ISSN:
1573-3904
Keywords:
Cyclic peptide
;
Receptor
;
Subtype
;
Endothelin
;
Antagonist
Source:
Springer Online Journal Archives 1860-2000
Topics:
Chemistry and Pharmacology
Notes:
Abstract RES-701-1 is an endothelin B receptor (ETB) selective peptidic antagonist, which has a novel cyclic structure of microbial origin. Modification at the C-terminal free carboxyl group of RES-701-1 by a methyl ester results in an ETA/ETB dual selective analog, which showed relatively high affinity for ETA receptor subtype, while retaining the affinity for ETB. The carboxyl-group-deleted analog with tryptamine as the C-terminal residue also showed relatively weak affinity for ETA; however, benzyl ester or amide analogs did not show remarkable affinity for ETA. It is suggested that the binding mode of RES-701-1 and its analogs is different from those of known ligands for ET receptors.
Type of Medium:
Electronic Resource
URL:
http://dx.doi.org/10.1023/A:1008887108419
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