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Emerging Bcl-2 inhibitors for the treatment of cancer

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Pages 59-70 | Published online: 03 Sep 2010

Bibliography

  • Moffitt KL, Martin SL, Walker B. From sentencing to execution – the processes of apoptosis. J Pharm Pharmacol 2010;62:547-62
  • Cosulich SC, Worrall V, Hedge PJ, Regulation of apoptosis by BH3 domains in a cell-free system. Curr Biol 1997;16:913-20
  • Ottilie S, Diaz JL, Horne W, Dimerization properties of human BAD. Identification of a BH-3 domain and analysis of its binding to mutant BCL-2 and BCL-XL proteins. J Biol Chem 1997;272:30866-72
  • Billen LP, Shamas-Din A, Andrews DW. Bid: a Bax-like BH3 protein. Oncogene 2008;27(Suppl 1):S93-104
  • Ghiotto F, Fais F, Bruno S. BH3-only proteins: the death-puppeteer's wires. Cytometry A 2010;77:11-21
  • Akiyama T, Dass CR, Choong PF. Bim-targeted cancer therapy: a link between drug action and underlying molecular changes. Mol Cancer Ther 2009;8:3173-80
  • Danial NN. BAD: undertaker by night, candyman by day. Oncogene 2008;27(Suppl 1):S53-70
  • Yu J, Zhang L. PUMA, a potent killer with or without p53. Oncogene 2008;27(Suppl 1):S71-83
  • Ploner C, Kofler R, Villunger A. Noxa: at the tip of the balance between life and death. Oncogene 2008;27(Suppl 1):S84-92
  • Fulda S. Tumor resistance to apoptosis. Int J Cancer 2009;124:511-15
  • Fulda S. Evasion of apoptosis as a cellular stress response in cancer. Int J Cell Biol 2010;2010:370835
  • Baguley BC. Multidrug resistance in cancer. Methods Mol Biol 2010;596:1-14
  • Patel MP, Masood A, Patel PS, Chanan-Khan AA. Targeting the Bcl-2. Curr Opin Oncol 2009;21:516-23
  • Vogler M, Dinsdale D, Dyer MJ, Cohen GM. Bcl-2 inhibitors: small molecules with a big impact on cancer therapy. Cell Death Differ 2009;16:360-7
  • Ashkenazi A. Targeting the extrinsic apoptosis pathway in cancer. Cytokine Growth Factor Rev 2008;19:325-31
  • Parsons MJ, Green DR. Mitochondria in cell death. Essays Biochem 2010;47:99-114
  • Russo M, Mupo A, Spagnuolo C, Russo GL. Exploring death receptor pathways as selective targets in cancer therapy. Biochem Pharmacol 2010;80:674-82
  • Shrestha-Bhattarai T, Rangnekar VM. Cancer-selective apoptotic effects of extracellular and intracellular Par-4. Oncogene 2010;29:3873-80
  • Burikhanov R, Zhao Y, Goswami A, The tumor suppressor Par-4 activates an extrinsic pathway for apoptosis. Cell 2009;138:377-88
  • Korsmeyer SJ, Gross A, Harada H, Death and survival signals determine active/inactive conformations of pro-apoptotic BAX, BAD, and BID molecules. Cold Spring Harb Symp Quant Biol 1999;64:343-50
  • Korsmeyer SJ, Shutter JR, Veis DJ, Bcl-2/Bax: a rheostat that regulates an anti-oxidant pathway and cell death. Semin Cancer Biol 1993;4:327-32
  • Oltvai ZN, Milliman CL, Korsmeyer SJ. Bcl-2 heterodimerizes in vivo with a conserved homolog, Bax, that accelerates programmed cell death. Cell 1993;74:609-19
  • Bartholomeusz G, Wu Y, Ali SM, Nuclear translocation of the pro-apoptotic Bcl-2 family member Bok induces apoptosis. Mol Carcinog 2006;45:73-83
  • Inohara N, Ekhterae D, Garcia I, Mtd, a novel Bcl-2 family member activates apoptosis in the absence of heterodimerization with Bcl-2 and Bcl-XL. J Biol Chem 1998;273:8705-10
  • Reed CJ. Apoptosis and cancer: strategies for integrating programmed cell death. Semin Hematol 2000;37:9-16
  • Korsmeyer SJ, Wei MC, Saito M, Pro-apoptotic cascade activates BID, which oligomerizes BAK or BAX into pores that result in the release of cytochrome c. Cell DeathDiffer 2000;7:1166-73
  • Acehan D, Jiang X, Morgan DG, Three-dimensional structure of the apoptosome: implications for assembly, procaspase-9 binding, and activation. Mol Cell 2002;9:423-32
  • Chao DT, Linette GP, Boise LH, Bcl-XL and Bcl-2 repress a common pathway of cell death. J Exp Med 1995;182:821-8
  • Chao DT, Korsmeyer SJ. BCL-2 family: regulators of cell death. Annu Rev Immunol 1998;16:395-419
  • Borner C. The Bcl-2 protein family: sensors and checkpoints for life-or-death decisions. Mol Immunol 2003;39:615-47
  • Reed JC. Bcl-2 family proteins: strategies for overcoming chemoresistance in cancer. Adv Pharmacol 1997;41:501-32
  • Cotter FE. Antisense therapy for B cell lymphomas. Cancer Surv 1997;30:311-25
  • Cotter FE. Antisense therapy for lymphomas. Hematol Oncol 1997;15:3-11
  • Cotter FE, Waters J, Cunningham D. Human Bcl-2 antisense therapy for lymphomas. Biochim Biophys Acta 1999;1489:97-106
  • Morris MJ, Tong WP, Cordon-Cardo C, Phase I trial of BCL-2 antisense oligonucleotide (G3139) administered by continuous intravenous infusion in patients with advanced cancer. Clin Cancer Res 2002;8:679-83
  • Morris MJ, Cordon-Cardo C, Kelly WK, Safety and biologic activity of intravenous BCL-2 antisense oligonucleotide (G3139) and taxane chemotherapy in patients with advanced cancer. Appl Immunohistochem Mol Morphol 2005;13:6-13
  • Mohammad R, Abubakr Y, Dan M, Bcl-2 antisense oligonucleotides are effective against systemic but not central nervous system disease in severe combined immunodeficient mice bearing human t(14;18) follicular lymphoma. Clin Cancer Res 2002;8:1277-83
  • Di CC, Koropatnick J. Antisense treatment in human prostate cancer and melanoma. Curr Cancer Drug Targets 2010
  • Shah MH, Varker KA, Collamore M, G3139 (Genasense) in patients with advanced merkel cell carcinoma. Am J Clin Oncol 2009;32:174-9
  • Moulder SL, Symmans WF, Booser DJ, Phase I/II study of G3139 (Bcl-2 antisense oligonucleotide) in combination with doxorubicin and docetaxel in breast cancer. Clin Cancer Res 2008;14:7909-16
  • Liu G, Kolesar J, McNeel DG, A phase I pharmacokinetic and pharmacodynamic correlative study of the antisense Bcl-2 oligonucleotide g3139, in combination with carboplatin and paclitaxel, in patients with advanced solid tumors. Clin Cancer Res 2008;14:2732-9
  • Rudin CM, Salgia R, Wang X, Randomized phase II Study of carboplatin and etoposide with or without the bcl-2 antisense oligonucleotide oblimersen for extensive-stage small-cell lung cancer: CALGB 30103. J Clin Oncol 2008;26:870-6
  • Dai G, Wei X, Liu Z, Characterization and quantification of Bcl-2 antisense G3139 and metabolites in plasma and urine by ion-pair reversed phase HPLC coupled with electrospray ion-trap mass spectrometry. J Chromatogr B Analyt Technol Biomed Life Sci 2005;825:201-13
  • Gleave ME, Monia BP. Antisense therapy for cancer. Nat Rev Cancer 2005;5:468-79
  • Piche A, Grim J, Rancourt C, Modulation of Bcl-2 protein levels by an intracellular anti-Bcl-2 single-chain antibody increases drug-induced cytotoxicity in the breast cancer cell line MCF-7. Cancer Res 1998;58:2134-40
  • Wang JL, Zhang ZJ, Choksi S, Cell permeable Bcl-2 binding peptides: a chemical approach to apoptosis induction in tumor cells. Cancer Res 2000;60:1498-502
  • Walensky LD, Kung AL, Escher I, Activation of apoptosis in vivo by a hydrocarbon-stapled BH3 helix. Science 2004;305:1466-70
  • Walensky LD, Pitter K, Morash J, A stapled BID BH3 helix directly binds and activates BAX. Mol Cell 2006;24:199-210
  • Muchmore SW, Sattler M, Liang H, X-ray and NMR structure of human Bcl-xL, an inhibitor of programmed cell death. Nature 1996;381:335-41
  • Sattler M, Liang H, Nettesheim D, Structure of Bcl-xL-Bak peptide complex: recognition between regulators of apoptosis. Science 1997;275:983-6
  • Wang G, Nikolovska-Coleska Z, Yang CY, Structure-based design of potent small-molecule inhibitors of anti-apoptotic Bcl-2 proteins. J Med Chem 2006;49:6139-42
  • Nakashima T, Miura M, Hara M. Tetrocarcin A inhibits mitochondrial functions of Bcl-2 and suppresses its anti-apoptotic activity. Cancer Res 2000;60:1229-35
  • Tzung SP, Kim KM, Basanez G, Antimycin A mimics a cell-death-inducing Bcl-2 homology domain 3. Nat Cell Biol 2001;3:183-91
  • Kitada S, Leone M, Sareth S, Discovery, characterization, and structure-activity relationships studies of proapoptotic polyphenols targeting B-cell lymphocyte/leukemia-2 proteins. J Med Chem 2003;46:4259-64
  • Wang X, Howell CP, Chen F, Gossypol – polyphenolic compound from cotton plant. Adv Food Nutr Res 2009;58:215-63
  • Bushunow P, Reidenberg MM, Wasenko J, Gossypol treatment of recurrent adult malignant gliomas. J Neurooncol 1999;43:79-86
  • Costantino A, Cerpolini S, Perrone AM, Current status and future perspectives in male contraception. Minerva Ginecol 2007;59:299-310
  • Zaidi R, Hadi SM. Complexes involving gossypol, DNA and Cu(II). Biochem Int 1992;28:1135-43
  • Zaidi R, Hadi SM. Strand scission in DNA by gossypol and Cu(II): role of Cu(I) and oxygen-free radicals. J Biochem Toxicol 1992;7:213-17
  • Ko CH, Shen SC, Yang LY, Gossypol reduction of tumor growth through ROS-dependent mitochondria pathway in human colorectal carcinoma cells. Int J Cancer 2007;121:1670-9
  • Voss V, Senft C, Lang V, The pan-Bcl-2 inhibitor (-)-gossypol triggers autophagic cell death in malignant glioma. Mol Cancer Res 2010;7:1002-16
  • Gao P, Bauvy C, Souquere S, The BH3-mimetic gossypol induces both beclin 1-dependent and beclin 1-independent cytoprotective autophagy in cancer cells. J Biol Chem 2010;285:25570-81
  • Azmi AS, Mohammad RM. Non-peptidic small molecule inhibitors against Bcl-2 for cancer therapy. J Cell Physiol 2009;218:13-21
  • Wang Z, Song W, Aboukameel A, TW-37, a small-molecule inhibitor of Bcl-2, inhibits cell growth and invasion in pancreatic cancer. Int J Cancer 2008;123:958-66
  • Mohammad RM, Goustin AS, Aboukameel A, Preclinical studies of TW-37, a new nonpeptidic small-molecule inhibitor of Bcl-2, in diffuse large cell lymphoma xenograft model reveal drug action on both Bcl-2 and Mcl-1. Clin Cancer Res 2007;13:2226-35
  • Zeitlin BD, Joo E, Dong Z, Antiangiogenic effect of TW37, a small-molecule inhibitor of Bcl-2. Cancer Res 2006;66:8698-706
  • Azmi AS, Wang Z, Burikhanov R, Critical role of prostate apoptosis response-4 in determining the sensitivity of pancreatic cancer cells to small-molecule inhibitor-induced apoptosis. Mol Cancer Ther 2008;7:2884-93
  • Hu ZY, Sun J, Zhu XF, ApoG2 induces cell cycle arrest of nasopharyngeal carcinoma cells by suppressing the c-Myc signaling pathway. J Transl Med 2009;7:74
  • Sun J, Li ZM, Hu ZY, Apogossypolone inhibits cell growth by inducing cell cycle arrest in U937 cells. Oncol Rep 2009;22:193-8
  • Hu ZY, Zhu XF, Zhong ZD, ApoG2, a novel inhibitor of antiapoptotic Bcl-2 family proteins, induces apoptosis and suppresses tumor growth in nasopharyngeal carcinoma xenografts. Int J Cancer 2008;123:2418-29
  • Arnold AA, Aboukameel A, Chen J, 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. Mol Cancer 2008;7:20
  • van Delft MF, Wei AH, Mason KD, The BH3 mimetic ABT-737 targets selective Bcl-2 proteins and efficiently induces apoptosis via Bak/Bax if Mcl-1 is neutralized. Cancer Cell 2006;10:389-99
  • Oltersdorf T, Elmore SW, Shoemaker AR, An inhibitor of Bcl-2 family proteins induces regression of solid tumours. Nature 2005;435:677-81
  • Ackler S, Xiao Y, Mitten MJ, ABT-263 and rapamycin act cooperatively to kill lymphoma cells in vitro and in vivo. Mol Cancer Ther 2008;7:3265-74
  • Park CM, Bruncko M, Adickes J, Discovery of an orally bioavailable small molecule inhibitor of prosurvival B-cell lymphoma 2 proteins. J Med Chem 2008;51:6902-15
  • Tse C, Shoemaker AR, Adickes J, ABT-263: a potent and orally bioavailable Bcl-2 family inhibitor. Cancer Res 2008;68:3421-8
  • Tahir SK, Wass J, Joseph MK, Identification of expression signatures predictive of sensitivity to the Bcl-2 family member inhibitor ABT-263 in small cell lung carcinoma and leukemia/lymphoma cell lines. Mol Cancer Ther 2010;9:545-57
  • Li J, Viallet J, Haura EB. A small molecule pan-Bcl-2 family inhibitor, GX15-070, induces apoptosis and enhances cisplatin-induced apoptosis in non-small cell lung cancer cells. Cancer Chemother Pharmacol 2008;61:525-34
  • Trudel S, Li ZH, Rauw J, Preclinical studies of the pan-Bcl inhibitor obatoclax (GX015-070) in multiple myeloma. Blood 2007;109:5430-8
  • Smoot RL, Blechacz BR, Werneburg NW, A Bax-mediated mechanism for obatoclax-induced apoptosis of cholangiocarcinoma cells. Cancer Res 2010;70:1960-9
  • Pan J, Cheng C, Verstovsek S, The BH3-mimetic GX15-070 induces autophagy, potentiates the cytotoxicity of carboplatin and 5-fluorouracil in esophageal carcinoma cells. Cancer Lett 2010;293:167-74
  • Konopleva M, Watt J, Contractor R, Mechanisms of antileukemic activity of the novel Bcl-2 homology domain-3 mimetic GX15-070 (obatoclax). Cancer Res 2008;68:3413-20
  • Wang JL, Liu D, Zhang ZJ, Structure-based discovery of an organic compound that binds Bcl-2 protein and induces apoptosis of tumor cells. Proc Natl Acad Sci USA 2000;97:7124-9
  • Manero F, Gautier F, Gallenne T, The small organic compound HA14-1 prevents Bcl-2 interaction with Bax to sensitize malignant glioma cells to induction of cell death. Cancer Res 2006;66:2757-64
  • Zimmermann AK, Loucks FA, Le SS, Distinct mechanisms of neuronal apoptosis are triggered by antagonism of Bcl-2/Bcl-x(L) versus induction of the BH3-only protein Bim. J Neurochem 2005;94:22-36
  • Tian D, Das SG, Doshi JM, sHA 14-1, a stable and ROS-free antagonist against anti-apoptotic Bcl-2 proteins, bypasses drug resistances and synergizes cancer therapies in human leukemia cell. Cancer Lett 2008;259:198-208
  • Witham J, Valenti MR, De-Haven-Brandon AK, The Bcl-2/Bcl-XL family inhibitor ABT-737 sensitizes ovarian cancer cells to carboplatin. Clin Cancer Res 2007;13:7191-8
  • Huang S, Okumura K, Sinicrope FA. BH3 mimetic obatoclax enhances TRAIL-mediated apoptosis in human pancreatic cancer cells. Clin Cancer Res 2009;15:150-9
  • Song JH, Kandasamy K, Kraft AS. ABT-737 induces expression of the death receptor 5 and sensitizes human cancer cells to TRAIL-induced apoptosis. J Biol Chem 2008;283:25003-13
  • Traini R, Ben-Josef G, Pastrana DV, ABT-737 overcomes resistance to immunotoxin-mediated apoptosis and enhances the delivery of Pseudomonas exotoxin-based proteins to the cell cytosol. Mol Cancer Ther 2010;7:2007-15
  • Kutuk O, Letai A. Alteration of the mitochondrial apoptotic pathway is key to acquired paclitaxel resistance and can be reversed by ABT-737. Cancer Res 2008;68:7985-94
  • Bingle CD, Craig RW, Swales BM, Exon skipping in Mcl-1 results in a bcl-2 homology domain 3 only gene product that promotes cell death. J Biol Chem 2000;275:22136-46
  • Shimazu T, Degenhardt K, Nur-E-Kamal, NBK/BIK antagonizes MCL-1 and BCL-XL and activates BAK-mediated apoptosis in response to protein synthesis inhibition. Genes Dev 2007;21:929-41
  • Clohessy JG, Zhuang J, de BJ, Mcl-1 interacts with truncated Bid and inhibits its induction of cytochrome c release and its role in receptor-mediated apoptosis. J Biol Chem 2006;281:5750-9
  • Willis SN, Chen L, Dewson G, Proapoptotic Bak is sequestered by Mcl-1 and Bcl-xL, but not Bcl-2, until displaced by BH3-only proteins. Genes Dev 2005;19:1294-305
  • Al-Katib AM, Sun Y, Goustin AS, SMI of Bcl-2 TW-37 is active across a spectrum of B-cell tumors irrespective of their proliferative and differentiation status. J Hematol Oncol 2009;2:8
  • Chen S, Dai Y, Harada H, Mcl-1 down-regulation potentiates ABT-737 lethality by cooperatively inducing Bak activation and Bax translocation. Cancer Res 2007;67:782-91
  • Lin X, Morgan-Lappe S, Huang X, ‘Seed’ analysis of off-target siRNAs reveals an essential role of Mcl-1 in resistance to the small-molecule Bcl-2/Bcl-XL inhibitor ABT-737. Oncogene 2007;26:3972-9
  • Tagscherer KE, Fassl A, Campos B, Apoptosis-based treatment of glioblastomas with ABT-737, a novel small molecule inhibitor of Bcl-2 family proteins. Oncogene 2008;27:6646-56
  • Del GMV, Schlis KD, Sallan SE, BCL-2 dependence and ABT-737 sensitivity in acute lymphoblastic leukemia. Blood 2008;111:2300-9
  • Del GMV, Brown JR, Certo M, Chronic lymphocytic leukemia requires BCL2 to sequester prodeath BIM, explaining sensitivity to BCL2 antagonist ABT-737. J Clin Invest 2007;117:112-21
  • Mohammad RM, Goustin AS, Aboukameel A, Preclinical studies of TW-37, a new nonpeptidic small-molecule inhibitor of Bcl-2, in diffuse large cell lymphoma xenograft model reveal drug action on both Bcl-2 and Mcl-1. Clin Cancer Res 2007;13:2226-35
  • Liu G, Kelly WK, Wilding G, An open-label, multicenter, phase I/II study of single-agent AT-101 in men with castrate-resistant prostate cancer. Clin Cancer Res 2009;15:3172-6
  • Wang Z, Song W, Aboukameel A, TW-37, a small-molecule inhibitor of Bcl-2, inhibits cell growth and invasion in pancreatic cancer. Int J Cancer 2008;123:958-66

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