Relative conformational rigidity in oxytocin and [1 penicillamine] oxytocin. A proposal for the relationship of conformational flexibility to peptide hormone agonism and antagonism

J. P. Meraldi, Victor J Hruby, A. I R Brewster

Research output: Contribution to journalArticle

92 Citations (Scopus)

Abstract

A comparative study of the proton and carbon 13 nuclear magnetic resonance spectral parameters of the peptide hormone oxytocin and of its competitive inhibitor [1 L penicillamine]oxytocin has been made, and the results analyzed in terms of comparative conformational and dynamic properties. The results indicate that oxytocin has a flexible conformation, while [1 L penicillamine]oxytocin has a more restricted conformation. The results provide a framework for understanding the mechanism of peptide hormone agonism and antagonism for these compounds, and an approach for understanding some features of the interaction of the hormone and related compounds with their receptor.

Original languageEnglish (US)
Pages (from-to)1373-1377
Number of pages5
JournalProceedings of the National Academy of Sciences of the United States of America
Volume74
Issue number4
StatePublished - 1977

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Peptide Hormones
Oxytocin
Protons
Magnetic Resonance Spectroscopy
Carbon
Hormones
penicillamine(1)-oxytocin

ASJC Scopus subject areas

  • General
  • Genetics

Cite this

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T1 - Relative conformational rigidity in oxytocin and [1 penicillamine] oxytocin. A proposal for the relationship of conformational flexibility to peptide hormone agonism and antagonism

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AU - Hruby, Victor J

AU - Brewster, A. I R

PY - 1977

Y1 - 1977

N2 - A comparative study of the proton and carbon 13 nuclear magnetic resonance spectral parameters of the peptide hormone oxytocin and of its competitive inhibitor [1 L penicillamine]oxytocin has been made, and the results analyzed in terms of comparative conformational and dynamic properties. The results indicate that oxytocin has a flexible conformation, while [1 L penicillamine]oxytocin has a more restricted conformation. The results provide a framework for understanding the mechanism of peptide hormone agonism and antagonism for these compounds, and an approach for understanding some features of the interaction of the hormone and related compounds with their receptor.

AB - A comparative study of the proton and carbon 13 nuclear magnetic resonance spectral parameters of the peptide hormone oxytocin and of its competitive inhibitor [1 L penicillamine]oxytocin has been made, and the results analyzed in terms of comparative conformational and dynamic properties. The results indicate that oxytocin has a flexible conformation, while [1 L penicillamine]oxytocin has a more restricted conformation. The results provide a framework for understanding the mechanism of peptide hormone agonism and antagonism for these compounds, and an approach for understanding some features of the interaction of the hormone and related compounds with their receptor.

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