Artikel ; Online: Development and Characterization of Potent Succinate Receptor Fluorescent Tracers.
Journal of medicinal chemistry
2023 Band 66, Heft 13, Seite(n) 8951–8974
Abstract: The succinate receptor (SUCNR1) has emerged as a potential target for the treatment of various metabolic and inflammatory diseases, including hypertension, inflammatory bowel disease, and rheumatoid arthritis. While several ligands for this receptor have ...
Abstract | The succinate receptor (SUCNR1) has emerged as a potential target for the treatment of various metabolic and inflammatory diseases, including hypertension, inflammatory bowel disease, and rheumatoid arthritis. While several ligands for this receptor have been reported, species differences in pharmacology between human and rodent orthologs have limited the validation of SUCNR1's therapeutic potential. Here, we describe the development of the first potent fluorescent tool compounds for SUCNR1 and use these to define key differences in ligand binding to human and mouse SUCNR1. Starting from known agonist scaffolds, we developed a potent agonist tracer, TUG-2384 ( |
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Mesh-Begriff(e) | Mice ; Humans ; Animals ; Succinic Acid/metabolism ; Receptors, G-Protein-Coupled/metabolism ; Coloring Agents |
Chemische Substanzen | Succinic Acid (AB6MNQ6J6L) ; Receptors, G-Protein-Coupled ; Coloring Agents |
Sprache | Englisch |
Erscheinungsdatum | 2023-06-15 |
Erscheinungsland | United States |
Dokumenttyp | Journal Article ; Research Support, Non-U.S. Gov't |
ZDB-ID | 218133-2 |
ISSN | 1520-4804 ; 0022-2623 |
ISSN (online) | 1520-4804 |
ISSN | 0022-2623 |
DOI | 10.1021/acs.jmedchem.3c00552 |
Datenquelle | MEDical Literature Analysis and Retrieval System OnLINE |
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