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Targeting BAX to drug death directly.

Walensky LD.

Nat Chem Biol. 2019 Jul;15(7):657-665. doi: 10.1038/s41589-019-0306-6. Epub 2019 Jun 17. Review.


Cheating Death: New Molecules Block BAX.

Walensky LD.

Trends Mol Med. 2019 Apr;25(4):259-261. doi: 10.1016/j.molmed.2019.02.008. Epub 2019 Mar 6.


MDM2 and MDM4 Are Therapeutic Vulnerabilities in Malignant Rhabdoid Tumors.

Howard TP, Arnoff TE, Song MR, Giacomelli AO, Wang X, Hong AL, Dharia NV, Wang S, Vazquez F, Pham MT, Morgan AM, Wachter F, Bird GH, Kugener G, Oberlick EM, Rees MG, Tiv HL, Hwang JH, Walsh KH, Cook A, Krill-Burger JM, Tsherniak A, Gokhale PC, Park PJ, Stegmaier K, Walensky LD, Hahn WC, Roberts CWM.

Cancer Res. 2019 May 1;79(9):2404-2414. doi: 10.1158/0008-5472.CAN-18-3066. Epub 2019 Feb 12.


Precision Targeting of BFL-1/A1 and an ATM Co-dependency in Human Cancer.

Guerra RM, Bird GH, Harvey EP, Dharia NV, Korshavn KJ, Prew MS, Stegmaier K, Walensky LD.

Cell Rep. 2018 Sep 25;24(13):3393-3403.e5. doi: 10.1016/j.celrep.2018.08.089.


Genome-scale CRISPR-Cas9 screen identifies druggable dependencies in TP53 wild-type Ewing sarcoma.

Stolte B, Iniguez AB, Dharia NV, Robichaud AL, Conway AS, Morgan AM, Alexe G, Schauer NJ, Liu X, Bird GH, Tsherniak A, Vazquez F, Buhrlage SJ, Walensky LD, Stegmaier K.

J Exp Med. 2018 Aug 6;215(8):2137-2155. doi: 10.1084/jem.20171066. Epub 2018 Jul 25.


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.


Iterative optimization yields Mcl-1-targeting stapled peptides with selective cytotoxicity to Mcl-1-dependent cancer cells.

Rezaei Araghi R, Bird GH, Ryan JA, Jenson JM, Godes M, Pritz JR, Grant RA, Letai A, Walensky LD, Keating AE.

Proc Natl Acad Sci U S A. 2018 Jan 30;115(5):E886-E895. doi: 10.1073/pnas.1712952115. Epub 2018 Jan 16.


Crystal Structures of Anti-apoptotic BFL-1 and Its Complex with a Covalent Stapled Peptide Inhibitor.

Harvey EP, Seo HS, Guerra RM, Bird GH, Dhe-Paganon S, Walensky LD.

Structure. 2018 Jan 2;26(1):153-160.e4. doi: 10.1016/j.str.2017.11.016. Epub 2017 Dec 21.


Paclitaxel Reduces Axonal Bclw to Initiate IP3R1-Dependent Axon Degeneration.

Pease-Raissi SE, Pazyra-Murphy MF, Li Y, Wachter F, Fukuda Y, Fenstermacher SJ, Barclay LA, Bird GH, Walensky LD, Segal RA.

Neuron. 2017 Oct 11;96(2):373-386.e6. doi: 10.1016/j.neuron.2017.09.034.


Direct Activation of BAX by BTSA1 Overcomes Apoptosis Resistance in Acute Myeloid Leukemia.

Reyna DE, Garner TP, Lopez A, Kopp F, Choudhary GS, Sridharan A, Narayanagari SR, Mitchell K, Dong B, Bartholdy BA, Walensky LD, Verma A, Steidl U, Gavathiotis E.

Cancer Cell. 2017 Oct 9;32(4):490-505.e10. doi: 10.1016/j.ccell.2017.09.001.


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.


Allosteric sensitization of proapoptotic BAX.

Pritz JR, Wachter F, Lee S, Luccarelli J, Wales TE, Cohen DT, Coote P, Heffron GJ, Engen JR, Massefski W, Walensky LD.

Nat Chem Biol. 2017 Sep;13(9):961-967. doi: 10.1038/nchembio.2433. Epub 2017 Jul 10.


Bim gene dosage is critical in modulating nephron progenitor survival in the absence of microRNAs during kidney development.

Cerqueira DM, Bodnar AJ, Phua YL, Freer R, Hemker SL, Walensky LD, Hukriede NA, Ho J.

FASEB J. 2017 Aug;31(8):3540-3554. doi: 10.1096/fj.201700010R. Epub 2017 Apr 26.


Mechanistic validation of a clinical lead stapled peptide that reactivates p53 by dual HDM2 and HDMX targeting.

Wachter F, Morgan AM, Godes M, Mourtada R, Bird GH, Walensky LD.

Oncogene. 2017 Apr;36(15):2184-2190. doi: 10.1038/onc.2016.361. Epub 2016 Oct 10.


Challenges in Targeting a Basic Helix-Loop-Helix Transcription Factor with Hydrocarbon-Stapled Peptides.

Edwards AL, Meijer DH, Guerra RM, Molenaar RJ, Alberta JA, Bernal F, Bird GH, Stiles CD, Walensky LD.

ACS Chem Biol. 2016 Nov 18;11(11):3146-3153. Epub 2016 Oct 4.


Selective Covalent Targeting of Anti-Apoptotic BFL-1 by Cysteine-Reactive Stapled Peptide Inhibitors.

Huhn AJ, Guerra RM, Harvey EP, Bird GH, Walensky LD.

Cell Chem Biol. 2016 Sep 22;23(9):1123-1134. doi: 10.1016/j.chembiol.2016.07.022. Epub 2016 Sep 8.


Biophysical determinants for cellular uptake of hydrocarbon-stapled peptide helices.

Bird GH, Mazzola E, Opoku-Nsiah K, Lammert MA, Godes M, Neuberg DS, Walensky LD.

Nat Chem Biol. 2016 Oct;12(10):845-52. doi: 10.1038/nchembio.2153. Epub 2016 Aug 22.


Allosteric inhibition of antiapoptotic MCL-1.

Lee S, Wales TE, Escudero S, Cohen DT, Luccarelli J, Gallagher CG, Cohen NA, Huhn AJ, Bird GH, Engen JR, Walensky LD.

Nat Struct Mol Biol. 2016 Jun;23(6):600-7. doi: 10.1038/nsmb.3223. Epub 2016 May 9.


Reply to Fernandez-Marrero et al.: Role of BOK at the intersection of endoplasmic reticulum stress and apoptosis regulation.

Carpio MA, Michaud M, Zhou W, Fisher JK, Walensky LD, Katz SG.

Proc Natl Acad Sci U S A. 2016 Feb 2;113(5):E494-5. doi: 10.1073/pnas.1521979113. Epub 2016 Jan 25. No abstract available.


SWI/SNF-mutant cancers depend on catalytic and non-catalytic activity of EZH2.

Kim KH, Kim W, Howard TP, Vazquez F, Tsherniak A, Wu JN, Wang W, Haswell JR, Walensky LD, Hahn WC, Orkin SH, Roberts CW.

Nat Med. 2015 Dec;21(12):1491-6. doi: 10.1038/nm.3968. Epub 2015 Nov 9.

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