Design, synthesis, and incorporation of a beta-turn mimetic in angiotensin II forming novel pseudopeptides with affinity for AT(1) and AT(2) receptors
2006 (English)In: Journal of Medicinal Chemistry, ISSN 0022-2623, E-ISSN 1520-4804, Vol. 49, no 20, 6133-6137 p.Article in journal (Refereed) Published
A benzodiazepine-based beta-turn mimetic has been designed, synthesized, and incorporated into angiotensin II. Comparison of the mimetic with beta-turns in crystallized proteins showed that it most closely resembles a type II beta-turn. The compounds exhibited high to moderate binding affinity for the AT(2) receptor, and one also displayed high affinity for the AT(1) receptor. Molecular modeling showed that the high-affinity compounds could be incorporated into a previously derived model of AT(2) receptor ligands.
Place, publisher, year, edition, pages
2006. Vol. 49, no 20, 6133-6137 p.
IdentifiersURN: urn:nbn:se:uu:diva-95769DOI: 10.1021/jm051222gISI: 000240826200029PubMedID: 17004728OAI: oai:DiVA.org:uu-95769DiVA: diva2:170105