G protein-coupled receptors and obesity
G protein-coupled receptors (GPCRs) have emerged as important drug targets for various chronic diseases, including obesity and diabetes. Obesity is a complex chronic disease that requires long term management predisposing to type 2 diabetes, heart disease, and some cancers. The therapeutic landscape...
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| Format: | Article |
| Language: | English |
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Frontiers Media S.A.
2023-12-01
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| Series: | Frontiers in Endocrinology |
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| Online Access: | https://www.frontiersin.org/articles/10.3389/fendo.2023.1301017/full |
| _version_ | 1797390977665597440 |
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| author | Alessandro Pocai |
| author_facet | Alessandro Pocai |
| author_sort | Alessandro Pocai |
| collection | DOAJ |
| description | G protein-coupled receptors (GPCRs) have emerged as important drug targets for various chronic diseases, including obesity and diabetes. Obesity is a complex chronic disease that requires long term management predisposing to type 2 diabetes, heart disease, and some cancers. The therapeutic landscape for GPCR as targets of anti-obesity medications has undergone significant changes with the approval of semaglutide, the first peptide glucagon like peptide 1 receptor agonist (GLP-1RA) achieving double digit weight loss (≥10%) and cardiovascular benefits. The enhanced weight loss, with the expected beneficial effect on obesity-related complications and reduction of major adverse cardiovascular events (MACE), has propelled the commercial opportunity for the obesity market leading to new players entering the space. Significant progress has been made on approaches targeting GPCRs such as single peptides that simultaneously activate GIP and/or GCGR in addition to GLP1, oral tablet formulation of GLP-1, small molecules nonpeptidic oral GLP1R and fixed-dose combination as well as add-on therapy for patients already treated with a GLP-1 agonist. |
| first_indexed | 2024-03-08T23:25:12Z |
| format | Article |
| id | doaj.art-d0cbfd0f641b40d88f4bbd381a7c6362 |
| institution | Directory Open Access Journal |
| issn | 1664-2392 |
| language | English |
| last_indexed | 2024-03-08T23:25:12Z |
| publishDate | 2023-12-01 |
| publisher | Frontiers Media S.A. |
| record_format | Article |
| series | Frontiers in Endocrinology |
| spelling | doaj.art-d0cbfd0f641b40d88f4bbd381a7c63622023-12-14T17:24:11ZengFrontiers Media S.A.Frontiers in Endocrinology1664-23922023-12-011410.3389/fendo.2023.13010171301017G protein-coupled receptors and obesityAlessandro PocaiG protein-coupled receptors (GPCRs) have emerged as important drug targets for various chronic diseases, including obesity and diabetes. Obesity is a complex chronic disease that requires long term management predisposing to type 2 diabetes, heart disease, and some cancers. The therapeutic landscape for GPCR as targets of anti-obesity medications has undergone significant changes with the approval of semaglutide, the first peptide glucagon like peptide 1 receptor agonist (GLP-1RA) achieving double digit weight loss (≥10%) and cardiovascular benefits. The enhanced weight loss, with the expected beneficial effect on obesity-related complications and reduction of major adverse cardiovascular events (MACE), has propelled the commercial opportunity for the obesity market leading to new players entering the space. Significant progress has been made on approaches targeting GPCRs such as single peptides that simultaneously activate GIP and/or GCGR in addition to GLP1, oral tablet formulation of GLP-1, small molecules nonpeptidic oral GLP1R and fixed-dose combination as well as add-on therapy for patients already treated with a GLP-1 agonist.https://www.frontiersin.org/articles/10.3389/fendo.2023.1301017/fullGLP-1GIPsemaglutidetirzepatideglucagonamylin |
| spellingShingle | Alessandro Pocai G protein-coupled receptors and obesity Frontiers in Endocrinology GLP-1 GIP semaglutide tirzepatide glucagon amylin |
| title | G protein-coupled receptors and obesity |
| title_full | G protein-coupled receptors and obesity |
| title_fullStr | G protein-coupled receptors and obesity |
| title_full_unstemmed | G protein-coupled receptors and obesity |
| title_short | G protein-coupled receptors and obesity |
| title_sort | g protein coupled receptors and obesity |
| topic | GLP-1 GIP semaglutide tirzepatide glucagon amylin |
| url | https://www.frontiersin.org/articles/10.3389/fendo.2023.1301017/full |
| work_keys_str_mv | AT alessandropocai gproteincoupledreceptorsandobesity |