Selective novel inverse agonists for human GPR43 augment GLP-1 secretion.
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Summary
It is demonstrated that a novel compound of pyrimidinecarboxamide class named as BTI-A-404 is a selective and potent competitive inverse agonist of human GPR43, but not the murine ortholog.
- Type
- article
- Published
- 2016-01-15
- Cited by
- 42
- References
- 39
- OpenAlex
- https://openalex.org/W26683635
- Semantic Scholar
- https://api.semanticscholar.org/CorpusID:12079671
Keywords
Political science, Computer science
References
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Cited by
- Key Questions for Translation of FFA Receptors: From Pharmacology to Medicines.
- Gastrointestinal Defense Mechanisms
- From gut dysbiosis to altered brain function and mental illness: mechanisms and pathways
- Complex Pharmacology of Free Fatty Acid Receptors.
- A Novel Allosteric Activator of Free Fatty Acid 2 Receptor Displays Unique Gi-functional Bias
- FFA2 and FFA3 in Metabolic Regulation.
- Ligands at the Free Fatty Acid Receptors 2/3 (GPR43/GPR41).
- Divergent Relationships between Fecal Microbiota and Metabolome following Distinct Antibiotic-Induced Disruptions
- FFAR2-FFAR3 receptor heteromerization modulates short-chain fatty acid sensing
- The impact of short-chain fatty acids on GLP-1 and PYY secretion from the isolated perfused rat colon.
- Investigating the molecular pharmacology of the short chain fatty acid receptor FFA2
- Effects of Obesity and Gastric Bypass Surgery on Nutrient Sensors, Endocrine Cells, and Mucosal Innervation of the Mouse Colon
- Dissecting the Physiology and Pathophysiology of Glucagon-Like Peptide-1
- Intestinal Sensing by Gut Microbiota: Targeting Gut Peptides
- GPCRs and Insulin Receptor Signaling in Conversation: Novel Avenues for Drug Discovery.
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- Free Fatty Acid Receptors as new potential therapeutic target in Inflammatory Bowel Diseases.
- GPR43 regulates HBV X protein (HBx)-induced inflammatory response in human LO2 hepatocytes.
- Activation of GPR43 suppresses TNF-α-induced inflammatory response in human fibroblast-like synoviocytes.
- FFAR2/3 as Microbial Metabolite Sensors to Shape Host Health: Pharmacophysiological View
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