Identification and pharmacological characterization of succinate receptor agonists.

ABSTRACT:

Background and purpose

The succinate receptor (formerly GPR91 or SUCNR1) is described as a metabolic sensor that may be involved in homeostasis. Notwithstanding its implication in important (patho)physiological processes, the function of succinate receptors has remained ill-defined because no pharmacological tools were available. We report on the discovery of the first family of potent synthetic agonists.

Experimental approach

We screened a library of succinate analogues and analysed their activity on succinate receptors. Also, we modelled a pharmacophore and a binding site for this receptor. New agonists were identified based on the information provided by these two approaches. Their activity was studied in various bioassays, including measurement of cAMP levels, [Ca²⁺

SUBMITTER: Geubelle P 

PROVIDER: S-EPMC5386996 | biostudies-literature | 2017 May

REPOSITORIES: biostudies-literature