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BH3 profiling discriminates on-target small molecule BH3 mimetics from putative mimetics.

Villalobos-Ortiz M, Ryan J, Mashaka TN, Opferman JT, Letai A.

Cell Death Differ. 2019 Jul 22. doi: 10.1038/s41418-019-0391-9. [Epub ahead of print]


Discovery of Potent Myeloid Cell Leukemia-1 (Mcl-1) Inhibitors That Demonstrate in Vivo Activity in Mouse Xenograft Models of Human Cancer.

Lee T, Christov PP, Shaw S, Tarr JC, Zhao B, Veerasamy N, Jeon KO, Mills JJ, Bian Z, Sensintaffar JL, Arnold AL, Fogarty SA, Perry E, Ramsey HE, Cook RS, Hollingshead M, Davis Millin M, Lee KM, Koss B, Budhraja A, Opferman JT, Kim K, Arteaga CL, Moore WJ, Olejniczak ET, Savona MR, Fesik SW.

J Med Chem. 2019 Apr 25;62(8):3971-3988. doi: 10.1021/acs.jmedchem.8b01991. Epub 2019 Apr 16.


Identification of substituted 5-membered heterocyclic compounds as potential anti-leukemic agents.

Ling T, Maier J, Das S, Budhraja A, Bassett R, Potts MB, Shelat A, Rankovic Z, Opferman JT, Rivas F.

Eur J Med Chem. 2019 Feb 15;164:391-398. doi: 10.1016/j.ejmech.2018.12.059. Epub 2018 Dec 24.


Rationally derived drug combinations with the novel Mcl-1 inhibitor EU-5346 in breast cancer.

Vallet S, Fan F, Malvestiti S, Pecherstorfer M, Sattler M, Schneeweiss A, Schulze-Bergkamen H, Opferman JT, Cardone MH, Jäger D, Podar K.

Breast Cancer Res Treat. 2019 Feb;173(3):585-596. doi: 10.1007/s10549-018-5022-5. Epub 2018 Oct 29.


Mcl-1 and Bcl-xL are essential for survival of the developing nervous system.

Fogarty LC, Flemmer RT, Geizer BA, Licursi M, Karunanithy A, Opferman JT, Hirasawa K, Vanderluit JL.

Cell Death Differ. 2019 Aug;26(8):1501-1515. doi: 10.1038/s41418-018-0225-1. Epub 2018 Oct 25.


LC3-Associated Phagocytosis in Myeloid Cells Promotes Tumor Immune Tolerance.

Cunha LD, Yang M, Carter R, Guy C, Harris L, Crawford JC, Quarato G, Boada-Romero E, Kalkavan H, Johnson MDL, Natarajan S, Turnis ME, Finkelstein D, Opferman JT, Gawad C, Green DR.

Cell. 2018 Oct 4;175(2):429-441.e16. doi: 10.1016/j.cell.2018.08.061. Epub 2018 Sep 20.


Dynamic Regulation of Long-Chain Fatty Acid Oxidation by a Noncanonical Interaction between the MCL-1 BH3 Helix and VLCAD.

Escudero S, Zaganjor E, Lee S, Mill CP, Morgan AM, Crawford EB, Chen J, Wales TE, Mourtada R, Luccarelli J, Bird GH, Steidl U, Engen JR, Haigis MC, Opferman JT, Walensky LD.

Mol Cell. 2018 Mar 1;69(5):729-743.e7. doi: 10.1016/j.molcel.2018.02.005.


Anti-apoptotic BCL-2 family members in development.

Opferman JT, Kothari A.

Cell Death Differ. 2018 Jan;25(1):37-45. doi: 10.1038/cdd.2017.170. Epub 2017 Nov 3. Review.


Anti-apoptotic BCL-2 family members in development.

Opferman JT, Kothari A.

Cell Death Differ. 2018 Jan;25(1):37-45. doi: 10.1038/cdd.2017.170. Epub 2017 Nov 3. Review.


Modulation of Navitoclax Sensitivity by Dihydroartemisinin-Mediated MCL-1 Repression in BCR-ABL+ B-Lineage Acute Lymphoblastic Leukemia.

Budhraja A, Turnis ME, Churchman ML, Kothari A, Yang X, Xu H, Kaminska E, Panetta JC, Finkelstein D, Mullighan CG, Opferman JT.

Clin Cancer Res. 2017 Dec 15;23(24):7558-7568. doi: 10.1158/1078-0432.CCR-17-1231. Epub 2017 Oct 3.


Extra-mitochondrial prosurvival BCL-2 proteins regulate gene transcription by inhibiting the SUFU tumour suppressor.

Wu X, Zhang LS, Toombs J, Kuo YC, Piazza JT, Tuladhar R, Barrett Q, Fan CW, Zhang X, Walensky LD, Kool M, Cheng SY, Brekken R, Opferman JT, Green DR, Moldoveanu T, Lum L.

Nat Cell Biol. 2017 Oct;19(10):1226-1236. doi: 10.1038/ncb3616. Epub 2017 Sep 25.


Small mitochondrial Arf (smArf) protein corrects p53-independent developmental defects of Arf tumor suppressor-deficient mice.

van Oosterwijk JG, Li C, Yang X, Opferman JT, Sherr CJ.

Proc Natl Acad Sci U S A. 2017 Jul 11;114(28):7420-7425. doi: 10.1073/pnas.1707292114. Epub 2017 Jun 26.


Male sterility in Mcl-1-flox mice is not due to enhanced Mcl1 protein stability.

Ah-Cann C, Tailler M, Kueh AJ, Herold MJ, Opferman JT, Asselin-Labat ML, Bouillet P.

Cell Death Dis. 2016 Dec 1;7(12):e2490. doi: 10.1038/cddis.2016.391. No abstract available.


Prolyl Hydroxylase 3 Attenuates MCL-1-Mediated ATP Production to Suppress the Metastatic Potential of Colorectal Cancer Cells.

Radhakrishnan P, Ruh N, Harnoss JM, Kiss J, Mollenhauer M, Scherr AL, Platzer LK, Schmidt T, Podar K, Opferman JT, Weitz J, Schulze-Bergkamen H, Koehler BC, Ulrich A, Schneider M.

Cancer Res. 2016 Apr 15;76(8):2219-30. doi: 10.1158/0008-5472.CAN-15-1474. Epub 2016 Feb 26.


Mcl-1 confers protection of Her2-positive breast cancer cells to hypoxia: therapeutic implications.

Bashari MH, Fan F, Vallet S, Sattler M, Arn M, Luckner-Minden C, Schulze-Bergkamen H, Zörnig I, Marme F, Schneeweiss A, Cardone MH, Opferman JT, Jäger D, Podar K.

Breast Cancer Res. 2016 Feb 26;18(1):26. doi: 10.1186/s13058-016-0686-4.


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 Mar 8;7(10):11500-11. doi: 10.18632/oncotarget.7204.


Apoptosome activation, an important molecular instigator in 6-mercaptopurine induced Leydig cell death.

Morgan JA, Lynch J, Panetta JC, Wang Y, Frase S, Bao J, Zheng J, Opferman JT, Janke L, Green DM, Chemaitilly W, Schuetz JD.

Sci Rep. 2015 Nov 18;5:16488. doi: 10.1038/srep16488.


Attacking cancer's Achilles heel: antagonism of anti-apoptotic BCL-2 family members.

Opferman JT.

FEBS J. 2016 Jul;283(14):2661-75. doi: 10.1111/febs.13472. Epub 2015 Sep 15. Review.


Functional Divergence in the Role of N-Linked Glycosylation in Smoothened Signaling.

Marada S, Navarro G, Truong A, Stewart DP, Arensdorf AM, Nachtergaele S, Angelats E, Opferman JT, Rohatgi R, McCormick PJ, Ogden SK.

PLoS Genet. 2015 Aug 20;11(8):e1005473. doi: 10.1371/journal.pgen.1005473. eCollection 2015 Aug.


Mcl-1 is a key regulator of the ovarian reserve.

Omari S, Waters M, Naranian T, Kim K, Perumalsamy AL, Chi M, Greenblatt E, Moley KH, Opferman JT, Jurisicova A.

Cell Death Dis. 2015 May 7;6:e1755. doi: 10.1038/cddis.2015.95.


Antagonism between MCL-1 and PUMA governs stem/progenitor cell survival during hematopoietic recovery from stress.

Delbridge AR, Opferman JT, Grabow S, Strasser A.

Blood. 2015 May 21;125(21):3273-80. doi: 10.1182/blood-2015-01-621250. Epub 2015 Apr 6.


Myeloid-derived suppressor activity is mediated by monocytic lineages maintained by continuous inhibition of extrinsic and intrinsic death pathways.

Haverkamp JM, Smith AM, Weinlich R, Dillon CP, Qualls JE, Neale G, Koss B, Kim Y, Bronte V, Herold MJ, Green DR, Opferman JT, Murray PJ.

Immunity. 2014 Dec 18;41(6):947-59. doi: 10.1016/j.immuni.2014.10.020. Epub 2014 Dec 11.


Mito-protective autophagy is impaired in erythroid cells of aged mtDNA-mutator mice.

Li-Harms X, Milasta S, Lynch J, Wright C, Joshi A, Iyengar R, Neale G, Wang X, Wang YD, Prolla TA, Thompson JE, Opferman JT, Green DR, Schuetz J, Kundu M.

Blood. 2015 Jan 1;125(1):162-74. doi: 10.1182/blood-2014-07-586396. Epub 2014 Nov 19.


Targeting Mcl-1 for multiple myeloma (MM) therapy: drug-induced generation of Mcl-1 fragment Mcl-1(128-350) triggers MM cell death via c-Jun upregulation.

Fan F, Tonon G, Bashari MH, Vallet S, Antonini E, Goldschmidt H, Schulze-Bergkamen H, Opferman JT, Sattler M, Anderson KC, Jäger D, Podar K.

Cancer Lett. 2014 Feb 28;343(2):286-94. doi: 10.1016/j.canlet.2013.09.042. Epub 2013 Oct 8.


Requirement for antiapoptotic MCL-1 in the survival of BCR-ABL B-lineage acute lymphoblastic leukemia.

Koss B, Morrison J, Perciavalle RM, Singh H, Rehg JE, Williams RT, Opferman JT.

Blood. 2013 Aug 29;122(9):1587-98. doi: 10.1182/blood-2012-06-440230. Epub 2013 Jul 23.


Mcl1 regulates the terminal mitosis of neural precursor cells in the mammalian brain through p27Kip1.

Hasan SM, Sheen AD, Power AM, Langevin LM, Xiong J, Furlong M, Day K, Schuurmans C, Opferman JT, Vanderluit JL.

Development. 2013 Aug;140(15):3118-27. doi: 10.1242/dev.090910. Epub 2013 Jul 3.


Deletion of MCL-1 causes lethal cardiac failure and mitochondrial dysfunction.

Wang X, Bathina M, Lynch J, Koss B, Calabrese C, Frase S, Schuetz JD, Rehg JE, Opferman JT.

Genes Dev. 2013 Jun 15;27(12):1351-64. doi: 10.1101/gad.215855.113.


Mcl-1 antagonizes Bax/Bak to promote effector CD4(+) and CD8(+) T-cell responses.

Tripathi P, Koss B, Opferman JT, Hildeman DA.

Cell Death Differ. 2013 Aug;20(8):998-1007. doi: 10.1038/cdd.2013.25. Epub 2013 Apr 5.


Delving deeper: MCL-1's contributions to normal and cancer biology.

Perciavalle RM, Opferman JT.

Trends Cell Biol. 2013 Jan;23(1):22-9. doi: 10.1016/j.tcb.2012.08.011. Epub 2012 Sep 28. Review.


A competitive stapled peptide screen identifies a selective small molecule that overcomes MCL-1-dependent leukemia cell survival.

Cohen NA, Stewart ML, Gavathiotis E, Tepper JL, Bruekner SR, Koss B, Opferman JT, Walensky LD.

Chem Biol. 2012 Sep 21;19(9):1175-86. doi: 10.1016/j.chembiol.2012.07.018.


Anti-apoptotic MCL-1 localizes to the mitochondrial matrix and couples mitochondrial fusion to respiration.

Perciavalle RM, Stewart DP, Koss B, Lynch J, Milasta S, Bathina M, Temirov J, Cleland MM, Pelletier S, Schuetz JD, Youle RJ, Green DR, Opferman JT.

Nat Cell Biol. 2012 Apr 29;14(6):575-83. doi: 10.1038/ncb2488.


Mcl-1 regulates the survival of adult neural precursor cells.

Malone CD, Hasan SM, Roome RB, Xiong J, Furlong M, Opferman JT, Vanderluit JL.

Mol Cell Neurosci. 2012 Apr;49(4):439-47. doi: 10.1016/j.mcn.2012.02.003. Epub 2012 Feb 13.


Genetically defining the mechanism of Puma- and Bim-induced apoptosis.

Garrison SP, Phillips DC, Jeffers JR, Chipuk JE, Parsons MJ, Rehg JE, Opferman JT, Green DR, Zambetti GP.

Cell Death Differ. 2012 Apr;19(4):642-9. doi: 10.1038/cdd.2011.136. Epub 2011 Oct 21.


MCL-1 is a stress sensor that regulates autophagy in a developmentally regulated manner.

Germain M, Nguyen AP, Le Grand JN, Arbour N, Vanderluit JL, Park DS, Opferman JT, Slack RS.

EMBO J. 2011 Jan 19;30(2):395-407. doi: 10.1038/emboj.2010.327. Epub 2010 Dec 7.


Contracting the 'mus cells'--does down-sizing suit us for diving into the memory pool?

Kurtulus S, Tripathi P, Opferman JT, Hildeman DA.

Immunol Rev. 2010 Jul;236:54-67. doi: 10.1111/j.1600-065X.2010.00920.x. Review.


Mcl1 haploinsufficiency protects mice from Myc-induced acute myeloid leukemia.

Xiang Z, Luo H, Payton JE, Cain J, Ley TJ, Opferman JT, Tomasson MH.

J Clin Invest. 2010 Jun;120(6):2109-18. doi: 10.1172/JCI39964. Epub 2010 May 17.


Ubiquitin-independent degradation of antiapoptotic MCL-1.

Stewart DP, Koss B, Bathina M, Perciavalle RM, Bisanz K, Opferman JT.

Mol Cell Biol. 2010 Jun;30(12):3099-110. doi: 10.1128/MCB.01266-09. Epub 2010 Apr 12.


DUB-le Trouble for Cell Survival.

Opferman JT, Green DR.

Cancer Cell. 2010 Feb 17;17(2):117-9. doi: 10.1016/j.ccr.2010.01.011.


Hepatocyte-specific deletion of the antiapoptotic protein myeloid cell leukemia-1 triggers proliferation and hepatocarcinogenesis in mice.

Weber A, Boger R, Vick B, Urbanik T, Haybaeck J, Zoller S, Teufel A, Krammer PH, Opferman JT, Galle PR, Schuchmann M, Heikenwalder M, Schulze-Bergkamen H.

Hepatology. 2010 Apr;51(4):1226-36. doi: 10.1002/hep.23479.


MCL-1-dependent leukemia cells are more sensitive to chemotherapy than BCL-2-dependent counterparts.

Brunelle JK, Ryan J, Yecies D, Opferman JT, Letai A.

J Cell Biol. 2009 Nov 2;187(3):429-42. doi: 10.1083/jcb.200904049. Epub 2009 Oct 26.


Knockout of myeloid cell leukemia-1 induces liver damage and increases apoptosis susceptibility of murine hepatocytes.

Vick B, Weber A, Urbanik T, Maass T, Teufel A, Krammer PH, Opferman JT, Schuchmann M, Galle PR, Schulze-Bergkamen H.

Hepatology. 2009 Feb;49(2):627-36. doi: 10.1002/hep.22664.


Selective roles for antiapoptotic MCL-1 during granulocyte development and macrophage effector function.

Steimer DA, Boyd K, Takeuchi O, Fisher JK, Zambetti GP, Opferman JT.

Blood. 2009 Mar 19;113(12):2805-15. doi: 10.1182/blood-2008-05-159145. Epub 2008 Dec 8.


Mcl-1 is a key regulator of apoptosis during CNS development and after DNA damage.

Arbour N, Vanderluit JL, Le Grand JN, Jahani-Asl A, Ruzhynsky VA, Cheung EC, Kelly MA, MacKenzie AE, Park DS, Opferman JT, Slack RS.

J Neurosci. 2008 Jun 11;28(24):6068-78. doi: 10.1523/JNEUROSCI.4940-07.2008.


Hax1-mediated processing of HtrA2 by Parl allows survival of lymphocytes and neurons.

Chao JR, Parganas E, Boyd K, Hong CY, Opferman JT, Ihle JN.

Nature. 2008 Mar 6;452(7183):98-102. doi: 10.1038/nature06604. Epub 2008 Feb 20. Erratum in: Nature. 2008 Apr 17;452(7189):900.


NIX is required for programmed mitochondrial clearance during reticulocyte maturation.

Schweers RL, Zhang J, Randall MS, Loyd MR, Li W, Dorsey FC, Kundu M, Opferman JT, Cleveland JL, Miller JL, Ney PA.

Proc Natl Acad Sci U S A. 2007 Dec 4;104(49):19500-5. Epub 2007 Nov 29.


Multiple signaling pathways promote B lymphocyte stimulator dependent B-cell growth and survival.

Woodland RT, Fox CJ, Schmidt MR, Hammerman PS, Opferman JT, Korsmeyer SJ, Hilbert DM, Thompson CB.

Blood. 2008 Jan 15;111(2):750-60. Epub 2007 Oct 17.


Life and death during hematopoietic differentiation.

Opferman JT.

Curr Opin Immunol. 2007 Oct;19(5):497-502. Epub 2007 Jul 26. Review.


A pivotal role for Mcl-1 in Bortezomib-induced apoptosis.

Podar K, Gouill SL, Zhang J, Opferman JT, Zorn E, Tai YT, Hideshima T, Amiot M, Chauhan D, Harousseau JL, Anderson KC.

Oncogene. 2008 Jan 31;27(6):721-31. Epub 2007 Jul 23.


Apoptosis in the development of the immune system.

Opferman JT.

Cell Death Differ. 2008 Feb;15(2):234-42. Epub 2007 Jun 15. Review.


Gene expression-based chemical genomics identifies rapamycin as a modulator of MCL1 and glucocorticoid resistance.

Wei G, Twomey D, Lamb J, Schlis K, Agarwal J, Stam RW, Opferman JT, Sallan SE, den Boer ML, Pieters R, Golub TR, Armstrong SA.

Cancer Cell. 2006 Oct;10(4):331-42. Epub 2006 Sep 28.

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