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Related Experiment Videos

Structure-function relationships of somatostatin analogs.

P Marbach1, W Bauer, U Briner

  • 1Preclinical Research Department, Sandoz Ltd., Basle, Switzerland.

Hormone Research
|January 1, 1988
PubMed
Summary

Peptide chemistry aims to create analogues with reduced size, longer half-life, and better specificity for clinical use. SMS 201-995, a somatostatin analogue, shows high potency and prolonged clearance.

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Area of Science:

  • Peptide chemistry
  • Medicinal chemistry
  • Pharmacology

Background:

  • Natural peptides often have limitations for clinical use, including short biological half-lives and low specificity.
  • Somatostatin, a natural peptide hormone, has therapeutic potential but requires analogues for improved clinical application.
  • Peptide chemistry focuses on synthesizing analogues to overcome limitations of natural peptides.

Purpose of the Study:

  • To produce peptide analogues with improved clinical properties such as reduced molecular size, prolonged biological half-life, and enhanced specificity.
  • To describe procedures for extending the duration of action of somatostatin derivatives.
  • To analyze factors influencing the specificity of synthetic peptide analogues.

Main Methods:

  • Synthesis of somatostatin analogues after elucidating its active core.

Related Experiment Videos

  • Selection of SMS 201-995, an octapeptide analogue, for further development based on potency and clearance.
  • Enhancement of lipophilicity and amino acid substitution to extend the duration of action.
  • Analysis of factors affecting analogue specificity.

    • Main Results:

    • SMS 201-995, a somatostatin analogue, was identified as a potent candidate with prolonged plasma clearance.
    • Procedures like lipophilicity enhancement and amino acid substitution can extend the duration of action of somatostatin derivatives.
    • Factors influencing the specificity of these peptide analogues were analyzed.

    Conclusions:

    • Peptide chemistry is crucial for developing clinically applicable analogues of natural peptides.
    • SMS 201-995 represents a promising somatostatin analogue with improved pharmacokinetic properties.
    • Strategies such as modifying lipophilicity and amino acid sequence are effective in optimizing peptide analogue performance for therapeutic use.