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Farnesoid X receptor (FXR) has been previously identified as an important drug target for nonalcoholic steatohepatitis (NASH) and other related diseases, with GW-4064 being the first nonsteroidal FXR agonist used to explore the biological functions of FXR. Scientists at KBP Biosciences Co. Ltd. and Shandong University designed a novel series of FXR agonists as potential candidates for the treatment of NASH.
Eli Lilly & Co. has synthesized glucagon-like peptide 1 receptor (GLP-1R) agonists reported to be useful for the treatment of type 2 diabetes and hyperglycemia.
The positively charged nanoparticle polyamidoamine generation 3 (P-G3) can be specifically targeted to either visceral or subcutaneous fat, and affects both types of fat in different ways, researchers from Columbia University reported in two papers recently published. The studies, published online in Nature Nanotechnology on Dec. 1, 2022, and in Biomaterials on Nov. 28, 2022, are both “a conceptual advance” and “quite amenable to translation,” co-corresponding author Kam Leong told BioWorld.
Chengdu Baiyu Pharmaceutical Co. Ltd. has disclosed NLRP3 inflammasome inhibitors acting as pyroptosis inhibitors reported to be useful for the treatment of gout, Alzheimer's disease, atherosclerosis, diabetes, psoriasis, rheumatoid arthritis, graft-vs.-host disease and familial cold urticaria syndrome.
Steric hindrance and electrostatic interactions often prevent the subsequent development of clinically relevant nanoparticles to the in vivo stage. Researchers at the Shanghai Institute of Materia Medica, Chinese Academy of Sciences, have now demonstrated the development of nanoparticles exhibiting pH-sensitive properties triggering the stretching of peptides to reveal accessible liver-targeted ligands that can deliver biologically active peptides in vivo.
Carmot Therapeutics Inc. has divulged benzimidazoyl compounds acting as glucagon-like peptide 1 receptor (GLP-1R) agonists reported to be useful for the treatment of metabolic diseases.
Leigh syndrome is a rare neurometabolic disorder that causes the CNS to degenerate. Investigators from the University of California, Davis, and Myto Therapeutics Inc. noted that the NDUFS4-knockout (KO) mouse is a well-characterized model for this disease and shared results on the effects of monomethyl fumarate prodrug MYT-109 in this murine model.
Genescience Pharmaceuticals Co. Ltd. has divulged indoline-containing spiro derivatives acting as growth hormone secretagogue receptor (GHSR) agonists reported to be useful for the treatment of growth hormone deficiency.
The liver X receptor (LXR) is a nuclear hormone receptor that is one of the most important regulators of cholesterol homeostasis and plays a key role in triglyceride (TG) regulation. Researchers from Orsobio Inc. and Phenex Pharmaceuticals AG have presented preclinical data on TLC-2716, a potent, small-molecule LXR inverse agonist for the treatment of lipid disorders.
Scientists from Orsobio Inc. and affiliated organizations have described preclinical data for the novel liver-targeted mitochondrial protonophore TLC-6740, being developed for the treatment of metabolic disease. In vitro, mild mitochondrial uncoupling caused by TLC-6740 had pleotropic metabolic benefits in multiple cell lines. TLC-6740 increased mitochondrial potential, oxygen consumption rate and tricarboxylic acid (TCA) cycle flux, and it also inhibited de novo lipogenesis with EC50 values of 6.9 µM.
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