Skip header and navigation

1 records – page 1 of 1.

Aliskiren binds to renin and prorenin bound to (pro)renin receptor in vitro.

https://arctichealth.org/en/permalink/ahliterature96250
Source
Hypertens Res. 2010 Jul 22;
Publication Type
Article
Date
Jul-22-2010
Author
Kazal Boron Biswas
Ahm Nurun Nabi
Yoshie Arai
Tsutomu Nakagawa
Akio Ebihara
Atsuhiro Ichihara
Toshifumi Watanabe
Tadashi Inagami
Fumiaki Suzuki
Author Affiliation
Laboratory of Animal Biochemistry, United Graduate School of Agricultural Science, Gifu University, Gifu, Japan.
Source
Hypertens Res. 2010 Jul 22;
Date
Jul-22-2010
Language
English
Publication Type
Article
Abstract
Human (pro)renin receptor ((P)RR) has been implicated in the augmentation of many biological and cellular processes through bindings to its ligands, renin and prorenin. In this study, we investigated the effects of aliskiren, a direct oral renin inhibitor, on the activities of free and (P)RR-bound forms of human mature renin. We also elucidated the effect of aliskiren on the 'renin activity' of the receptor-bound form of prorenin. Aliskiren had an IC(50) of 0.72 nmol l(-1) against renin. The compound competitively inhibited renin activity with an inhibitory constant (K(i)) of 0.18 nmol l(-1). Furthermore, the dissociation constants (K(D)) for aliskiren from renin and prorenin bound to (P)RR were determined using surface plasmon resonance in a BIAcore assay system (Uppsala, Sweden). These values were estimated to be 0.46+/-0.03 and 0.25+/-0.01 nmol l(-1), respectively. The compound competitively inhibited the renin activities of (P)RR-bound forms of both renin and prorenin with a K(i) of 0.14 and 0.15 nmol l(-1), respectively. These results indicate that aliskiren could be a potent inhibitor of the free forms of mature renin and of the receptor-bound forms of renin and prorenin.Hypertension Research advance online publication, 22 July 2010; doi:10.1038/hr.2010.136.
PubMed ID
20664543 View in PubMed
Less detail