Chemogenomics for steroid hormone receptors (NR3)
Abstract The nine human NR3 nuclear receptors translate steroid hormone signals in transcriptomic responses and operate multiple highly important processes ranging from development over reproductive tissue function to inflammatory and metabolic homeostasis. Although several NR3 ligands such as gluco...
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| Format: | Article |
| Language: | English |
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Nature Portfolio
2025-02-01
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| Series: | Communications Chemistry |
| Online Access: | https://doi.org/10.1038/s42004-025-01427-z |
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| _version_ | 1823863223449812992 |
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| author | Espen Schallmayer Laura Isigkeit Lewis Elson Susanne Müller Stefan Knapp Julian A. Marschner Daniel Merk |
| author_facet | Espen Schallmayer Laura Isigkeit Lewis Elson Susanne Müller Stefan Knapp Julian A. Marschner Daniel Merk |
| author_sort | Espen Schallmayer |
| collection | DOAJ |
| description | Abstract The nine human NR3 nuclear receptors translate steroid hormone signals in transcriptomic responses and operate multiple highly important processes ranging from development over reproductive tissue function to inflammatory and metabolic homeostasis. Although several NR3 ligands such as glucocorticoids are invaluable drugs, this family is only partially explored, for example, in autoimmune diseases and neurodegeneration, but may hold therapeutic potential in new areas. Here we report a chemogenomics (CG) library to reveal elusive effects of NR3 receptor modulation in phenotypic settings. 34 highly annotated and chemically diverse ligands covering all NR3 receptors were selected considering complementary modes of action and activity, selectivity and lack of toxicity. Endoplasmic reticulum stress resolving effects of N3 CG subsets in proof-of-concept application validate suitability of the set to connect phenotypic outcomes with targets and to explore NR3 receptors from a translational perspective. |
| format | Article |
| id | doaj-art-e4f8953323ca44af9c00502b4ca28855 |
| institution | Kabale University |
| issn | 2399-3669 |
| language | English |
| publishDate | 2025-02-01 |
| publisher | Nature Portfolio |
| record_format | Article |
| series | Communications Chemistry |
| spelling | doaj-art-e4f8953323ca44af9c00502b4ca288552025-02-09T12:16:29ZengNature PortfolioCommunications Chemistry2399-36692025-02-018111110.1038/s42004-025-01427-zChemogenomics for steroid hormone receptors (NR3)Espen Schallmayer0Laura Isigkeit1Lewis Elson2Susanne Müller3Stefan Knapp4Julian A. Marschner5Daniel Merk6Institute of Pharmaceutical Chemistry, Goethe-Universität FrankfurtInstitute of Pharmaceutical Chemistry, Goethe-Universität FrankfurtInstitute of Pharmaceutical Chemistry, Goethe-Universität FrankfurtInstitute of Pharmaceutical Chemistry, Goethe-Universität FrankfurtInstitute of Pharmaceutical Chemistry, Goethe-Universität FrankfurtDepartment of Pharmacy, Ludwig-Maximilians-Universität MünchenInstitute of Pharmaceutical Chemistry, Goethe-Universität FrankfurtAbstract The nine human NR3 nuclear receptors translate steroid hormone signals in transcriptomic responses and operate multiple highly important processes ranging from development over reproductive tissue function to inflammatory and metabolic homeostasis. Although several NR3 ligands such as glucocorticoids are invaluable drugs, this family is only partially explored, for example, in autoimmune diseases and neurodegeneration, but may hold therapeutic potential in new areas. Here we report a chemogenomics (CG) library to reveal elusive effects of NR3 receptor modulation in phenotypic settings. 34 highly annotated and chemically diverse ligands covering all NR3 receptors were selected considering complementary modes of action and activity, selectivity and lack of toxicity. Endoplasmic reticulum stress resolving effects of N3 CG subsets in proof-of-concept application validate suitability of the set to connect phenotypic outcomes with targets and to explore NR3 receptors from a translational perspective.https://doi.org/10.1038/s42004-025-01427-z |
| spellingShingle | Espen Schallmayer Laura Isigkeit Lewis Elson Susanne Müller Stefan Knapp Julian A. Marschner Daniel Merk Chemogenomics for steroid hormone receptors (NR3) Communications Chemistry |
| title | Chemogenomics for steroid hormone receptors (NR3) |
| title_full | Chemogenomics for steroid hormone receptors (NR3) |
| title_fullStr | Chemogenomics for steroid hormone receptors (NR3) |
| title_full_unstemmed | Chemogenomics for steroid hormone receptors (NR3) |
| title_short | Chemogenomics for steroid hormone receptors (NR3) |
| title_sort | chemogenomics for steroid hormone receptors nr3 |
| url | https://doi.org/10.1038/s42004-025-01427-z |
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