Researchers at the Gwangju Institute of Science and Technology Discover a Novel Drug Candidate to Combat Fatty Liver Disease. Metabolic dysfunction-associated steatotic liver disease is a significant global health concern, burdening healthcare systems and jeopardizing public health.
It is characterized by the accumulation of fat in the liver, which can progress to more severe conditions like metabolic dysfunction-associated steatohepatitis (MASH), characterized by inflammation, ballooning, and potential fibrosis.
Obesity-related MASH is a leading cause of liver transplantation, underscoring the importance of identifying effective treatments.
Compound 11c, developed by the Gwangju Institute of Science and Technology (GIST), is a novel peripheral 5HT2A antagonist with promising therapeutic potential.
The journey from drug library screening to compound refinement involved identifying Desloratadine, a promising peripheral agent, and using molecular docking techniques to transform it into the potent compound 11c.
Published in Nature Communications, the research highlights 11c's efficacy in preclinical models, demonstrating robust biological activity and a favorable safety profile, particularly in reducing inflammatory and fibrosis markers.
The journey from drug library screening to compound refinement involved leveraging Desloratadine and molecular docking techniques.
With its excellent safety attributes, including stability, low toxicity, and minimal inhibition of cytochrome P450, along with high oral bioavailability, compound 11c emerges as a compelling candidate for advancing MASH therapy.
