Article (Scientific journals)
Insight into SUCNR1 (GPR91) structure and function
Gilissen, Julie; Jouret, François; Pirotte, Bernard et al.
2016In Pharmacology and Therapeutics
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Keywords :
SUCNR1; GPR91; succinate; ischemia-reperfusion injury; hypertension; diabetes
Abstract :
[en] SUCNR1 (or GPR91) belongs to the family of G protein-coupled receptors (GPCR), which represents the largest group of membrane proteins in human genome. The majority of marketed drugs targets GPCRs, directly or indirectly. SUCNR1 has been classified as an orphan receptor until a landmark study paired it with succinate, a citric acid cycle intermediate. According to the current paradigm, succinate triggers SUCNR1 signaling pathways to indicate local stress that may affect cellular metabolism. SUCNR1 implication has been well documented in renin-induced hypertension, ischemia/reperfusion injury, inflammation and immune response, platelet aggregation and retinal angiogenesis. In addition, the SUCNR1-induced increase of blood pressure may contribute to diabetic nephropathy or cardiac hypertrophy. The understanding of SUCNR1 activation, signaling pathways and functions remains largely elusive, which calls for deeper investigations. SUCNR1 shows a high potential as an innovative drug target and is probably an important regulator of basic physiology. In order to achieve the full characterization of this receptor,more specific pharmacological tools such as small-molecules modulators will represent an important asset. In this review, we describe the structural features of SUCNR1, its current ligands and putative binding pocket. We give an exhaustive overview of the known and hypothetical signaling partners of the receptor in different in vitro and in vivo systems. The link between SUCNR1 intracellular pathways and its pathophysiological roles are also extensively discussed.
Disciplines :
Pharmacy, pharmacology & toxicology
Biochemistry, biophysics & molecular biology
Author, co-author :
Gilissen, Julie ;  Université de Liège > Département de pharmacie > Chimie pharmaceutique
Jouret, François  ;  Université de Liège > Département des sciences cliniques > Néphrologie
Pirotte, Bernard ;  Université de Liège > Département de pharmacie > Chimie pharmaceutique
Hanson, Julien  ;  Université de Liège > Département de pharmacie > Chimie pharmaceutique
Language :
English
Title :
Insight into SUCNR1 (GPR91) structure and function
Publication date :
2016
Journal title :
Pharmacology and Therapeutics
ISSN :
0163-7258
eISSN :
1879-016X
Publisher :
Elsevier Science
Peer reviewed :
Peer Reviewed verified by ORBi
Available on ORBi :
since 11 March 2016

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