Design and Synthesis of a Specific Endothelin-1 Antagonist,

Abstract

Members of the endothelin (Et) family of vasoconstrictors are highly homologous, 21 amino acid peptides with two conserved disulfide bonds (Cys1-Cys15THE OUTER DISULFIDE), and (Cys3-Cys11 INNER). To assess the importance of the outer disulfide bond, we synthesized a peptide in which the outer disulfide of Et-1 was replaced with an amide linkage. The resulting analog, Dpr1-Asp15 Et-1, potently inhibited Et-1 mediated vasoconstriction in the lung.

Document Details

Document Type
Technical Report
Publication Date
Jan 01, 1992
Accession Number
ADP008545

Entities

People

  • Asrar B Malik
  • John Everitt
  • Michael J. Spinella
  • Thomas T. Andersen

Organizations

  • Albany Medical College

Tags

DTIC Thesaurus Topics

  • Amino Acids
  • Amino Acids Peptides And Proteins
  • Biomolecules
  • Chemical Compounds
  • Chemical Synthesis
  • Chemistry
  • Continents
  • Geographic Regions
  • Massachusetts

Fields of Study

  • Chemistry

Readers

  • Molecular and Cellular Biochemistry