The Zinc-Sensing Receptor GPR39 in Physiology and as a Pharmacological Target
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The Zinc-Sensing Receptor GPR39 in Physiology and as a Pharmacological Target. / Laitakari, Anna; Liu, Lingzhi; Frimurer, Thomas M.; Holst, Birgitte.
In: International Journal of Molecular Sciences, Vol. 22, No. 8, 3872, 2021.Research output: Contribution to journal › Review › Research › peer-review
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TY - JOUR
T1 - The Zinc-Sensing Receptor GPR39 in Physiology and as a Pharmacological Target
AU - Laitakari, Anna
AU - Liu, Lingzhi
AU - Frimurer, Thomas M.
AU - Holst, Birgitte
PY - 2021
Y1 - 2021
N2 - 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.
AB - 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.
KW - GPR39
KW - GPR39 agonist
KW - zinc
KW - zinc signaling
U2 - 10.3390/ijms22083872
DO - 10.3390/ijms22083872
M3 - Review
C2 - 33918078
VL - 22
JO - International Journal of Molecular Sciences (Online)
JF - International Journal of Molecular Sciences (Online)
SN - 1661-6596
IS - 8
M1 - 3872
ER -
ID: 261514466