Loren D. Walensky, MD, PhD

Publications

Gavathiotis E, Reyna DE, Bellairs JA, Leshchiner ES, Walensky LD.Direct and selective small-molecule activation of proapoptotic BAX.Nat Chem Biol. 2012 Jul;8(7):639-45.
22634637
LaBelle JL, Katz SG, Bird GH, Gavathiotis E, Stewart ML, Lawrence C, Fisher JK, Godes M, Pitter K, Kung AL, Walensky LD.A stapled BIM peptide overcomes apoptotic resistance in hematologic cancers.J Clin Invest. 2012 Jun 1;122(6):2018-31.
22622039
Gavathiotis E, Walensky LD.Tracking BAX once its trigger is pulled.Cell Cycle. 2011 Mar 15;10(6).
21325897
Braun CR, Mintseris J, Gavathiotis E, Bird GH, Gygi SP, Walensky LD.Photoreactive stapled BH3 peptides to dissect the BCL-2 family interactome.Chem Biol. 2010 Dec 22;17(12):1325-33.
21168768
Bernal F, Wade M, Godes M, Davis TN, Whitehead DG, Kung AL, Wahl GM, Walensky LD.A stapled p53 helix overcomes HDMX-mediated suppression of p53.Cancer Cell. 2010 Nov 16;18(5):411-22.
21075307
Gavathiotis E, Reyna DE, Davis ML, Bird GH, Walensky LD.BH3-triggered structural reorganization drives the activation of proapoptotic BAX.Mol Cell. 2010 Nov 12;40(3):481-92.
21070973
Bird GH, Madani N, Perry AF, Princiotto AM, Supko JG, He X, Gavathiotis E, Sodroski JG, Walensky LD.Hydrocarbon double-stapling remedies the proteolytic instability of a lengthy peptide therapeutic.Proc Natl Acad Sci U S A. 2010 Aug 10;107(32):14093-8.
20660316
Stewart ML, Fire E, Keating AE, Walensky LD.The MCL-1 BH3 helix is an exclusive MCL-1 inhibitor and apoptosis sensitizer.Nat Chem Biol. 2010 Aug;6(8):595-601.
20562877
Gavathiotis E,Suzuki M,Davis ML,Pitter K,Bird GH,Katz SG,Tu HC,Kim H,Cheng EH,Tjandra N,Walensky LD.BAX activation is initiated at a novel interaction site.Nature. 2008 Oct 23;455(7216):1076-81.
18948948
Bird GH,Bernal F,Pitter K,Walensky LD.Synthesis and biophysical characterization of stabilized alpha-helices of BCL-2 domains.Methods Enzymol. 2008;446:369-86.
18603134
Pitter K,Bernal F,Labelle J,Walensky LD.Dissection of the BCL-2 family signaling network with stabilized alpha-helices of BCL-2 domains.Methods Enzymol. 2008;446:387-408.
18603135
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.Dual role
18223655
Verdine GL, Walensky LD.The challenge of drugging undruggable targets in cancer: lessons learned from targeting BCL-2 family members.Clin Cancer Res. 2007 Dec 15;13(24):7264-70. Review.
18094406
Bernal F, Tyler AF, Korsmeyer SJ, Walensky LD, Verdine GL.Reactivation of the p53 Tumor Suppressor Pathway by a Stapled p53 Peptide [J. Am. Chem. Soc. 2007, 129, 2456-2457].J Am Chem Soc. 2007 Apr 25;129(16):5298.
17388600
Oh KJ, Barbuto S, Pitter K, Morash J, Walensky LD, Korsmeyer SJ.A membrane-targeted BID BH3 peptide is sufficient for high potency activation of BAX in vitro.J Biol Chem. 2006 Dec 1;281(48):36999-7008.
16987815
Walensky LD, Pitter K, Morash J, Oh KJ, Barbuto S, Fisher J, Smith E, Verdine GL, Korsmeyer SJ.A stapled BID BH3 helix directly binds and activates BAX.Mol Cell. 2006 Oct 20;24(2):199-210.
17052454
Walensky LD.BCL-2 in the crosshairs: tipping the balance of life and death.Cell Death Differ. 2006 Aug;13(8):1339-50. Review.
16763614
Walensky LD, Kung AL, Escher I, Malia TJ, Barbuto S, Wright RD, Wagner G, Verdine GL, Korsmeyer SJ.Activation of apoptosis in vivo by a hydrocarbon-stapled BH3 helix.Science. 2004 Sep 3;305(5689):1466-70.
15353804
Letai A, Bassik MC, Walensky LD, Sorcinelli MD, Weiler S, Korsmeyer SJ.Distinct BH3 domains either sensitize or activate mitochondrial apoptosis, serving as prototype cancer therapeutics.Cancer Cell. 2002 Sep;2(3):183-92.
12242151

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DF/HCC Directory Login Update Member Profile Change Account Settings Applying for Membership Benefits Requirements Responsibilities	Loren D. Walensky, MD, PhD Publications Gavathiotis E, Reyna DE, Bellairs JA, Leshchiner ES, Walensky LD.Direct and selective small-molecule activation of proapoptotic BAX.Nat Chem Biol. 2012 Jul;8(7):639-45. 22634637 LaBelle JL, Katz SG, Bird GH, Gavathiotis E, Stewart ML, Lawrence C, Fisher JK, Godes M, Pitter K, Kung AL, Walensky LD.A stapled BIM peptide overcomes apoptotic resistance in hematologic cancers.J Clin Invest. 2012 Jun 1;122(6):2018-31. 22622039 Gavathiotis E, Walensky LD.Tracking BAX once its trigger is pulled.Cell Cycle. 2011 Mar 15;10(6). 21325897 Braun CR, Mintseris J, Gavathiotis E, Bird GH, Gygi SP, Walensky LD.Photoreactive stapled BH3 peptides to dissect the BCL-2 family interactome.Chem Biol. 2010 Dec 22;17(12):1325-33. 21168768 Bernal F, Wade M, Godes M, Davis TN, Whitehead DG, Kung AL, Wahl GM, Walensky LD.A stapled p53 helix overcomes HDMX-mediated suppression of p53.Cancer Cell. 2010 Nov 16;18(5):411-22. 21075307 Gavathiotis E, Reyna DE, Davis ML, Bird GH, Walensky LD.BH3-triggered structural reorganization drives the activation of proapoptotic BAX.Mol Cell. 2010 Nov 12;40(3):481-92. 21070973 Bird GH, Madani N, Perry AF, Princiotto AM, Supko JG, He X, Gavathiotis E, Sodroski JG, Walensky LD.Hydrocarbon double-stapling remedies the proteolytic instability of a lengthy peptide therapeutic.Proc Natl Acad Sci U S A. 2010 Aug 10;107(32):14093-8. 20660316 Stewart ML, Fire E, Keating AE, Walensky LD.The MCL-1 BH3 helix is an exclusive MCL-1 inhibitor and apoptosis sensitizer.Nat Chem Biol. 2010 Aug;6(8):595-601. 20562877 Gavathiotis E,Suzuki M,Davis ML,Pitter K,Bird GH,Katz SG,Tu HC,Kim H,Cheng EH,Tjandra N,Walensky LD.BAX activation is initiated at a novel interaction site.Nature. 2008 Oct 23;455(7216):1076-81. 18948948 Bird GH,Bernal F,Pitter K,Walensky LD.Synthesis and biophysical characterization of stabilized alpha-helices of BCL-2 domains.Methods Enzymol. 2008;446:369-86. 18603134 Pitter K,Bernal F,Labelle J,Walensky LD.Dissection of the BCL-2 family signaling network with stabilized alpha-helices of BCL-2 domains.Methods Enzymol. 2008;446:387-408. 18603135 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.Dual role 18223655 Verdine GL, Walensky LD.The challenge of drugging undruggable targets in cancer: lessons learned from targeting BCL-2 family members.Clin Cancer Res. 2007 Dec 15;13(24):7264-70. Review. 18094406 Bernal F, Tyler AF, Korsmeyer SJ, Walensky LD, Verdine GL.Reactivation of the p53 Tumor Suppressor Pathway by a Stapled p53 Peptide [J. Am. Chem. Soc. 2007, 129, 2456-2457].J Am Chem Soc. 2007 Apr 25;129(16):5298. 17388600 Oh KJ, Barbuto S, Pitter K, Morash J, Walensky LD, Korsmeyer SJ.A membrane-targeted BID BH3 peptide is sufficient for high potency activation of BAX in vitro.J Biol Chem. 2006 Dec 1;281(48):36999-7008. 16987815 Walensky LD, Pitter K, Morash J, Oh KJ, Barbuto S, Fisher J, Smith E, Verdine GL, Korsmeyer SJ.A stapled BID BH3 helix directly binds and activates BAX.Mol Cell. 2006 Oct 20;24(2):199-210. 17052454 Walensky LD.BCL-2 in the crosshairs: tipping the balance of life and death.Cell Death Differ. 2006 Aug;13(8):1339-50. Review. 16763614 Walensky LD, Kung AL, Escher I, Malia TJ, Barbuto S, Wright RD, Wagner G, Verdine GL, Korsmeyer SJ.Activation of apoptosis in vivo by a hydrocarbon-stapled BH3 helix.Science. 2004 Sep 3;305(5689):1466-70. 15353804 Letai A, Bassik MC, Walensky LD, Sorcinelli MD, Weiler S, Korsmeyer SJ.Distinct BH3 domains either sensitize or activate mitochondrial apoptosis, serving as prototype cancer therapeutics.Cancer Cell. 2002 Sep;2(3):183-92. 12242151
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