GPCRs: The most promiscuous druggable receptor of the mankind
All physiological events in living organisms originated as specific chemical/biochemical signals on the cell surface and transmitted into the cytoplasm. This signal is translated within milliseconds–hours to a specific and unique order required to maintain optimum performance and homeostasis of livi...
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| Format: | Article |
| Language: | English |
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Springer
2021-06-01
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| Series: | Saudi Pharmaceutical Journal |
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| Online Access: | http://www.sciencedirect.com/science/article/pii/S1319016421000724 |
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| author | Khaled Alhosaini Asim Azhar Asma Alonazi F Al-Zoghaibi |
| author_facet | Khaled Alhosaini Asim Azhar Asma Alonazi F Al-Zoghaibi |
| author_sort | Khaled Alhosaini |
| collection | DOAJ |
| description | All physiological events in living organisms originated as specific chemical/biochemical signals on the cell surface and transmitted into the cytoplasm. This signal is translated within milliseconds–hours to a specific and unique order required to maintain optimum performance and homeostasis of living organisms. Examples of daily biological functions include neuronal communication and neurotransmission in the process of learning and memory, secretion (hormones, sweat, and saliva), muscle contraction, cellular growth, differentiation and migration during wound healing, and immunity to fight infections. Among the different transducers for such life-dependent signals is the large family of G protein-coupled receptors (GPCRs). GPCRs constitute roughly 800 genes, corresponding to 2% of the human genome. While GPCRs control a plethora of pathophysiological disorders, only approximately one-third of GPCR families have been deorphanized and characterized. Recent drug data show that around 40% of the recommended drugs available in the market target mainly GPCRs. In this review, we presented how such system signals, either through G protein or via other players, independent of G protein, function within the biological system. We also discussed drugs in the market or clinical trials targeting mainly GPCRs in various diseases, including cancer. |
| format | Article |
| id | doaj-art-407845beffc343f69e60f6a68e734ff7 |
| institution | Kabale University |
| issn | 1319-0164 |
| language | English |
| publishDate | 2021-06-01 |
| publisher | Springer |
| record_format | Article |
| series | Saudi Pharmaceutical Journal |
| spelling | doaj-art-407845beffc343f69e60f6a68e734ff72025-08-20T03:55:36ZengSpringerSaudi Pharmaceutical Journal1319-01642021-06-0129653955110.1016/j.jsps.2021.04.015GPCRs: The most promiscuous druggable receptor of the mankindKhaled Alhosaini0Asim Azhar1Asma Alonazi2F Al-Zoghaibi3Department of Pharmacology & Toxicology, College of Pharmacy, King Saud University, Post Box 2457, Riyadh 11451, Saudi Arabia; Corresponding author.Interdisciplinary Biotechnology Unit, AMU Aligarh, UP, IndiaDepartment of Pharmacology & Toxicology, College of Pharmacy, King Saud University, Post Box 2457, Riyadh 11451, Saudi ArabiaMolecular BioMedicine Program, Research Centre, King Faisal Specialist Hospital and Research Centre, P.O.Box: 3354, MBC:03, Riyadh 11211, Saudi ArabiaAll physiological events in living organisms originated as specific chemical/biochemical signals on the cell surface and transmitted into the cytoplasm. This signal is translated within milliseconds–hours to a specific and unique order required to maintain optimum performance and homeostasis of living organisms. Examples of daily biological functions include neuronal communication and neurotransmission in the process of learning and memory, secretion (hormones, sweat, and saliva), muscle contraction, cellular growth, differentiation and migration during wound healing, and immunity to fight infections. Among the different transducers for such life-dependent signals is the large family of G protein-coupled receptors (GPCRs). GPCRs constitute roughly 800 genes, corresponding to 2% of the human genome. While GPCRs control a plethora of pathophysiological disorders, only approximately one-third of GPCR families have been deorphanized and characterized. Recent drug data show that around 40% of the recommended drugs available in the market target mainly GPCRs. In this review, we presented how such system signals, either through G protein or via other players, independent of G protein, function within the biological system. We also discussed drugs in the market or clinical trials targeting mainly GPCRs in various diseases, including cancer.http://www.sciencedirect.com/science/article/pii/S1319016421000724ArrestinDrugsG proteinsGPCRGRKsHeterodimerization |
| spellingShingle | Khaled Alhosaini Asim Azhar Asma Alonazi F Al-Zoghaibi GPCRs: The most promiscuous druggable receptor of the mankind Saudi Pharmaceutical Journal Arrestin Drugs G proteins GPCR GRKs Heterodimerization |
| title | GPCRs: The most promiscuous druggable receptor of the mankind |
| title_full | GPCRs: The most promiscuous druggable receptor of the mankind |
| title_fullStr | GPCRs: The most promiscuous druggable receptor of the mankind |
| title_full_unstemmed | GPCRs: The most promiscuous druggable receptor of the mankind |
| title_short | GPCRs: The most promiscuous druggable receptor of the mankind |
| title_sort | gpcrs the most promiscuous druggable receptor of the mankind |
| topic | Arrestin Drugs G proteins GPCR GRKs Heterodimerization |
| url | http://www.sciencedirect.com/science/article/pii/S1319016421000724 |
| work_keys_str_mv | AT khaledalhosaini gpcrsthemostpromiscuousdruggablereceptorofthemankind AT asimazhar gpcrsthemostpromiscuousdruggablereceptorofthemankind AT asmaalonazi gpcrsthemostpromiscuousdruggablereceptorofthemankind AT falzoghaibi gpcrsthemostpromiscuousdruggablereceptorofthemankind |