gft505 has been researched along with Disease-Models--Animal* in 2 studies
2 other study(ies) available for gft505 and Disease-Models--Animal
| Article | Year |
|---|---|
Design, synthesis, and biological evaluation of a novel dual peroxisome proliferator-activated receptor alpha/delta agonist for the treatment of diabetic kidney disease through anti-inflammatory mechanisms.
Topics: Animals; Anti-Inflammatory Agents, Non-Steroidal; Cell Survival; Cells, Cultured; Diabetes Mellitus, Experimental; Diabetic Nephropathies; Disease Models, Animal; Dose-Response Relationship, Drug; Drug Design; Humans; Hypoglycemic Agents; Male; Molecular Structure; NF-kappa B; PPAR alpha; PPAR gamma; Rats; Rats, Sprague-Dawley; Streptozocin; Structure-Activity Relationship | 2021 |
Discovery of chalcone analogues as novel NLRP3 inflammasome inhibitors with potent anti-inflammation activities.
NLRP3 inflammasome activation plays a critical role in inflammation and its related disorders. Herein we report a hit-to-lead effort resulting in the discovery of a novel and potent class of NLRP3 inflammasome inhibitors. Among these, the most potent lead 40 exhibited improved inhibitory potency and almost no toxicity. Further mechanistic study indicated that compound 40 inhibited the NLRP3 inflammasome activation via suppressing ROS production. More importantly, treatment with 40 showed remarkable therapeutic effects on LPS-induced sepsis and DSS-induced colitis. This study encourages further development of more potent inhibitors based on this chemical scaffold and provides a chemical tool to identify its cellular binding target. Topics: Animals; Anti-Inflammatory Agents; Cell Line; Chalcones; Colitis; Disease Models, Animal; Drug Design; Female; Inflammasomes; Lipopolysaccharides; Macrophages; Male; Mice; Mice, Inbred C57BL; NLR Family, Pyrin Domain-Containing 3 Protein; Pyroptosis; Reactive Oxygen Species; Sepsis; Structure-Activity Relationship | 2021 |