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The enkephalins and opiates: structure-activity relations.

A S Horn, J R Rodgers

    The Journal of Pharmacy and Pharmacology
    |May 1, 1977
    PubMed
    Summary
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    Enkephalins and related peptides exhibit morphine-like activity due to a tyrosine residue, also known as a tyramine, at their amino terminal position. This structural feature is common in many opiate drugs and their analogues.

    Area of Science:

    • Pharmacology
    • Structural Biology
    • Medicinal Chemistry

    Background:

    • Opiate drugs are widely used for pain relief but have significant side effects.
    • Enkephalins and related peptides are endogenous opioid peptides with analgesic properties.
    • Understanding the structural basis of opioid activity is crucial for developing safer analgesics.

    Purpose of the Study:

    • To investigate the structural basis for the morphine-like activity of enkephalins and related peptides.
    • To identify common structural features between endogenous opioid peptides and traditional opiate drugs.

    Main Methods:

    • Detailed examination of the X-ray structures of nine "opiate" drugs.
    • Comparative analysis of structural data to identify conserved pharmacophores.

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    Main Results:

    • A tyrosine residue, or a conformationally similar moiety, was identified at the amino terminal position of enkephalins and related peptides.
    • This tyrosine/tyramine residue was found to be present in many opiate drugs and their analogues.
    • The presence of this residue is proposed as a key factor contributing to morphine-like activity.

    Conclusions:

    • The tyrosine/tyramine residue at the amino terminus is a significant structural determinant for the pharmacological activity of enkephalins and related peptides.
    • This finding provides a structural rationale for the observed opioid activity of these peptides and highlights a common feature with traditional opiate drugs.
    • This knowledge can inform the design of novel analgesic compounds with potentially improved safety profiles.