Collect. Czech. Chem. Commun. 1999, 64, 1211-1252

Biological Function and Chemistry of Endothelin. A Review

Jan Hlaváček* and Renáta Marcová

Institute of Organic Chemistry and Biochemistry, Academy of Sciences of the Czech Republic, 166 10 Prague 6, Flemingovo nám. 2, Czech Republic


The first part of this review deals with the biosynthesis and a biological function of strongly vasoactive peptides named endothelins (ETs) including vasoactive intestinal contractor. Where it was useful, snake venoms sarafotoxins which are structural endothelin derivatives, were also mentioned. In the second part, an attention is paid to structural basis of the ETs biological activity, with respect to alterations of amino acid residues in the parent peptides modifying the conformation and consequently the physico-chemical and biological properties in corresponding ETs analogs. Special attention is focussed on the area of ETs receptors and their interaction with peptide and non peptide agonists and antagonists, important in designing selective inhibitors of ETs receptors potentially applicable as drugs in a medicine. A review with 182 references.

Keywords: Peptides; Endothelin; Sarafotoxin; Peptide synthesis; Vasoconstriction; Vasodilatation; Peptide antagonists; Non peptide antagonists; Conformation analysis.