2024

Covalent inhibition of pro-apoptotic BAX.
McHenry MW, Shi P, Camara CM, Cohen DT, Rettenmaier TJ, Adhikary U, Gygi MA, Yang K, Gygi SP, Wales TE, Engen JR, Wells JA, Walensky LD.
Nat Chem Biol. 2024 Jan 17. doi:https://doi.org/10.1038/s41589-023-01537-6. Epub 2024 Jan 17.

A stapled lipopeptide platform for preventing and treating highly pathogenic viruses of pandemic potential.
Bird GH, Patten JJ, Zavadoski W, Barucci N, Godes M, Moyer BM, Owen CD, DaSilva-Jardine P, Neuberg DS, Bowen RA, Davey RA, Walensky LD.
Nat Commun. 2024 Jan 4;15(1):274. doi: 10.1038/s41467-023-44361-1. Epub 2024 Jan 4. PMID: 38177138; PMCID: PMC10766962.

2023

Targeting MCL-1 triggers DNA damage and an anti-proliferative response independent from apoptosis induction.
Adhikary U, Paulo JA, Godes M, Roychoudhury S, Prew MS, Ben-Nun Y, Yu EW, Budhraja A, Opferman JT, Chowdhury D, Gygi SP, Walensky LD.
Cell Rep. 2023 Oct 31;42(10):113176. doi:https://doi.org/10.1016/j.celrep.2023.113176. Epub 2023 Sep 27. PMID: 37773750 PMCID: PMC10787359.

Preclinical models for prediction of immunotherapy outcomes and immune evasion mechanisms in genetically heterogeneous multiple myeloma.
Larrayoz M, Garcia-Barchino MJ, Celay J, Etxebeste A, Jimenez M, Perez C, Ordoñez R, Cobaleda C, Botta C, Fresquet V, Roa S, Goicoechea I, Maia C, Lasaga M, Chesi M, Bergsagel PL, Larrayoz MJ, Calasanz MJ, Campos-Sanchez E, Martinez-Cano J, Panizo C, Rodriguez-Otero P, Vicent S, Roncador G, Gonzalez P, Takahashi S, Katz SG, Walensky LD, Ruppert SM, Lasater EA, Amann M, Lozano T, Llopiz D, Sarobe P, Lasarte JJ, Planell N, Gomez-Cabrero D, Kudryashova O, Kurilovich A, Revuelta MV, Cerchietti L, Agirre X, San Miguel J, Paiva B, Prosper F, Martinez-Climent JA.
Nat Med. 2023 Mar;29(3):632-645. doi: 10.1038/s41591-022-02178-3. Epub 2023 Mar 16. PMID: 36928817; PMCID: PMC10033443.

2022

Inhibition of FOXP3 by stapled alpha-helical peptides dampens regulatory T cell function.
Hawley KM, Eclov RJ, Schnorenberg MR, Tian Y, Shah RN, Thomas-Toth AT, Fefferman M, Bird GH, Walensky LD, Tirrell MV, LaBelle JL.
Proc Natl Acad Sci U S A. 2022 Oct 18;119(42):e2209044119. doi: 10.1073/pnas.2209044119. Epub 2022 Oct 13. PMID: 36227917

MCL-1 is a master regulator of cancer dependency on fatty acid oxidation.
Prew MS, Adhikary U, Choi DW, Portero EP, Paulo JA, Gowda P, Budhraja A, Opferman JT, Gygi SP, Danial NN, Walensky LD.
Cell Rep. 2022 Oct 4;41(1):111445. doi: 10.1016/j.celrep.2022.111445. PMID: 36198266

Generation of Potent and Stable GLP-1 Analogues Via “Serine Ligation”.
Levine PM, Craven TW, Li X, Balana AT, Bird GH, Godes M, Salveson PJ, Erickson PW, Lamb M, Ahlrichs M, Murphy M, Ogohara C, Said MY, Walensky LD, Pratt MR, Baker D.
ACS Chem Biol. 2022 Apr 15;17(4):804-809. doi: 10.1021/acschembio.2c00075. Epub 2022 Mar 23.

Structural basis for defective membrane targeting of mutant enzyme in human VLCAD deficiency.
Prew MS, Camara CM, Botzanowski T, Moroco JA, Bloch NB, Levy HR, Seo HS, Dhe-Paganon S, Bird GH, Herce HD, Gygi MA, Escuerdo S, Wales TE, Engen JR, Walensky LD.
Nat Commun. 2022 Jun 27;13(1):3669. doi: 10.1038/s41467-022-31466-2.

2021

Glucose metabolism and pyruvate carboxylase enhance glutathione synthesis and restrict oxidative stress in pancreatic islets.
Fu A, van Rooyen L, Evans L, Armstrong N, Avizonis D, Kin T, Bird GH, Reddy A, Chouchani ET, Liesa-Roig M, Walensky LD, Shapiro AMJ, Danial NN.
Cell Rep. 2021 Nov 23;37(8):110037. doi: 10.1016/j.celrep.2021.110037.

The conformational stability of pro-apoptotic BAX is dictated by discrete residues of the protein core.
Bloch NB, Wales TE, Prew MS, Levy HR, Engen JR, Walensky LD.
Nat Commun. 2021 Aug 13;12(1):4932. doi: 10.1038/s41467-021-25200-7.

Characterizing native and hydrocarbon-stapled enfuvirtide conformations with ion mobility mass spectrometry and hydrogen-deuterium exchange.
Stocks BB, Bird GH, Walensky LD, Melanson JE.
J Am Soc Mass Spectrom. 2021 Mar 3;32(3):753-761. doi: 10.1021/jasms.0c00453. Epub 2021 Feb 3.

Binding and transport of SFPQ-RNA granules by KIF5A/KLC1 motors promotes axon survival.
Fukuda Y, Pazyra-Murphy MF, Silagi ES, Tasdemir-Yilmaz OE, Li Y, Rose L, Yeoh ZC, Vangos NE, Geffken EA, Seo HS, Adelmant G, Bird GH, Walensky LD, Marto JA, Dhe-Paganon S, Segal RA.
J Cell Biol. 2021 Jan 4;220(1):e202005051. doi: 10.1083/jcb.202005051.

2020

Glucose-dependent partitioning of arginine to the urea cycle protects β-cells from inflammation.
Fu A, Alvarez-Perez JC, Avizonis D, Kin T, Ficarro SB, Choi DW, Karakose E, Badur MG, Evans L, Rosselot C, Bridon G, Bird GH, Seo HS, Dhe-Paganon S, Kamphorst JJ, Stewart AF, James Shapiro AM, Marto JA, Walensky LD, Jones RG, Garcia-Ocana A, Danial NN.
Nat Metab. 2020 May;2(5):432-446. doi: 10.1038/s42255-020-0199-4. Epub 2020 May 11.

Hydrocarbon-Stitched Peptide Agonists of Glucagon-Like Peptide-1 Receptor.
Bird GH, Fu A, Escudero S, Godes M, Opoku-Nsiah K, Wales TE, Cameron MD, Engen JR, Danial NN, Walensky LD.
ACS Chem Biol. 2020 Jun 19;15(6):1340-1348. doi: 10.1021/acschembio.0c00308. Epub 2020 May 27.

Identification of a Structural Determinant for Selective Targeting of HDMX.
Ben-Nun Y, Seo HS, Harvey EP, Hauseman ZJ, Wales TE, Newman CE, Cathcart AM, Engen JR, Dhe-Paganon S, Walensky LD.
Structure. 2020 Jul 7;28(7):847-857.e5. doi: 10.1016/j.str.2020.04.011. Epub 2020 Apr 30.

Site-Dependent Cysteine Lipidation Potentiates the Activation of Proapoptotic BAX.
Cohen DT, Wales TE, McHenry MW, Engen JR, Walensky LD.
Cell Rep. 2020 Mar 10;30(10):3229-3239.e6. doi: 10.1016/j.celrep.2020.02.057.

Mind the gap: Expediting gender parity in MD-PhD admissions.
Rowell TR, Redd RA, Neuberg DS, Walensky LD.
JCI Insight. 2020 Feb 27;5(4):e136037. doi: 10.1172/jci.insight.136037.

A redox switch regulates the structure and function of anti-apoptotic BFL-1.
Korshavn KJ, Wales TE, Bird GH, Engen JR, Walensky LD.
Nat Struct Mol Biol. 2020 Sep;27(9):781-789. doi: 10.1038/s41594-020-0458-9. Epub 2020 Jul 13.

Homogenous Oligomers of Pro-apoptotic BAX Reveal Structural Determinants of Mitochondrial Membrane Permiabilization.
Hauseman ZJ, Harvey EP, Newman CE, Wales TE, Bucci JC, Mintseris J, Schweppe DK, David L, Fan L, Cohen DT, Herce HD, Mourtada R, Ben-Nun Y, Bloch NB, Hansen SB, Wu H, Gygi SP, Engen JR, Walensky LD.
Mol Cell. 2020 Jul 2;79(1):68-83.e7. doi: 10.1016/j.molcel.2020.05.029. Epub 2020 Jun 12.

Targeting a helix-in-groove interaction between E! and E2 blocks ubiquitin transfer.
Cathcart AM, Bird GH, Wales TE, Herce HD, Harvey EP, Hauseman ZJ, Newman CE, Adhikary U, Prew MS, Oo T, Lee S, Engen JR, Walensky LD.
Nat Chem Biol. 2020 Nov;16(11):1218-1226. doi: 10.1038/s41589-020-0625-7. Epub 2020 Aug 17.

Identification of a Covalent Molecular Inhibitor of Anti-apoptotic BFL-1 by Disulfide Tethering.
Harvey EP, Hauseman ZJ, Cohen DT, Rettenmaier TJ, Lee S, Huhn AJ, Wales TE, Seo HS, Luccarelli J, Newman CE, Guerra RM, Bird GH, Dhe-Paganon S, Engen JR, Wells JA, Walensky LD.
Cell Chem Biol. 2020 Jun 18;27(6):647-656.e6. doi: 10.1016/j.chembiol.2020.04.004. Epub 2020 May 14.

2019

Design of stapled antimicrobial peptides that are stable, nontoxic and kill antibiotic-resistant bacteria in mice.
Mourtada R, Herce HD, Yin DJ, Moroco JA, Wales TE, Engen JR, Walensky LD.
Nat Biotechnol. 2019 Oct;37(10):1186-1197. doi: 10.1038/s41587-019-0222-z. Epub 2019 Aug 19.

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.

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.

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.

2018

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.

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.

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.

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.

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.

2017

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.

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.

Paclitaxel Reduces Axonal Bclw to Initiate IP 3 R1-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.

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.

2016

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. doi: 10.1021/acschembio.6b00465. Epub 2016 Oct 4.

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.

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.

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.

2015

Cellular Uptake and Ultrastructural Localization Underlie the Pro-apoptotic Activity of a Hydrocarbon-stapled BIM BH3 Peptide.
Edwards AL, Wachter F, Lammert M, Huhn AJ, Luccarelli J, Bird GH, Walensky LD.
ACS Chem Biol. 2015 Sep 18;10(9):2149-57. doi: 10.1021/acschembio.5b00214. Epub 2015 Jul 21.

Inhibition of Pro-apoptotic BAX by a noncanonical interaction mechanism.
Barclay LA, Wales TE, Garner TP, Wachter F, Lee S, Guerra RM, Stewart ML, Braun CR, Bird GH, Gavathiotis E, Engen JR, Walensky LD.
Mol Cell. 2015 Mar 5;57(5):873-886. doi: 10.1016/j.molcel.2015.01.014. Epub 2015 Feb 12.

Direct inhibition of oncogenic KRAS by hydrocarbon-stapled SOS1 helices.
Leshchiner ES, Parkhitko A, Bird GH, Luccarelli J, Bellairs JA, Escudero S, Opoku-Nsiah K, Godes M, Perrimon N, Walensky LD.
Proc Natl Acad Sci U S A. 2015 Feb 10;112(6):1761-6. doi: 10.1073/pnas.1413185112. Epub 2015 Jan 26.

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.

Generation of multiple reporter ions from a single isobaric reagent increases multiplexing capacity for quantitative proteomics.
Braun CR, Bird GH, Wühr M, Erickson BK, Rad R, Walensky LD, Gygi SP, Haas W.
Anal Chem. 2015 Oct 6;87(19):9855-63. doi: 10.1021/acs.analchem.5b02307.

Regulation of mitochondrial ceramide distribution by members of the BCL-2 family.
Zhang T, Barclay L, Walensky LD, Saghatelian A.
J Lipid Res. 2015 Aug;56(8):1501-10. doi: 10.1194/jlr.M058750.

BCL-2 family member BOK promotes apoptosis in response to endoplasmic reticulum stress.
Carpio MA, Michaud M, Zhou W, Fisher JK, Walensky LD, Katz SG.
Proc Natl Acad Sci U S A. 2015 Jun 9;112(23):7201-6. doi: 10.1073/pnas.1421063112.

A nonapoptotic role for BAX and BAK in eicosanoid metabolism.
Zhang T, Walensky LD, Saghatelian A.
ACS Chem Biol. 2015 Jun 19;10(6):1398-403. doi: 10.1021/acschembio.5b00168.

Phospho-BAD BH3 mimicry protects β cells and restores functional β cell mass in diabetes.
Ljubicic S, Polak K, Fu A, Wiwczar J, Szlyk B, Chang Y, Alvarez-Perez JC, Bird GH, Walensky LD, Garcia-Ocaña A, Danial NN.
Cell Rep. 2015 Feb 3;10(4):497-504. doi: 10.1016/j.celrep.2014.12.056.

2014

Stapled HIV-1 peptides recapitulate antigenic structures and engage broadly neutralizing antibodies.
Bird GH, Irimia A, Ofek G, Kwong PD, Wilson IA, Walensky LD.
Nat Struct Mol Biol. 2014 Dec;21(12):1058-67. doi: 10.1038/nsmb.2922. Epub 2014 Nov 24.

Photoreactive stapled peptides to identify and characterize BCL-2 family interaction sites by mass spectrometry.
Lee S, Braun CR, Bird GH, Walensky LD.
Methods Enzymol. 2014;544:25-48. doi: 10.1016/B978-0-12-417158-9.00002-9.

Mucosal delivery of a double-stapled RSV peptide prevents nasopulmonary infection.
Bird GH, Boyapalle S, Wong T, Opoku-Nsiah K, Bedi R, Crannell WC, Perry AF, Nguyen H, Sampayo V, Devareddy A, Mohapatra S, Mohapatra SS, Walensky LD.
J Clin Invest. 2014 May;124(5):2113-24. doi: 10.1172/JCI71856. Epub 2014 Apr 17.

Distinct BimBH3 (BimSAHB) stapled peptides for structural and cellular studies.
Bird GH, Gavathiotis E, LaBelle JL, Katz SG, Walensky LD.
ACS Chem Biol. 2014 Mar 21;9(3):831-7. doi: 10.1021/cb4003305. Epub 2014 Jan 3.

Mantle cell lymphoma in cyclin D1 transgenic mice with Bim-deficient B cells.
Katz SG, Labelle JL, Meng H, Valeriano RP, Fisher JK, Sun H, Rodig SJ, Kleinstein SH, Walensky LD.
Blood. 2014 Feb 6;123(6):884-93. doi: 10.1182/blood-2013-04-499079. Epub 2013 Dec 18.

Complementary genomic approaches highlight the PI3K/mTOR pathway as a common vulnerability in osteosarcoma.
Perry JA, Kiezun A, Tonzi P, Van Allen EM, Carter SL, Baca SC, Cowley GS, Bhatt AS, Rheinbay E, Pedamallu CS, Helman E, Taylor-Weiner A, McKenna A, DeLuca DS, Lawrence MS, Ambrogio L, Sougnez C, Sivachenko A, Walensky LD, Wagle N, Mora J, de Torres C, Lavarino C, Dos Santos Aguiar S, Yunes JA, Brandalise SR, Mercado-Celis GE, Melendez-Zajgla J, Cárdenas-Cardós R, Velasco-Hidalgo L, Roberts CW, Garraway LA, Rodriguez-Galindo C, Gabriel SB, Lander ES, Golub TR, Orkin SH, Getz G, Janeway KA.
Proc Natl Acad Sci U S A. 2014 Dec 23;111(51):E5564-73. doi: 10.1073/pnas.1419260111.

Repression of BIM mediates survival signaling by MYC and AKT in high-risk T-cell acute lymphoblastic leukemia.
Reynolds C, Roderick JE, LaBelle JL, Bird G, Mathieu R, Bodaar K, Colon D, Pyati U, Stevenson KE, Qi J, Harris M, Silverman LB, Sallan SE, Bradner JE, Neuberg DS, Look AT, Walensky LD, Kelliher MA, Gutierrez A.
Leukemia. 2014 Sep;28(9):1819-27. doi: 10.1038/leu.2014.78.

A phospho-BAD BH3 helix activates glucokinase by a mechanism distinct from that of allosteric activators.
Szlyk B, Braun CR, Ljubicic S, Patton E, Bird GH, Osundiji MA, Matschinsky FM, Walensky LD, Danial NN.
Nat Struct Mol Biol. 2014 Jan;21(1):36-42. doi: 10.1038/nsmb.2717.

2013

Direct activation of full-length proapoptotic BAK.
Leshchiner ES, Braun CR, Bird GH, Walensky LD.
Proc Natl Acad Sci USA. 2013 Mar 12;110(11):E986-95. doi: 10.1073/pnas.1214313110. Epub 2013 Feb 12.

Multimodal interaction with BCL-2 family proteins underlies the proapoptotic activity of PUMA BH3.
Edwards AL, Gavathiotis E, LaBelle JL, Braun CR, Opoku-Nsiah KA, Bird GH, Walensky LD.
Chem Biol. 2013 Jul 25;20(7):888-902. doi: 10.1016/j.chembiol.2013.06.007.

Direct BAKtivation.
Walensky LD.
Nat Struct Mol Biol. 2013 May;20(5):536-8. doi: 10.1038/nsmb.2579.

Playing fullBAK.
Walensky LD.
Cell Cycle. 2013 May 1;12(9):1333-4. doi: 10.4161/cc.24607. Epub 2013 Apr 11.

Protein-protein interactions: A PUMA mechanism unfolds.
Walensky LD.
Nat Chem Biol. 2013 Mar;9(3):141-3. doi: 10.1038/nchembio.1177.

Brain and testicular tumors in mice with progenitor cells lacking BAX and BAK.
Katz SG, Fisher JK, Correll M, Bronson RT, Ligon KL, Walensky LD.
Oncogene. 2013 Aug 29;32(35):4078-85. doi: 10.1038/onc.2012.421. Epub 2012 Sep 17.

Targeted disruption of the EZH2-EED complex inhibits EZH2-dependent cancer.
Kim W, Bird GH, Neff T, Guo G, Kerenyi MA, Walensky LD, Orkin SH.
Nat Chem Biol. 2013 Oct;9(10):643-50. doi: 10.1038/nchembio.1331.

Evaluation and critical assessment of putative MCL-1 inhibitors.
Varadarajan S, Vogler M, Butterworth M, Dinsdale D, Walensky LD, Cohen GM.
Cell Death Differ. 2013 Nov;20(11):1475-84. doi: 10.1038/cdd.2013.79.

The retinoblastoma protein induces apoptosis directly at the mitochondria.
Hilgendorf KI, Leshchiner ES, Nedelcu S, Maynard MA, Calo E, Ianari A, Walensky LD, Lees JA.
Genes Dev. 2013 May 1;27(9):1003-15. doi: 10.1101/gad.211326.112.

2012

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.

Direct and selective small-molecule activation of proapoptotic BAX.
Gavathiotis E, Reyna DE, Bellairs JA, Leshchiner ES, Walensky LD.
Nat Chem Biol. 2012 Jul;8(7):639-45. doi: 10.1038/nchembio.995. Epub 2012 May 27.

A stapled BIM peptide overcomes apoptotic resistance in hematologic cancers.
LaBelle JL, Katz SG, Bird GH, Gavathiotis E, Stewart ML, Lawrence C, Fisher JK, Godes M, Pitter K, Kung AL, Walensky LD.
J Clin Invest. 2012 Jun;122(6):2018-31. doi: 10.1172/JCI46231. Epub 2012 May 24.

Targeted disruption of the BCL9/β-catenin complex inhibits oncogenic Wnt signaling.
Takada K, Zhu D, Bird GH, Sukhdeo K, Zhao JJ, Mani M, Lemieux M, Carrasco DE, Ryan J, Horst D, Fulciniti M, Munshi NC, Xu W, Kung AL, Shivdasani RA, Walensky LD, Carrasco DR.
Sci Transl Med. 2012 Aug 22;4(148):148ra117. doi: 10.1126/scitranslmed.3003808.

2011

Chemical synthesis of hydrocarbon-stapled peptides for protein interaction research and therapeutic targeting.
Bird GH, Crannell WC, Walensky LD.
Curr Protoc Chem Biol. 2011 Sep 1;3(3):99-117. doi: 10.1002/9780470559277.ch110042.

BAX unleashed: the biochemical transformation of an inactive cytosolic monomer into a toxic mitochondrial pore.
Walensky LD, Gavathiotis E.

2010

Hydrocarbon double-stapling remedies the proteolytic instability of a lengthy peptide therapeutic.
Bird GH, Madani N, Perry AF, Princiotto AM, Supko JG, He X, Gavathiotis E, Sodroski JG, Walensky LD.
Proc Natl Acad Sci U S A. 2010 Aug 10;107(32):14093-8. doi: 10.1073/pnas.1002713107. Epub 2010 Jul 21.

A stapled p53 helix overcomes HDMX-mediated suppression of p53.
Bernal F, Wade M, Godes M, Davis TN, Whitehead DG, Kung AL, Wahl GM, Walensky LD.
Cancer Cell. 2010 Nov 16;18(5):411-22. doi: 10.1016/j.ccr.2010.10.024.

BH3-triggered structural reorganization drives the activation of proapoptotic BAX.
Gavathiotis E, Reyna DE, Davis ML, Bird GH, Walensky LD.
Mol Cell. 2010 Nov 12;40(3):481-92. doi: 10.1016/j.molcel.2010.10.019.

Photoreactive stapled BH3 peptides to dissect the BCL-2 family interactome.
Braun CR, Mintseris J, Gavathiotis E, Bird GH, Gygi SP, Walensky LD.
Chem Biol. 2010 Dec 22;17(12):1325-33. doi: 10.1016/j.chembiol.2010.09.015.

The MCL-1 BH3 helix is an exclusive MCL-1 inhibitor and apoptosis sensitizer.
Stewart ML, Fire E, Keating AE, Walensky LD.
Nat Chem Biol. 2010 Aug;6(8):595-601. doi: 10.1038/nchembio.391. Epub 2010 Jun 20.

2008

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.

Dissection of the BCL-2 family signaling network with stabilized alpha-helices of BCL-2 domains.
Pitter K, Bernal F, Labelle J, Walensky LD.
Methods Enzymol. 2008;446:387-408. doi: 10.1016/S0076-6879(08)01623-6.

Synthesis and biophysical characterization of stabilized alpha-helices of BCL-2 domains.
Bird GH, Bernal F, Pitter K, Walensky LD.
Methods Enzymol. 2008;446:369-86. doi: 10.1016/S0076-6879(08)01622-4.

Dual role of proapoptotic BAD in insulin secretion and beta cell survival.
Danial NN, Walensky LD, Zhang CY, Choi CS, Fisher JK, Molina AJ, Datta SR, Pitter KL, Bird GH, Wikstrom JD, Deeney JT, Robertson K, Morash J, Kulkarni A, Neschen S, Kim S, Greenberg ME, Corkey BE, Shirihai OS, Shulman GI, Lowell BB, Korsmeyer SJ.
Nat Med. 2008 Feb;14(2):144-53. doi: 10.1038/nm1717.

2007

The challenge of drugging undruggable targets in cancer: lessons learned from targeting BCL-2 family members.
Verdine GL, Walensky LD.
Clin Cancer Res. 2007 Dec 15;13(24):7264-70. doi: 10.1158/1078-0432.CCR-07-2184.

Reactivation of the p53 tumor suppressor pathway by a stapled p53 peptide.
Bernal F, Tyler AF, Korsmeyer SJ, Walensky LD, Verdine GL.
J Am Chem Soc. 2007 Mar 7;129(9):2456-7. doi: 10.1021/ja0693587.

2006

BCL-2 in the crosshairs: tipping the balance of life and death.
Walensky LD.
Cell Death Differ. 2006 Aug;13(8):1339-50. doi: 10.1038/sj.cdd.4401992. Epub 2006 Jun 9.

2004

Activation of apoptosis in vivo by a hydrocarbon-stapled BH3 helix.
Loren D Walensky 1, Andrew L Kung, Iris Escher, Thomas J Malia, Scott Barbuto, Renee D Wright, Gerhard Wagner, Gregory L Verdine, Stanley J Korsmeyer
Science. 2004 Sep 3;305(5689):1466-70. doi: 10.1126/science.1099191.

2003

Management of an anaphylactoid reaction to methotrexate with a stepwise graded challenge.
MacGinnitie AJ, Walensky LD, Turvey SE, Orange JS, Bonilla FA, Silverman LB, Oettgen H.
Pediatr Allergy Immunol. 2003 Oct;14(5):409-11. doi: 10.1034/j.1399-3038.2003.00073.x.

Distinct distribution of specific members of protein 4.1 gene family in the mouse nephron.
Ramez M, Blot-Chabaud M, Cluzeaud F, Chanan S, Patterson M, Walensky LD, Marfatia S, Baines AJ, Chasis JA, Conboy JG, Mohandas N, Gascard P.
Kidney Int. 2003 Apr;63(4):1321-37. doi: 10.1046/j.1523-1755.2003.00870.x.

2002

Distinct BH3 domains either sensitize or activate mitochondrial apoptosis, serving as prototype cancer therapeutics.
Anthony Letai, Michael C Bassik, Loren D Walensky, Mia D Sorcinelli, Solly Weiler, Stanley J Korsmeyer
Cancer Cell. 2002 Sep;2(3):183-92. doi: 10.1016/s1535-6108(02)00127-7.