Synthesis of leucine enkephalin derivatives: Structure-function studies

Nirankar S. Agarwal, Victor J. Hruby, Robert Katz, Werner Klee, Marshall Nirenberg

Research output: Contribution to journalArticlepeer-review

16 Scopus citations

Abstract

The solid phase synthesis of highly purified [Leu5] enkephalin and of seven derivatives including [Ala2,Leu5]-, [Ser2,Leu5]-, [Ser3,Leu5]-, [Aba2,Leu5]-, and [des-Gly2(3),Leu5]enkephalins are reported, and their morphine-like activities in neuroblastoma x glioma cell homogenates were measured. Changes at the 2, 3, and 5 positions of the enkephalin provided analogues which were all less active than [Leu5] enkephalin. The results are discussed in terms of recently suggested conformational structures for the enkephalin peptides. No melanocyte stimulating activity was observed for [Leu5] enkephalin, [Ala2,Leu5]enkephalin, or [Ser2,Leu5] enkephalin.

Original languageEnglish (US)
Pages (from-to)129-135
Number of pages7
JournalBiochemical and Biophysical Research Communications
Volume76
Issue number1
DOIs
StatePublished - May 9 1977

ASJC Scopus subject areas

  • Biophysics
  • Biochemistry
  • Molecular Biology
  • Cell Biology

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