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Inhibition of Bfl-1 with N-aryl maleimides.

Cashman JR, MacDonald M, Ghirmai S, Okolotowicz KJ, Sergienko E, Brown B, Garcia X, Zhai D, Dahl R, Reed JC.

Bioorg Med Chem Lett. 2010 Nov 15;20(22):6560-4. doi: 10.1016/j.bmcl.2010.09.046.


Towards patient-based cancer therapeutics.

Cancer Target Discovery and Development Network., Schreiber SL, Shamji AF, Clemons PA, Hon C, Koehler AN, Munoz B, Palmer M, Stern AM, Wagner BK, Powers S, Lowe SW, Guo X, Krasnitz A, Sawey ET, Sordella R, Stein L, Trotman LC, Califano A, Dalla-Favera R, Ferrando A, Iavarone A, Pasqualucci L, Silva J, Stockwell BR, Hahn WC, Chin L, DePinho RA, Boehm JS, Gopal S, Huang A, Root DE, Weir BA, Gerhard DS, Zenklusen JC, Roth MG, White MA, Minna JD, MacMillan JB, Posner BA.

Nat Biotechnol. 2010 Sep;28(9):904-6. doi: 10.1038/nbt0910-904. No abstract available.


A small-molecule inducer of the antioxidant response element.

Hur W, Sun Z, Jiang T, Mason DE, Peters EC, Zhang DD, Luesch H, Schultz PG, Gray NS.

Chem Biol. 2010 May 28;17(5):537-47. doi: 10.1016/j.chembiol.2010.03.013.


Apogossypol derivatives as pan-active inhibitors of antiapoptotic B-cell lymphoma/leukemia-2 (Bcl-2) family proteins.

Wei J, Kitada S, Rega MF, Stebbins JL, Zhai D, Cellitti J, Yuan H, Emdadi A, Dahl R, Zhang Z, Yang L, Reed JC, Pellecchia M.

J Med Chem. 2009 Jul 23;52(14):4511-23. doi: 10.1021/jm900472s.


Completing the family portrait of the anti-apoptotic Bcl-2 proteins: crystal structure of human Bfl-1 in complex with Bim.

Herman MD, Nyman T, Welin M, Lehtiö L, Flodin S, Trésaugues L, Kotenyova T, Flores A, Nordlund P.

FEBS Lett. 2008 Oct 29;582(25-26):3590-4. doi: 10.1016/j.febslet.2008.09.028.


Bcl-2 inhibitors: small molecules with a big impact on cancer therapy.

Vogler M, Dinsdale D, Dyer MJ, Cohen GM.

Cell Death Differ. 2009 Mar;16(3):360-7. doi: 10.1038/cdd.2008.137. Review.


Non-peptidic small molecule inhibitors against Bcl-2 for cancer therapy.

Azmi AS, Mohammad RM.

J Cell Physiol. 2009 Jan;218(1):13-21. doi: 10.1002/jcp.21567. Review.


Gambogic acid is an antagonist of antiapoptotic Bcl-2 family proteins.

Zhai D, Jin C, Shiau CW, Kitada S, Satterthwait AC, Reed JC.

Mol Cancer Ther. 2008 Jun;7(6):1639-46. doi: 10.1158/1535-7163.MCT-07-2373.


Structural plasticity underpins promiscuous binding of the prosurvival protein A1.

Smits C, Czabotar PE, Hinds MG, Day CL.

Structure. 2008 May;16(5):818-29. doi: 10.1016/j.str.2008.02.009.


ABT-263: a potent and orally bioavailable Bcl-2 family inhibitor.

Tse C, Shoemaker AR, Adickes J, Anderson MG, Chen J, Jin S, Johnson EF, Marsh KC, Mitten MJ, Nimmer P, Roberts L, Tahir SK, Xiao Y, Yang X, Zhang H, Fesik S, Rosenberg SH, Elmore SW.

Cancer Res. 2008 May 1;68(9):3421-8. doi: 10.1158/0008-5472.CAN-07-5836.


Chelerythrine induces apoptosis through a Bax/Bak-independent mitochondrial mechanism.

Wan KF, Chan SL, Sukumaran SK, Lee MC, Yu VC.

J Biol Chem. 2008 Mar 28;283(13):8423-33. doi: 10.1074/jbc.M707687200.


Bcl-2 antagonist apogossypol (NSC736630) displays single-agent activity in Bcl-2-transgenic mice and has superior efficacy with less toxicity compared with gossypol (NSC19048).

Kitada S, Kress CL, Krajewska M, Jia L, Pellecchia M, Reed JC.

Blood. 2008 Mar 15;111(6):3211-9. doi: 10.1182/blood-2007-09-113647.


Proapoptotic BH3-only BCL-2 family protein BIM connects death signaling from epidermal growth factor receptor inhibition to the mitochondrion.

Deng J, Shimamura T, Perera S, Carlson NE, Cai D, Shapiro GI, Wong KK, Letai A.

Cancer Res. 2007 Dec 15;67(24):11867-75.


Gefitinib-induced killing of NSCLC cell lines expressing mutant EGFR requires BIM and can be enhanced by BH3 mimetics.

Cragg MS, Kuroda J, Puthalakath H, Huang DC, Strasser A.

PLoS Med. 2007 Oct;4(10):1681-89; discussion 1690.


BIM mediates EGFR tyrosine kinase inhibitor-induced apoptosis in lung cancers with oncogenic EGFR mutations.

Costa DB, Halmos B, Kumar A, Schumer ST, Huberman MS, Boggon TJ, Tenen DG, Kobayashi S.

PLoS Med. 2007 Oct;4(10):1669-79; discussion 1680.


Induction of BIM is essential for apoptosis triggered by EGFR kinase inhibitors in mutant EGFR-dependent lung adenocarcinomas.

Gong Y, Somwar R, Politi K, Balak M, Chmielecki J, Jiang X, Pao W.

PLoS Med. 2007 Oct 9;4(10):e294.


Downregulation of Bfl-1 protein expression sensitizes malignant B cells to apoptosis.

Brien G, Trescol-Biemont MC, Bonnefoy-Bérard N.

Oncogene. 2007 Aug 23;26(39):5828-32.


Preclinical studies of the pan-Bcl inhibitor obatoclax (GX015-070) in multiple myeloma.

Trudel S, Li ZH, Rauw J, Tiedemann RE, Wen XY, Stewart AK.

Blood. 2007 Jun 15;109(12):5430-8.


The Bcl-2 apoptotic switch in cancer development and therapy.

Adams JM, Cory S.

Oncogene. 2007 Feb 26;26(9):1324-37. Review.

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