Cleaved Cell Lymphoma model
AA Arnold, A Aboukameel, J Chen, D Yang, S Wang, A Al-Katib, RM Mohammad |
Molecular Cancer | 2008 |
Postnatal developmental regulation of Bcl-2 family proteins in brain mitochondria
L Soane, ZT Siegel, RA Schuh, G Fiskum |
Journal of Neuroscience Research | 2008 |
Targeting the Bcl-2-regulated apoptosis pathway by BH3 mimetics: a breakthrough in anticancer therapy?
V Labi, F Grespi, F Baumgartner, A Villunger |
Cell Death and Differentiation | 2008 |
How do BCL-2 proteins induce mitochondrial outer membrane permeabilization?
JE Chipuk, DR Green |
Trends in Cell Biology | 2008 |
Mimicking the BH3 domain to kill cancer cells
TN Chonghaile, A Letai |
Oncogene | 2008 |
Alteration of the Mitochondrial Apoptotic Pathway Is Key to Acquired Paclitaxel Resistance and Can Be Reversed by ABT-737
O Kutuk, A Letai |
Cancer research | 2008 |
Small-molecule Bcl-2 antagonists as targeted therapy in oncology.
Warr MR, Shore GC |
Current oncology (Toronto, Ont.) | 2008 |
Bcl-2-regulated apoptosis: mechanism and therapeutic potential
JM Adams, S Cory |
Current Opinion in Immunology | 2007 |
BCL-2 dependence and ABT-737 sensitivity in acute lymphoblastic leukemia
VD Moore, KD Schlis, SE Sallan, SA Armstrong, A Letai |
Blood | 2007 |
Induction of BIM is essential for apoptosis triggered by EGFR kinase inhibitors in mutant EGFR-dependent lung adenocarcinomas
Y Gong, R Somwar, K Politi, M Balak, J Chmielecki, X Jiang, W Pao |
PLoS Medicine | 2007 |
BH3 mimetics to improve cancer therapy; mechanisms and examples
L Zhang, L Ming, J Yu |
Drug resistance updates : reviews and commentaries in antimicrobial and anticancer chemotherapy | 2007 |
The cancer cell’s “power plants” as promising therapeutic targets: An overview
PL Pedersen |
Journal of Bioenergetics and Biomembranes | 2007 |