Modifications op the 4,4'-residues and SAR studies of Biphalin, a highly potent opioid receptor active peptide

Guigen Li, W. Haq, Li Xiang, Bih Show Lou, Robert Hughes, Irene A. De Leon, Peg Davis, Terrence J. Gillespie, Marek Romanowski, Zhu Xiaoyun, Aleksandra Misicka, Andrzej W. Lipkowski, Frank Porreca, Thomas P. Davis, Henry I. Yamamura, David F. O'Brien, Victor J. Hruby

Research output: Contribution to journalArticle

22 Scopus citations

Abstract

Modifications of 4,4' residues of Biphalin have resulted in greater binding selectivity and biological potency for the μ opioid receptor. A higher partition coefficient across the phospholipid bilayer membrane has been achieved by using a β-branched unusual amino acids.

Original languageEnglish (US)
Pages (from-to)555-560
Number of pages6
JournalBioorganic and Medicinal Chemistry Letters
Volume8
Issue number5
DOIs
StatePublished - Mar 3 1998

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry

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    Li, G., Haq, W., Xiang, L., Lou, B. S., Hughes, R., De Leon, I. A., Davis, P., Gillespie, T. J., Romanowski, M., Xiaoyun, Z., Misicka, A., Lipkowski, A. W., Porreca, F., Davis, T. P., Yamamura, H. I., O'Brien, D. F., & Hruby, V. J. (1998). Modifications op the 4,4'-residues and SAR studies of Biphalin, a highly potent opioid receptor active peptide. Bioorganic and Medicinal Chemistry Letters, 8(5), 555-560. https://doi.org/10.1016/S0960-894X(98)00065-1