Angiotensin II analogues with N-terminal lactam bridge cyclization: an overview on AT(1) receptor activation and tachyphylaxis

Angiotensin II analogues with N-terminal lactam bridge cyclization: an overview on AT(1) receptor activation and tachyphylaxis

Author Alves, Flavio Lopes Autor UNIFESP Google Scholar
Oliveira, Vani Xavier, Jr. Google Scholar
Miranda, Antonio Autor UNIFESP Google Scholar
Abstract Angiotensin II (AngII) is the final active product of the renin enzymatic cascade, which is responsible for sustaining blood pressure. To investigate the effect of N-terminal cyclization on AT(1) activation and tachyphylaxis, we designed conformationally constrained analogues with an i-(i+1) lactam bridge. All analogues presented the same binding coefficient and tachyphylactic index, but some of them such as Cyclo (0-1a) [Glu(0), endo-(Lys(1a))]-AngII and Cyclo (0-1a) [Asp(0), endo-(Orn(1a))]-AngII showed higher potency. The same tachyphylactic index presented by AngII and cyclic analogues was surprising. We expected a variation after the modification of AngII N-terminal region.
Keywords angiotensin II
lactam bridge
peptides
synthesis
tachyphylaxis
xmlui.dri2xhtml.METS-1.0.item-coverage Hoboken
Language English
Sponsor Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq)
Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)
Date 2016
Published in Chemical Biology & Drug Design. Hoboken, v. 88, n. 5, p. 677-682, 2016.
ISSN 1747-0277 (Sherpa/Romeo, impact factor)
Publisher Wiley
Extent 677-682
Origin http://dx.doi.org/10.1111/cbdd.12795
Access rights Closed access
Type Article
Web of Science ID WOS:000386065500004
URI https://repositorio.unifesp.br/handle/11600/56862

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