The Zinc-Sensing Receptor GPR39 in Physiology and as a Pharmacological Target
The G-protein coupled receptor GPR39 is abundantly expressed in various tissues and can be activated by changes in extracellular Zn<sup>2+</sup> in physiological concentrations. Previously, genetically modified rodent models have been able to shed some light on the physiological function...
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| Format: | Article |
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MDPI AG
2021-04-01
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| Series: | International Journal of Molecular Sciences |
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| Online Access: | https://www.mdpi.com/1422-0067/22/8/3872 |
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| author | Anna Laitakari Lingzhi Liu Thomas M. Frimurer Birgitte Holst |
| author_facet | Anna Laitakari Lingzhi Liu Thomas M. Frimurer Birgitte Holst |
| author_sort | Anna Laitakari |
| collection | DOAJ |
| description | The G-protein coupled receptor GPR39 is abundantly expressed in various tissues and can be activated by changes in extracellular Zn<sup>2+</sup> 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 Zn<sup>2+</sup> 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. |
| first_indexed | 2024-03-10T12:30:17Z |
| format | Article |
| id | doaj.art-ca3ed5a823db4b67b31f9b5329936114 |
| institution | Directory Open Access Journal |
| issn | 1661-6596 1422-0067 |
| language | English |
| last_indexed | 2024-03-10T12:30:17Z |
| publishDate | 2021-04-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | International Journal of Molecular Sciences |
| spelling | doaj.art-ca3ed5a823db4b67b31f9b53299361142023-11-21T14:46:16ZengMDPI AGInternational Journal of Molecular Sciences1661-65961422-00672021-04-01228387210.3390/ijms22083872The Zinc-Sensing Receptor GPR39 in Physiology and as a Pharmacological TargetAnna Laitakari0Lingzhi Liu1Thomas M. Frimurer2Birgitte Holst3Novo Nordisk Foundation Center for Basic Metabolic Research, Faculty of Health and Medical Sciences, University of Copenhagen, Blegdamsvej 3B, 2200 Copenhagen, DenmarkNovo Nordisk Foundation Center for Basic Metabolic Research, Faculty of Health and Medical Sciences, University of Copenhagen, Blegdamsvej 3B, 2200 Copenhagen, DenmarkNovo Nordisk Foundation Center for Basic Metabolic Research, Faculty of Health and Medical Sciences, University of Copenhagen, Blegdamsvej 3B, 2200 Copenhagen, DenmarkNovo Nordisk Foundation Center for Basic Metabolic Research, Faculty of Health and Medical Sciences, University of Copenhagen, Blegdamsvej 3B, 2200 Copenhagen, DenmarkThe G-protein coupled receptor GPR39 is abundantly expressed in various tissues and can be activated by changes in extracellular Zn<sup>2+</sup> 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 Zn<sup>2+</sup> 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.https://www.mdpi.com/1422-0067/22/8/3872GPR39GPR39 agonistzinczinc signaling |
| spellingShingle | Anna Laitakari Lingzhi Liu Thomas M. Frimurer Birgitte Holst The Zinc-Sensing Receptor GPR39 in Physiology and as a Pharmacological Target International Journal of Molecular Sciences GPR39 GPR39 agonist zinc zinc signaling |
| title | The Zinc-Sensing Receptor GPR39 in Physiology and as a Pharmacological Target |
| title_full | The Zinc-Sensing Receptor GPR39 in Physiology and as a Pharmacological Target |
| title_fullStr | The Zinc-Sensing Receptor GPR39 in Physiology and as a Pharmacological Target |
| title_full_unstemmed | The Zinc-Sensing Receptor GPR39 in Physiology and as a Pharmacological Target |
| title_short | The Zinc-Sensing Receptor GPR39 in Physiology and as a Pharmacological Target |
| title_sort | zinc sensing receptor gpr39 in physiology and as a pharmacological target |
| topic | GPR39 GPR39 agonist zinc zinc signaling |
| url | https://www.mdpi.com/1422-0067/22/8/3872 |
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