The fibrate gemfibrozil is a NO- and haem-independent activator of soluble guanylyl cyclase: in vitro studies.

ABSTRACT:

Background and purpose

Fibrates are a class of drugs widely used to treat dyslipidaemias. They regulate lipid metabolism and act as PPARα agonists. Clinical trials demonstrate that besides changes in lipid profiles, fibrates decrease the incidence of cardiovascular events, with gemfibrozil exhibiting the most pronounced benefit. This study aims to characterize the effect of gemfibrozil on the activity and function of soluble guanylyl cyclase (sGC), the key mediator of NO signalling.

Experimental approach

High-throughput screening of a drug library identified gemfibrozil as a direct sGC activator. Activation of sGC is unique to gemfibrozil and is not shared by other fibrates.

Key results

Gemfibrozil activated purified sGC, induced endothelium-independent relaxation of

SUBMITTER: Sharina IG 

PROVIDER: S-EPMC4403096 | biostudies-literature | 2015 May

REPOSITORIES: biostudies-literature