Synthesis of a new class of druglike angiotensin II C-terminal mimics with affinity for the AT2 receptor
2007 (English)In: Journal of Medicinal Chemistry, ISSN 0022-2623, E-ISSN 1520-4804, Vol. 50, no 7, 1711-1715 p.Article in journal (Refereed) Published
Four tripeptides corresponding to the C-terminal region of angiotensin II were synthesized. One of these peptides (Ac-His-Pro-Ile) showed moderate binding affinity for the AT2 receptor. Two aromatic histidine-related scaffolds were synthesized and introduced in the tripeptides to give eight new peptidomimetic structures. Three of the new peptide-derived druglike molecules exhibited selective, nanomolar affinity for the AT2 receptor. These ligands may become lead compounds in the future development of novel classes of selective AT2 receptor agonists.
Place, publisher, year, edition, pages
2007. Vol. 50, no 7, 1711-1715 p.
IdentifiersURN: urn:nbn:se:uu:diva-95771DOI: 10.1021/jm0613469ISI: 000245259000033PubMedID: 17358051OAI: oai:DiVA.org:uu-95771DiVA: diva2:170107