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