Structure-activity relationship in vasoconstrictor effects of sarafotoxins and endothelin-1.

Abstract:

:Sarafotoxins (SRTa, SRTb and SRTc) as well as endothelin-1 (ET-1) produced vasoconstrictions in rat thoracic aorta, rat isolated perfused mesentery and pithed rat in various of extents. The potency was ET-1 greater than SRTb greater than SRTa greater than SRTc at lower doses, but SRTb greater than ET-1 greater than SRTa greater than SRTc at higher doses. [Nitrophenylsulfenylated Trp21]SRTb and SRTb(1-19) caused no vasoconstriction. Either the reduction and carboxymethylation of Cys residues, the destruction of the intramolecular loop or the production of the non-natural disulfide bond, eliminated the constrictor activity. These results indicate that Trp21 and the intramolecular loop structure are essential, and Lys9 and Tyr13 may play some important roles for the vasoconstrictor activity of these peptides.

journal_name

FEBS Lett

journal_title

FEBS letters

authors

Kitazumi K,Shiba T,Nishiki K,Furukawa Y,Takasaki C,Tasaka K

doi

10.1016/0014-5793(90)80120-8

subject

Has Abstract

pub_date

1990-01-29 00:00:00

pages

269-72

issue

2

eissn

0014-5793

issn

1873-3468

journal_volume

260

pub_type

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