The Zinc-Sensing Receptor GPR39 in Physiology and as a Pharmacological Target

International Journal of Molecular Sciences

Lingzhi Liu¹  Anna Laitakari¹  ThomasM. Frimurer¹  Birgitte Holst¹ 

[1] Novo Nordisk Foundation Center for Basic Metabolic Research, Faculty of Health and Medical Sciences, University of Copenhagen, Blegdamsvej 3, 2200 Copenhagen, Denmark;

关键词: GPR39;    GPR39 agonist;    zinc;    zinc signaling;   

DOI  :  10.3390/ijms22083872

来源: DOAJ

【 摘 要 】

The G-protein coupled receptor GPR39 is abundantly expressed in various tissues and can be activated by changes in extracellular Zn²⁺ in physiological concentrations. Previously, genetically modified rodent models have been able to shed some light on the physiological functions of GPR39, and more recently the utilization of novel synthetic agonists has led to the unraveling of several new functions in the variety of tissues GPR39 is expressed. Indeed, GPR39 seems to be involved in many important metabolic and endocrine functions, but also to play a part in inflammation, cardiovascular diseases, saliva secretion, bone formation, male fertility, addictive and depression disorders and cancer. These new discoveries offer opportunities for the development of novel therapeutic approaches against many diseases where efficient therapeutics are still lacking. This review focuses on Zn²⁺ as an endogenous ligand as well as on the novel synthetic agonists of GPR39, placing special emphasis on the recently discovered physiological functions and discusses their pharmacological potential.

【 授权许可】

Unknown