News & Publications

Research Articles:

  • Stapled α−helical peptide drug development: A potent dual inhibitor of MDM2 and MDMX for p53-dependent cancer therapy
    Chang, Y.S., Graves, B., Guerlavais, V., Tovar, C., Packman, K., To, K. -H., Olson, K. A., Kesavan, K., Gangurde, P., Mukherjee, A., Baker, T., Darlak, K., Elkin, C., Filipovic, Z., Qureshi, F. Z., Cai, H., Berry, P., Feyfant, E., Shi, X. E., Horstick, J., Annis, D. A., Manning, A. M., Fotouhi, N., Nash, H., Vassilev, L. T. & Sawyer, T. K. Stapled α−helical peptide drug development: A potent dual inhibitor of MDM2 and MDMX for p53-dependent cancer therapy. Proc Natl Acad Sci USA. doi:10.1073/pnas.1303002110 (2013). link to article
  • A stapled BIM peptide overcomes apoptotic resistance in hematologic cancers
    LaBelle, J. L., Katz, S. G., Bird, G. H., Gavathiotis, E., Stewart, M. L., Lawrence, C., Fisher, J. K., Godes, M., Pitter, K., Kung, A. L., & Walensky, L.D. A stapled BIM peptide overcomes apoptotic resistance in hematologic cancers. J Clin Invest. doi:10.1172/JCI46231 (2012). link to article
  • A stapled p53 helix overcomes HDMX-mediated suppression of p53
    Bernal, F., Wade, M., Godes, M., Davis, T. N., Whitehead, D. G., Kung, A. L., Wahl, G.M. & Walensky, L. D. A stapled p53 helix overcomes HDMX-mediated suppression of p53. Cancer Cell. 18, 411-422 (2010). link to article or link to Research Highlight in Nature Reviews Drug Discovery.
  • Hydrocarbon double-stapling remedies the proteolytic instability of a lengthy peptide therapeutic
    Bird, G. H. et al. Hydrocarbon double-stapling remedies the proteolytic instability of a lengthy peptide therapeutic. Proc. Natl. Acad. Sci. USA 107, 14093-14098 (2010). link to article
  • Reactivation of the p53 tumor suppressor pathway by a stapled p53 peptide
    Bernal, F., Tyler, A. F., Korsmeyer, S. J., Walensky, L. D. & Verdine, G. L. Reactivation of the p53 tumor suppressor pathway by a stapled p53 peptide.  J. Am. Chem. Soc. 129, 2456-2457 (2007). link to article
  • Activation of apoptosis in vivo by a hydrocarbon-stapled BH3 helix
    Walensky, L. D., Kung, A. L., Escher, I., Malia, T.J., Barbuto, S., Wright, R. D., Wagner, G., Verdine, G. L. & Korsmeyer, S. J. Activation of apoptosis in vivo by a hydrocarbon-stapled BH3 helix. Science 305, 1466-1470 (2004). link to article

Review Articles:

  • Stapled peptide reactivates p53
    Crunkhorn, S. Stapled peptide reactivates p53. Nat. Rev. Drug Discov. 12, 741 (2013). link to abstract
  • Systematic analysis of helical protein interfaces reveals targets for synthetic inhibitors
    Jochim, A. L  & Arora, P. S. Systematic analysis of helical protein interfaces reveals targets for synthetic inhibitors. ACS Chem. Biol. 5, 919-923 (2010). link to abstract
  • Current trends in the clinical development of peptide therapeutics
    Saladin, P. M., Zhang, B. D. & Reichert, J. M. Current trends in the clinical development of peptide therapeutics IDrugs 12, 779-784 (2009). link to abstract
  • The medicinal chemistry of peptides
    Nestor, J. J. Jr., The medicinal chemistry of peptides. Curr. Med. Chem. 16, 4399-4418 (2009). link to abstract
  • Synthesis and biophysical characterization of stabilized alpha-helices of BCL-2 domains
    Bird, G. H., Bernal, F., Pitter, K. & Walensky, L. D. Synthesis and biophysical characterization of stabilized alpha-helices of BCL-2 domains. Methods Enzymol. 446, 369-386 (2008). link to abstract
  • Contemporary strategies for the stabilization of peptides in the alpha-helical conformation
    Henchey, L. K., Jochim, A. L. & Arora, P. S. Contemporary strategies for the stabilization of peptides in the alpha-helical conformation. Current Opin. Chem. Biol. 12, 692-697 (2008). link to abstract
  • Principles of protein-protein interactions: What are the preferred ways for proteins to interact?
    Keskin, Z., Gursoy, A., Ma, B. & Nussinov, R. Principles of protein-protein interactions: What are the preferred ways for proteins to interact? Chem. Rev. 108, 1225–1244 (2008). link to abstract
  • The challenge of drugging undruggable targets in cancer: lessons learned from targeting BCL-2 family members
    Verdine, G. L. & Walensky, L. D. The challenge of drugging undruggable targets in cancer: lessons learned from targeting BCL-2 family members. Clin. Cancer Res. 13, 7264-7270 (2007). link to abstract