Allosteric modulation of gonadotropin receptors
Gonadotropins regulate reproductive functions by binding to G protein-coupled receptors (FSHR and LHCGR) expressed in the gonads. They activate multiple, cell-specific signalling pathways, consisting of ligand-dependent intracellular events. Signalling cascades may be modulated by synthetic compound...
| Main Authors: | , , , |
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| Format: | Article |
| Language: | English |
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Frontiers Media S.A.
2023-05-01
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| Series: | Frontiers in Endocrinology |
| Subjects: | |
| Online Access: | https://www.frontiersin.org/articles/10.3389/fendo.2023.1179079/full |
| _version_ | 1827941528482349056 |
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| author | Clara Lazzaretti Manuela Simoni Manuela Simoni Manuela Simoni Livio Casarini Livio Casarini Elia Paradiso |
| author_facet | Clara Lazzaretti Manuela Simoni Manuela Simoni Manuela Simoni Livio Casarini Livio Casarini Elia Paradiso |
| author_sort | Clara Lazzaretti |
| collection | DOAJ |
| description | Gonadotropins regulate reproductive functions by binding to G protein-coupled receptors (FSHR and LHCGR) expressed in the gonads. They activate multiple, cell-specific signalling pathways, consisting of ligand-dependent intracellular events. Signalling cascades may be modulated by synthetic compounds which bind allosteric sites of FSHR and LHCGR or by membrane receptor interactions. Despite the hormone binding to the orthosteric site, allosteric ligands, and receptor heteromerizations may reshape intracellular signalling pattern. These molecules act as positive, negative, or neutral allosteric modulators, as well as non-competitive or inverse agonist ligands, providing a set of new compounds of a different nature and with unique pharmacological characteristics. Gonadotropin receptor allosteric modulation is gathering increasing interest from the scientific community and may be potentially exploited for clinical purposes. This review summarizes the current knowledge on gonadotropin receptor allosteric modulation and their potential, clinical use. |
| first_indexed | 2024-03-13T09:39:39Z |
| format | Article |
| id | doaj.art-89d2fefed892427aa8eaf8028228c8cf |
| institution | Directory Open Access Journal |
| issn | 1664-2392 |
| language | English |
| last_indexed | 2024-03-13T09:39:39Z |
| publishDate | 2023-05-01 |
| publisher | Frontiers Media S.A. |
| record_format | Article |
| series | Frontiers in Endocrinology |
| spelling | doaj.art-89d2fefed892427aa8eaf8028228c8cf2023-05-25T04:54:01ZengFrontiers Media S.A.Frontiers in Endocrinology1664-23922023-05-011410.3389/fendo.2023.11790791179079Allosteric modulation of gonadotropin receptorsClara Lazzaretti0Manuela Simoni1Manuela Simoni2Manuela Simoni3Livio Casarini4Livio Casarini5Elia Paradiso6Unit of Endocrinology, Department of Biomedical, Metabolic and Neural Sciences, Baggiovara Hospital, University of Modena and Reggio Emilia, Modena, ItalyUnit of Endocrinology, Department of Biomedical, Metabolic and Neural Sciences, Baggiovara Hospital, University of Modena and Reggio Emilia, Modena, ItalyCenter for Genomic Research, University of Modena and Reggio Emilia, Modena, ItalyDepartment of Medical Specialties, Azienda Ospedaliero-Universitaria di Modena, Baggiovara Hospital, Modena, ItalyUnit of Endocrinology, Department of Biomedical, Metabolic and Neural Sciences, Baggiovara Hospital, University of Modena and Reggio Emilia, Modena, ItalyCenter for Genomic Research, University of Modena and Reggio Emilia, Modena, ItalyUnit of Endocrinology, Department of Biomedical, Metabolic and Neural Sciences, Baggiovara Hospital, University of Modena and Reggio Emilia, Modena, ItalyGonadotropins regulate reproductive functions by binding to G protein-coupled receptors (FSHR and LHCGR) expressed in the gonads. They activate multiple, cell-specific signalling pathways, consisting of ligand-dependent intracellular events. Signalling cascades may be modulated by synthetic compounds which bind allosteric sites of FSHR and LHCGR or by membrane receptor interactions. Despite the hormone binding to the orthosteric site, allosteric ligands, and receptor heteromerizations may reshape intracellular signalling pattern. These molecules act as positive, negative, or neutral allosteric modulators, as well as non-competitive or inverse agonist ligands, providing a set of new compounds of a different nature and with unique pharmacological characteristics. Gonadotropin receptor allosteric modulation is gathering increasing interest from the scientific community and may be potentially exploited for clinical purposes. This review summarizes the current knowledge on gonadotropin receptor allosteric modulation and their potential, clinical use.https://www.frontiersin.org/articles/10.3389/fendo.2023.1179079/fullFSHRLHCGRallosteric modulatorsgonadotropinsbiased signalling |
| spellingShingle | Clara Lazzaretti Manuela Simoni Manuela Simoni Manuela Simoni Livio Casarini Livio Casarini Elia Paradiso Allosteric modulation of gonadotropin receptors Frontiers in Endocrinology FSHR LHCGR allosteric modulators gonadotropins biased signalling |
| title | Allosteric modulation of gonadotropin receptors |
| title_full | Allosteric modulation of gonadotropin receptors |
| title_fullStr | Allosteric modulation of gonadotropin receptors |
| title_full_unstemmed | Allosteric modulation of gonadotropin receptors |
| title_short | Allosteric modulation of gonadotropin receptors |
| title_sort | allosteric modulation of gonadotropin receptors |
| topic | FSHR LHCGR allosteric modulators gonadotropins biased signalling |
| url | https://www.frontiersin.org/articles/10.3389/fendo.2023.1179079/full |
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