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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.


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. Epub 2015 Sep 4.


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.


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. Epub 2015 Jun 9.


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. Epub 2015 May 26.


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. Epub 2015 Apr 6.


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.


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. Epub 2015 Jan 29.


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.


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. Epub 2014 Dec 15.


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.


Hydrocarbon-stapled peptides: principles, practice, and progress.

Walensky LD, Bird GH.

J Med Chem. 2014 Aug 14;57(15):6275-88. doi: 10.1021/jm4011675. Epub 2014 Mar 6. Review.


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. Epub 2014 Feb 20.


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.


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. Epub 2013 Dec 8.


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. Epub 2013 Aug 25.


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.


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. Epub 2013 Jul 5.


Direct BAKtivation.

Walensky LD.

Nat Struct Mol Biol. 2013 May;20(5):536-8. doi: 10.1038/nsmb.2579. No abstract available.


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. Epub 2013 Apr 25.


Playing fullBAK.

Walensky LD.

Cell Cycle. 2013 May 1;12(9):1333-4. doi: 10.4161/cc.24607. Epub 2013 Apr 11. No abstract available.


Protein-protein interactions: A PUMA mechanism unfolds.

Walensky LD.

Nat Chem Biol. 2013 Mar;9(3):141-3. doi: 10.1038/nchembio.1177. No abstract available.


Direct activation of full-length proapoptotic BAK.

Leshchiner ES, Braun CR, Bird GH, Walensky LD.

Proc Natl Acad Sci U S A. 2013 Mar 12;110(11):E986-95. doi: 10.1073/pnas.1214313110. Epub 2013 Feb 12.


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.


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.


Interview with Loren D Walensky.

Walensky LD.

Future Med Chem. 2012 Aug;4(12):1537-9. doi: 10.4155/fmc.12.86.


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.


Stemming danger with Golgified BAX.

Walensky LD.

Mol Cell. 2012 Jun 8;46(5):554-6. doi: 10.1016/j.molcel.2012.05.034.


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.


From mitochondrial biology to magic bullet: navitoclax disarms BCL-2 in chronic lymphocytic leukemia.

Walensky LD.

J Clin Oncol. 2012 Feb 10;30(5):554-7. doi: 10.1200/JCO.2011.37.9339. Epub 2011 Dec 19. No abstract available.


BAX unleashed: the biochemical transformation of an inactive cytosolic monomer into a toxic mitochondrial pore.

Walensky LD, Gavathiotis E.

Trends Biochem Sci. 2011 Dec;36(12):642-52. doi: 10.1016/j.tibs.2011.08.009. Epub 2011 Oct 4. Review.


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.

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