GPCRs Are Optimal Regulators of Complex Biological Systems and Orchestrate the Interface between Health and Disease
GPCRs arguably represent the most effective current therapeutic targets for a plethora of diseases. GPCRs also possess a pivotal role in the regulation of the physiological balance between healthy and pathological conditions; thus, their importance in systems biology cannot be underestimated. The mo...
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| Format: | Article |
| Language: | English |
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MDPI AG
2021-12-01
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| Series: | International Journal of Molecular Sciences |
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| Online Access: | https://www.mdpi.com/1422-0067/22/24/13387 |
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| author | Hanne Leysen Deborah Walter Bregje Christiaenssen Romi Vandoren İrem Harputluoğlu Nore Van Loon Stuart Maudsley |
| author_facet | Hanne Leysen Deborah Walter Bregje Christiaenssen Romi Vandoren İrem Harputluoğlu Nore Van Loon Stuart Maudsley |
| author_sort | Hanne Leysen |
| collection | DOAJ |
| description | GPCRs arguably represent the most effective current therapeutic targets for a plethora of diseases. GPCRs also possess a pivotal role in the regulation of the physiological balance between healthy and pathological conditions; thus, their importance in systems biology cannot be underestimated. The molecular diversity of GPCR signaling systems is likely to be closely associated with disease-associated changes in organismal tissue complexity and compartmentalization, thus enabling a nuanced GPCR-based capacity to interdict multiple disease pathomechanisms at a systemic level. GPCRs have been long considered as controllers of communication between tissues and cells. This communication involves the ligand-mediated control of cell surface receptors that then direct their stimuli to impact cell physiology. Given the tremendous success of GPCRs as therapeutic targets, considerable focus has been placed on the ability of these therapeutics to modulate diseases by acting at cell surface receptors. In the past decade, however, attention has focused upon how stable multiprotein GPCR superstructures, termed receptorsomes, both at the cell surface membrane and in the intracellular domain dictate and condition long-term GPCR activities associated with the regulation of protein expression patterns, cellular stress responses and DNA integrity management. The ability of these receptorsomes (often in the absence of typical cell surface ligands) to control complex cellular activities implicates them as key controllers of the functional balance between health and disease. A greater understanding of this function of GPCRs is likely to significantly augment our ability to further employ these proteins in a multitude of diseases. |
| first_indexed | 2024-03-10T03:56:16Z |
| format | Article |
| id | doaj.art-1236550d1b8744dfb0f3fabace5a95b0 |
| institution | Directory Open Access Journal |
| issn | 1661-6596 1422-0067 |
| language | English |
| last_indexed | 2024-03-10T03:56:16Z |
| publishDate | 2021-12-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | International Journal of Molecular Sciences |
| spelling | doaj.art-1236550d1b8744dfb0f3fabace5a95b02023-11-23T08:45:35ZengMDPI AGInternational Journal of Molecular Sciences1661-65961422-00672021-12-0122241338710.3390/ijms222413387GPCRs Are Optimal Regulators of Complex Biological Systems and Orchestrate the Interface between Health and DiseaseHanne Leysen0Deborah Walter1Bregje Christiaenssen2Romi Vandoren3İrem Harputluoğlu4Nore Van Loon5Stuart Maudsley6Receptor Biology Lab, University of Antwerp, 2610 Wilrijk, BelgiumReceptor Biology Lab, University of Antwerp, 2610 Wilrijk, BelgiumReceptor Biology Lab, University of Antwerp, 2610 Wilrijk, BelgiumReceptor Biology Lab, University of Antwerp, 2610 Wilrijk, BelgiumReceptor Biology Lab, University of Antwerp, 2610 Wilrijk, BelgiumReceptor Biology Lab, University of Antwerp, 2610 Wilrijk, BelgiumReceptor Biology Lab, University of Antwerp, 2610 Wilrijk, BelgiumGPCRs arguably represent the most effective current therapeutic targets for a plethora of diseases. GPCRs also possess a pivotal role in the regulation of the physiological balance between healthy and pathological conditions; thus, their importance in systems biology cannot be underestimated. The molecular diversity of GPCR signaling systems is likely to be closely associated with disease-associated changes in organismal tissue complexity and compartmentalization, thus enabling a nuanced GPCR-based capacity to interdict multiple disease pathomechanisms at a systemic level. GPCRs have been long considered as controllers of communication between tissues and cells. This communication involves the ligand-mediated control of cell surface receptors that then direct their stimuli to impact cell physiology. Given the tremendous success of GPCRs as therapeutic targets, considerable focus has been placed on the ability of these therapeutics to modulate diseases by acting at cell surface receptors. In the past decade, however, attention has focused upon how stable multiprotein GPCR superstructures, termed receptorsomes, both at the cell surface membrane and in the intracellular domain dictate and condition long-term GPCR activities associated with the regulation of protein expression patterns, cellular stress responses and DNA integrity management. The ability of these receptorsomes (often in the absence of typical cell surface ligands) to control complex cellular activities implicates them as key controllers of the functional balance between health and disease. A greater understanding of this function of GPCRs is likely to significantly augment our ability to further employ these proteins in a multitude of diseases.https://www.mdpi.com/1422-0067/22/24/13387dimensionalityG protein-coupled receptornetworkpharmacologyprecisionquantitative |
| spellingShingle | Hanne Leysen Deborah Walter Bregje Christiaenssen Romi Vandoren İrem Harputluoğlu Nore Van Loon Stuart Maudsley GPCRs Are Optimal Regulators of Complex Biological Systems and Orchestrate the Interface between Health and Disease International Journal of Molecular Sciences dimensionality G protein-coupled receptor network pharmacology precision quantitative |
| title | GPCRs Are Optimal Regulators of Complex Biological Systems and Orchestrate the Interface between Health and Disease |
| title_full | GPCRs Are Optimal Regulators of Complex Biological Systems and Orchestrate the Interface between Health and Disease |
| title_fullStr | GPCRs Are Optimal Regulators of Complex Biological Systems and Orchestrate the Interface between Health and Disease |
| title_full_unstemmed | GPCRs Are Optimal Regulators of Complex Biological Systems and Orchestrate the Interface between Health and Disease |
| title_short | GPCRs Are Optimal Regulators of Complex Biological Systems and Orchestrate the Interface between Health and Disease |
| title_sort | gpcrs are optimal regulators of complex biological systems and orchestrate the interface between health and disease |
| topic | dimensionality G protein-coupled receptor network pharmacology precision quantitative |
| url | https://www.mdpi.com/1422-0067/22/24/13387 |
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