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Discovery of a novel proteasome inhibitor selective for cancer cells over non-transformed cells.

Kazi A, Lawrence H, Guida WC, McLaughlin ML, Springett GM, Berndt N, Yip RM, Sebti SM.

Cell Cycle. 2009 Jun 15;8(12):1940-51.


Blockade of protein geranylgeranylation inhibits Cdk2-dependent p27Kip1 phosphorylation on Thr187 and accumulates p27Kip1 in the nucleus: implications for breast cancer therapy.

Kazi A, Carie A, Blaskovich MA, Bucher C, Thai V, Moulder S, Peng H, Carrico D, Pusateri E, Pledger WJ, Berndt N, Hamilton A, Sebti SM.

Mol Cell Biol. 2009 Apr;29(8):2254-63. doi: 10.1128/MCB.01029-08.


Membrane binding by tBid initiates an ordered series of events culminating in membrane permeabilization by Bax.

Lovell JF, Billen LP, Bindner S, Shamas-Din A, Fradin C, Leber B, Andrews DW.

Cell. 2008 Dec 12;135(6):1074-84. doi: 10.1016/j.cell.2008.11.010.


BH3 mimetic ABT-737 and a proteasome inhibitor synergistically kill melanomas through Noxa-dependent apoptosis.

Miller LA, Goldstein NB, Johannes WU, Walton CH, Fujita M, Norris DA, Shellman YG.

J Invest Dermatol. 2009 Apr;129(4):964-71. doi: 10.1038/jid.2008.327.


BAX activation is initiated at a novel interaction site.

Gavathiotis E, Suzuki M, Davis ML, Pitter K, Bird GH, Katz SG, Tu HC, Kim H, Cheng EH, Tjandra N, Walensky LD.

Nature. 2008 Oct 23;455(7216):1076-81. doi: 10.1038/nature07396.


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.


The BH3-only mimetic ABT-737 synergizes the antineoplastic activity of proteasome inhibitors in lymphoid malignancies.

Paoluzzi L, Gonen M, Bhagat G, Furman RR, Gardner JR, Scotto L, Gueorguiev VD, Heaney ML, Manova K, O'Connor OA.

Blood. 2008 Oct 1;112(7):2906-16. doi: 10.1182/blood-2007-12-130781.


How do BCL-2 proteins induce mitochondrial outer membrane permeabilization?

Chipuk JE, Green DR.

Trends Cell Biol. 2008 Apr;18(4):157-64. doi: 10.1016/j.tcb.2008.01.007. Review.


Targeting Bcl-2 family members with the BH3 mimetic AT-101 markedly enhances the therapeutic effects of chemotherapeutic agents in in vitro and in vivo models of B-cell lymphoma.

Paoluzzi L, Gonen M, Gardner JR, Mastrella J, Yang D, Holmlund J, Sorensen M, Leopold L, Manova K, Marcucci G, Heaney ML, O'Connor OA.

Blood. 2008 Jun 1;111(11):5350-8. doi: 10.1182/blood-2007-12-129833.


Small molecule obatoclax (GX15-070) antagonizes MCL-1 and overcomes MCL-1-mediated resistance to apoptosis.

Nguyen M, Marcellus RC, Roulston A, Watson M, Serfass L, Murthy Madiraju SR, Goulet D, Viallet J, BĂ©lec L, Billot X, Acoca S, Purisima E, Wiegmans A, Cluse L, Johnstone RW, Beauparlant P, Shore GC.

Proc Natl Acad Sci U S A. 2007 Dec 4;104(49):19512-7.


Bim and the pro-survival Bcl-2 proteins: opposites attract, ERK repels.

Ewings KE, Wiggins CM, Cook SJ.

Cell Cycle. 2007 Sep 15;6(18):2236-40. Review.


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.

Mohammad RM, Goustin AS, Aboukameel A, Chen B, Banerjee S, Wang G, Nikolovska-Coleska Z, Wang S, Al-Katib A.

Clin Cancer Res. 2007 Apr 1;13(7):2226-35.


Structural insights into the degradation of Mcl-1 induced by BH3 domains.

Czabotar PE, Lee EF, van Delft MF, Day CL, Smith BJ, Huang DC, Fairlie WD, Hinds MG, Colman PM.

Proc Natl Acad Sci U S A. 2007 Apr 10;104(15):6217-22.


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

Adams JM, Cory S.

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


Cell biology. Cellular demolition and the rules of engagement.

Youle RJ.

Science. 2007 Feb 9;315(5813):776-7. No abstract available.


Studies leading to potent, dual inhibitors of Bcl-2 and Bcl-xL.

Bruncko M, Oost TK, Belli BA, Ding H, Joseph MK, Kunzer A, Martineau D, McClellan WJ, Mitten M, Ng SC, Nimmer PM, Oltersdorf T, Park CM, Petros AM, Shoemaker AR, Song X, Wang X, Wendt MD, Zhang H, Fesik SW, Rosenberg SH, Elmore SW.

J Med Chem. 2007 Feb 22;50(4):641-62.


Hierarchical regulation of mitochondrion-dependent apoptosis by BCL-2 subfamilies.

Kim H, Rafiuddin-Shah M, Tu HC, Jeffers JR, Zambetti GP, Hsieh JJ, Cheng EH.

Nat Cell Biol. 2006 Dec;8(12):1348-58.


The BH3 mimetic ABT-737 targets selective Bcl-2 proteins and efficiently induces apoptosis via Bak/Bax if Mcl-1 is neutralized.

van Delft MF, Wei AH, Mason KD, Vandenberg CJ, Chen L, Czabotar PE, Willis SN, Scott CL, Day CL, Cory S, Adams JM, Roberts AW, Huang DC.

Cancer Cell. 2006 Nov;10(5):389-99.


Mechanisms of apoptosis sensitivity and resistance to the BH3 mimetic ABT-737 in acute myeloid leukemia.

Konopleva M, Contractor R, Tsao T, Samudio I, Ruvolo PP, Kitada S, Deng X, Zhai D, Shi YX, Sneed T, Verhaegen M, Soengas M, Ruvolo VR, McQueen T, Schober WD, Watt JC, Jiffar T, Ling X, Marini FC, Harris D, Dietrich M, Estrov Z, McCubrey J, May WS, Reed JC, Andreeff M.

Cancer Cell. 2006 Nov;10(5):375-88.

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