Synthesis and study of a cyclic angiotensin II antagonist analogue reveals the role of π*–π* interactions in the C-terminal aromatic residue for agonist activity and its structure resemblance with AT1 non-peptide antagonists
作者:Ludmila Polevaya、Thomas Mavromoustakos、Panagiotis Zoumboulakis、Simona Golic Grdadolnik、Panagiota Roumelioti、Nektarios Giatas、Ilze Mutule、Tatjana Keivish、Demetrios V Vlahakos、Efstathios K Iliodromitis、Dimitrios Th Kremastinos、John Matsoukas
DOI:10.1016/s0968-0896(01)00059-1
日期:2001.6
clustering between the side chains of the key aminoacids Tyr(4)-His(6)-Ile(8) similar to that observed with ANG II. The obtained data show that only pi*--pi* interactions observed in ANG II or its superagonist Sar(1) [ANG II] are missing. Therefore, it can be concluded that these interactions are essential for agonist activity. Conformational analysis comparisons between AT(1) antagonists losartan, eprosartan