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News & Publications

Scientific Publications

  • The MCL-1 BH3 helix is an exclusive MCL-1 inhibitor and apoptosis sensitizer. M.L. Stewart, E. Fire, A.E. Keating & L.D. Walensky, Nature Chemical Biology, 2010. 6, p. 595–601.
    link to abstract or link to News and Views commentary
  • Hydrocarbon double-stapling remedies the proteolytic instability of a lengthy peptide therapeutic. G.H. Bird, N. Madani, A.F. Perry, A.M. Princiotto, J.G. Supko, X. He, E. Gavathiotis, J.G. Sodroski, and L.D. Walensky, PNAS, 2010. Published online before print July 21, 2010, doi: 10.1073/pnas.1002713107. link to abstract
  • Probing the α-Helical Structural Stability of Stapled p53 Peptides: Molecular Dynamics Simulations and Analysis. Z. Guo, U. Mohanty, J. Noehre, T. K. Sawyer, W. Sherman, G. Krilov, Chem Biol Drug Des, 2010. 75: p. 348-359. link to article
  • Direct inhibition of the NOTCH transcription factor complex. Moellering, R.E., M. Cornejo, T. Davis, C. Del Bianco, J.C. Aster, S.C. Blacklow, A.L. Kung, D.G. Gilliland, G.L. Verdine, and J.E. Bradner, Nature, 2009. 462, p. 182-188. link to abstract
  • BAX activation is initiated at a novel interaction site. Gavathiotis, E., M. Suzuki, M.L. Davis, K. Pitter, G.H. Bird, S.G. Katz, H.-C. Tu, H. Kim, E.H.Y. Cheng, N. Tjandra, and L.D. Walensky, Nature, 2008. 455(7216): p. 1076-1081.  link to abstract
  • A cell-penetrating helical peptide as a potential HIV-1 inhibitor. Zhang, H., Q. Zhao, S. Bhattacharya, A.A. Waheed, X. Tong, A. Hong, S. Heck, F. Curreli, M. Goger, D. Cowburn, E.O. Freed, and A.K. Debnath, J Mol Biol, 2008. 378(3): p. 565-80.  link to abstract
  • Inhibition of HIV-1 fusion by hydrogen-bond-surrogate-based alpha helices. Wang, D., M. Lu, and P.S. Arora, Angew Chem Int Ed Engl, 2008. 47(10): p. 1879-82.  link to abstract
  • Dissection of the BCL-2 family signaling network with stabilized alpha-helices of BCL-2 domains. Pitter, K., F. Bernal, J. Labelle, and L.D. Walensky, Methods Enzymol, 2008. 446: p. 387-408.  link to abstract
  • A Hydrogen Bond Surrogate Approach for Stabilization of Short Peptide Sequences in alpha-Helical Conformation. Patgiri, A., A.L. Jochim, and P.S. Arora, Acc Chem Res, 2008.  link to abstract
  • Atomic structure of a short alpha-helix stabilized by a main chain hydrogen-bond surrogate. Liu, J., D. Wang, Q. Zheng, M. Lu, and P.S. Arora, J Am Chem Soc, 2008. 130(13): p. 4334-7.  link to abstract
  • Contemporary strategies for the stabilization of peptides in the alpha-helical conformation. Henchey, L.K., A.L. Jochim, and P.S. Arora, Curr Opin Chem Biol, 2008.  link to abstract
  • Dual role of proapoptotic BAD in insulin secretion and beta cell survival. Danial, N.N., L.D. Walensky, C.Y. Zhang, C.S. Choi, J.K. Fisher, A.J. Molina, S.R. Datta, K.L. Pitter, G.H. Bird, J.D. Wikstrom, J.T. Deeney, K. Robertson, J. Morash, A. Kulkarni, S. Neschen, S. Kim, M.E. Greenberg, B.E. Corkey, O.S. Shirihai, G.I. Shulman, B.B. Lowell, and S.J. Korsmeyer, Nat Med, 2008. 14(2): p. 144-53.  link to abstract
  • Synthesis and biophysical characterization of stabilized alpha-helices of BCL-2 domains. Bird, G.H., F. Bernal, K. Pitter, and L.D. Walensky, Methods Enzymol, 2008. 446: p. 369-86.  link to abstract
  • Solution structure of a hydrocarbon stapled peptide inhibitor in complex with monomeric C-terminal domain of HIV-1 capsid. Bhattacharya, S., H. Zhang, A.K. Debnath, and D. Cowburn, J Biol Chem, 2008. 283(24): p. 16274-8.  link to abstract
  • The challenge of drugging undruggable targets in cancer: lessons learned from targeting BCL-2 family members. Verdine, G.L. and L.D. Walensky, Clin Cancer Res, 2007. 13(24): p. 7264-70.  link to abstract
  • Reactivation of the p53 tumor suppressor pathway by a stapled p53 peptide. Bernal, F., A.F. Tyler, S.J. Korsmeyer, L.D. Walensky, and G.L. Verdine, J Am Chem Soc, 2007. 129(9): p. 2456-7.  link to abstract
  • Evaluation of biologically relevant short alpha-helices stabilized by a main-chain hydrogen-bond surrogate. Wang, D., K. Chen, J.L. Kulp Iii, and P.S. Arora, J Am Chem Soc, 2006. 128(28): p. 9248-56.  link to abstract
  • Nucleation and stability of hydrogen-bond surrogate-based alpha-helices. Wang, D., K. Chen, G. Dimartino, and P.S. Arora, Org Biomol Chem, 2006. 4(22): p. 4074-81.  link to abstract
  • A stapled BID BH3 helix directly binds and activates BAX. Walensky, L.D., K. Pitter, J. Morash, K.J. Oh, S. Barbuto, J. Fisher, E. Smith, G.L. Verdine, and S.J. Korsmeyer, Mol Cell, 2006. 24(2): p. 199-210.  link to abstract
  • BCL-2 in the crosshairs: tipping the balance of life and death. Walensky, L.D., Cell Death Differ, 2006. 13(8): p. 1339-50.  link to abstract
  • Optimized synthesis of hydrogen-bond surrogate helices: surprising effects of microwave heating on the activity of Grubbs catalysts. Chapman, R.N. and P.S. Arora, Org Lett, 2006. 8(25): p. 5825-8.  link to abstract
  • Solid-phase synthesis of hydrogen-bond surrogate-derived alpha-helices. Dimartino, G., D. Wang, R.N. Chapman, and P.S. Arora, Org Lett, 2005. 7(12): p. 2389-92.  link to abstract
  • Stapled peptide induces cancer cell death. Whelan, J., Drug Discov Today, 2004. 9(21): p. 907.  link to abstract
  • Activation of apoptosis in vivo by a hydrocarbon-stapled BH3 helix. Walensky, L.D., A.L. Kung, I. Escher, T.J. Malia, S. Barbuto, R.D. Wright, G. Wagner, G.L. Verdine, and S.J. Korsmeyer, Science, 2004. 305(5689): p. 1466-70.  link to abstract
  • A highly stable short alpha-helix constrained by a main-chain hydrogen-bond surrogate. Chapman, R.N., G. Dimartino, and P.S. Arora, J Am Chem Soc, 2004. 126(39): p. 12252-3.  link to abstract
  • An All-Hydrocarbon Cross-Linking System for Enhancing the Helicity and Metabolic Stability of Peptides. Schafmeister, C.E., J. Po, and G.L. Verdine, Journal of the American Chemical Society, 2000. 122(24): p. 5891-5892.