bms-309403 has been researched along with Inflammation* in 2 studies
2 other study(ies) available for bms-309403 and Inflammation
| Article | Year |
|---|---|
Exploration of Fragment Binding Poses Leading to Efficient Discovery of Highly Potent and Orally Effective Inhibitors of FABP4 for Anti-inflammation.
Fatty-acid binding protein 4 (FABP4) is a promising therapeutic target for immunometabolic diseases, while its potential for systemic inflammatory response syndrome treatment has not been explored. Here, a series of 2-(phenylamino)benzoic acids as novel and potent FABP4 inhibitors are rationally designed based on an interesting fragment that adopts multiple binding poses within FABP4. A fusion of these binding poses leads to the design of compound Topics: 3T3 Cells; Administration, Oral; Animals; Anti-Inflammatory Agents; Biphenyl Compounds; Caco-2 Cells; Dose-Response Relationship, Drug; Drug Discovery; Fatty Acid-Binding Proteins; Humans; Inflammation; Male; Mice; Mice, Inbred C57BL; Mice, Inbred ICR; Protein Binding; Protein Structure, Secondary; Protein Structure, Tertiary; Pyrazoles; Treatment Outcome | 2020 |
Treatment of diabetes and atherosclerosis by inhibiting fatty-acid-binding protein aP2.
Adipocyte fatty-acid-binding protein, aP2 (FABP4) is expressed in adipocytes and macrophages, and integrates inflammatory and metabolic responses. Studies in aP2-deficient mice have shown that this lipid chaperone has a significant role in several aspects of metabolic syndrome, including type 2 diabetes and atherosclerosis. Here we demonstrate that an orally active small-molecule inhibitor of aP2 is an effective therapeutic agent against severe atherosclerosis and type 2 diabetes in mouse models. In macrophage and adipocyte cell lines with or without aP2, we also show the target specificity of this chemical intervention and its mechanisms of action on metabolic and inflammatory pathways. Our findings demonstrate that targeting aP2 with small-molecule inhibitors is possible and can lead to a new class of powerful therapeutic agents to prevent and treat metabolic diseases such as type 2 diabetes and atherosclerosis. Topics: Adipocytes; Adipose Tissue; Animals; Apolipoproteins E; Atherosclerosis; Biphenyl Compounds; Cell Line; Cholesterol; Diabetes Mellitus; Fatty Acid-Binding Proteins; Humans; Inflammation; Liver; Macrophages; Mice; Mice, Inbred C57BL; Mice, Mutant Strains; Models, Biological; Obesity; Pyrazoles | 2007 |