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Chronic lymphocytic leukemia requires BCL2 to sequester prodeath BIM, explaining sensitivity to BCL2 antagonist ABT-737.

Del Gaizo Moore V, Brown JR, Certo M, Love TM, Novina CD, Letai A.

J Clin Invest. 2007 Jan;117(1):112-21.


BCL-2 dependence and ABT-737 sensitivity in acute lymphoblastic leukemia.

Del Gaizo Moore V, Schlis KD, Sallan SE, Armstrong SA, Letai A.

Blood. 2008 Feb 15;111(4):2300-9. Epub 2007 Dec 4.


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.

Renault TT, Elkholi R, Bharti A, Chipuk JE.

J Biol Chem. 2014 Sep 19;289(38):26481-91. doi: 10.1074/jbc.M114.569632. Epub 2014 Aug 5.


Multiple BH3 mimetics antagonize antiapoptotic MCL1 protein by inducing the endoplasmic reticulum stress response and up-regulating BH3-only protein NOXA.

Albershardt TC, Salerni BL, Soderquist RS, Bates DJ, Pletnev AA, Kisselev AF, Eastman A.

J Biol Chem. 2011 Jul 15;286(28):24882-95. doi: 10.1074/jbc.M111.255828. Epub 2011 May 31.


The BH3 mimetic compound, ABT-737, synergizes with a range of cytotoxic chemotherapy agents in chronic lymphocytic leukemia.

Mason KD, Khaw SL, Rayeroux KC, Chew E, Lee EF, Fairlie WD, Grigg AP, Seymour JF, Szer J, Huang DC, Roberts AW.

Leukemia. 2009 Nov;23(11):2034-41. doi: 10.1038/leu.2009.151. Epub 2009 Jul 30.


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.


MEK inhibition enhances ABT-737-induced leukemia cell apoptosis via prevention of ERK-activated MCL-1 induction and modulation of MCL-1/BIM complex.

Konopleva M, Milella M, Ruvolo P, Watts JC, Ricciardi MR, Korchin B, McQueen T, Bornmann W, Tsao T, Bergamo P, Mak DH, Chen W, McCubrey J, Tafuri A, Andreeff M.

Leukemia. 2012 Apr;26(4):778-87. doi: 10.1038/leu.2011.287. Epub 2011 Nov 8.


Bcl-2 phosphorylation confers resistance on chronic lymphocytic leukaemia cells to the BH3 mimetics ABT-737, ABT-263 and ABT-199 by impeding direct binding.

Song T, Chai G, Liu Y, Yu X, Wang Z, Zhang Z.

Br J Pharmacol. 2016 Feb;173(3):471-83. doi: 10.1111/bph.13370. Epub 2016 Jan 16.


Acquired resistance to ABT-737 in lymphoma cells that up-regulate MCL-1 and BFL-1.

Yecies D, Carlson NE, Deng J, Letai A.

Blood. 2010 Apr 22;115(16):3304-13. doi: 10.1182/blood-2009-07-233304. Epub 2010 Mar 2.


BH3 mimetic ABT-737 potentiates TRAIL-mediated apoptotic signaling by unsequestering Bim and Bak in human pancreatic cancer cells.

Huang S, Sinicrope FA.

Cancer Res. 2008 Apr 15;68(8):2944-51. doi: 10.1158/0008-5472.CAN-07-2508.


Bcl-2, Bcl-x(L), and Bcl-w are not equivalent targets of ABT-737 and navitoclax (ABT-263) in lymphoid and leukemic cells.

Mérino D, Khaw SL, Glaser SP, Anderson DJ, Belmont LD, Wong C, Yue P, Robati M, Phipson B, Fairlie WD, Lee EF, Campbell KJ, Vandenberg CJ, Cory S, Roberts AW, Ludlam MJ, Huang DC, Bouillet P.

Blood. 2012 Jun 14;119(24):5807-16. doi: 10.1182/blood-2011-12-400929. Epub 2012 Apr 26.


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. Epub 2008 Jun 30.


Tipping the Noxa/Mcl-1 balance overcomes ABT-737 resistance in chronic lymphocytic leukemia.

Tromp JM, Geest CR, Breij EC, Elias JA, van Laar J, Luijks DM, Kater AP, Beaumont T, van Oers MH, Eldering E.

Clin Cancer Res. 2012 Jan 15;18(2):487-98. doi: 10.1158/1078-0432.CCR-11-1440. Epub 2011 Nov 29.


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 Nov 3;6(34):35667-83. doi: 10.18632/oncotarget.5523.


Cap-translation inhibitor, 4EGI-1, restores sensitivity to ABT-737 apoptosis through cap-dependent and -independent mechanisms in chronic lymphocytic leukemia.

Willimott S, Beck D, Ahearne MJ, Adams VC, Wagner SD.

Clin Cancer Res. 2013 Jun 15;19(12):3212-23. doi: 10.1158/1078-0432.CCR-12-2185. Epub 2013 Apr 30.


The mTORC1/2 Inhibitor AZD8055 Strengthens the Efficiency of the MEK Inhibitor Trametinib to Reduce the Mcl-1/[Bim and Puma] ratio and to Sensitize Ovarian Carcinoma Cells to ABT-737.

Pétigny-Lechartier C, Duboc C, Jebahi A, Louis MH, Abeilard E, Denoyelle C, Gauduchon P, Poulain L, Villedieu M.

Mol Cancer Ther. 2017 Jan;16(1):102-115. doi: 10.1158/1535-7163.MCT-16-0342. Epub 2016 Dec 15.


Decreased sensitivity of 17p-deleted chronic lymphocytic leukemia cells to a small molecule BCL-2 antagonist ABT-737.

Kojima K, Duvvuri S, Ruvolo V, Samaniego F, Younes A, Andreeff M.

Cancer. 2012 Feb 15;118(4):1023-31. doi: 10.1002/cncr.26360. Epub 2011 Jul 14.

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