Accession Number : ADP008545

Title :   Design and Synthesis of a Specific Endothelin-1 Antagonist,

Corporate Author : ALBANY MEDICAL COLL NY

Personal Author(s) : Spinella, Michael J. ; Everitt, John ; Malik, Asrar B. ; Andersen, Thomas T.

Report Date : 1992

Pagination or Media Count : 2

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.

Descriptors :   *PHARMACOLOGICAL ANTAGONISTS, *VASOCONSTRICTING, AMINO ACIDS, SULFIDES, CHEMICAL BONDS, LUNG.

Subject Categories : Pharmacology

Distribution Statement : APPROVED FOR PUBLIC RELEASE