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  • Title: Methionine enkephalin and isosteric analogues. Part II.: Receptor conformation of methionine enkephalin.
    Author: Hudson D, Sharpe R, Szelke M.
    Journal: Int J Pept Protein Res; 1980 Feb; 15(2):122-9. PubMed ID: 6246014.
    Abstract:
    Biological activities are reported for two different types of analogues of methionine enkephalin. Cyclic analogues, bridged between the amino- and carboxy- terminals of the parent peptide, are inactive. In contrast, significant levels of activity are displayed by linear isosterically modified analogues in which the Tyr1-Gly2 peptide bond is replaced by either -CH2NH- or -CH2CH2-. Similar replacements of the Gly2-Gly3 peptide bond yield compounds with much reduced potency. These modifications serve as useful probes of the receptor conformation. Based on these findings, a model is proposed for interaction between enkephalin and its receptor.
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