title: A structure-activity study of a C-terminal endothelin analogue.
abstract: We report a structure-activity study of an endothelin (ET) analogue, obtained by introduction of a non-aminoacidic portion on the C-terminal ET pentapeptide. The peptidic moiety was modified with systematic replacement of each residue by alanine (Ala scan); further modifications were performed at the C-terminus. The biological activity was analyzed at both ET(A) and ET(B) receptor subtypes, showing that the two C-terminal residues (Ile-Trp) are very important for the activity. On the contrary, the aminoacidic central portion of the molecule appears to be much more tolerant toward modifications.
authors.affiliation: Istituto di Mutagenesi e Differenziamento, CNR, Laboratorio Sintesi Peptidica, Pisa, Italy.
authors.forename: E
authors.initials: E
authors.lastname: Cassano
authors.forename: C
authors.initials: C
authors.lastname: Galoppini
authors.forename: L
authors.initials: L
authors.lastname: Giusti
authors.forename: M
authors.initials: M
authors.lastname: Hamdan
authors.forename: M
authors.initials: M
authors.lastname: Macchia
authors.forename: M R
authors.initials: MR
authors.lastname: Mazzoni
authors.forename: E
authors.initials: E
authors.lastname: Menchini
authors.forename: S
authors.initials: S
authors.lastname: Pegoraro
authors.forename: P
authors.initials: P
authors.lastname: Rovero
mesh_terms: D000595:Amino Acid Sequence; D000818:Animals; D001667:Binding, Competitive; D001921:Brain / Q000378:metabolism; D019332:Endothelin-1 / Q000378:metabolism; D016232:Endothelins / Q000737:chemistry* / Q000494:pharmacology*; D005260:Female; D066298:In Vitro Techniques; D008297:Male; D010446:Peptide Fragments / Q000737:chemistry / Q000494:pharmacology; D011869:Radioligand Assay; D051381:Rats; D017207:Rats, Sprague-Dawley; D044022:Receptor, Endothelin A; D044023:Receptor, Endothelin B; D017466:Receptors, Endothelin / Q000378:metabolism; D013329:Structure-Activity Relationship; D014599:Uterus / Q000378:metabolism
chemical_list: D019332:Endothelin-1; D016232:Endothelins; D010446:Peptide Fragments; D044022:Receptor, Endothelin A; D044023:Receptor, Endothelin B; D017466:Receptors, Endothelin