一般描述
Potent dual inhibitor of glycolate oxidase and lactate dehydrogenase A, demonstrating strong efficacy in reducing oxalate production and liver fibrosis with minimal toxicity and oral bioavailability.
MDMG-935P is a potent dual, noncompetitive inhibitor of glycolate oxidase (GO) and lactate dehydrogenase A (LDHA), targeting catalytic binding sites with an IC50 of 9 µM for hLDHA and demonstrating robust in vitro oxalate reduction. It selectively modulates key pathways involved in oxalate overproduction and upregulates fatty acid oxidation genes, such as CPT1α, showing significant efficacy in reducing liver triglycerides, oxalate levels, and hepatic fibrosis in MASH mouse models at an oral dose of 10 mg/kg. In vitro, Agxt1−/− mouse hepatocytes are employed to model primary hyperoxaluria, and HEK-293 cells are used to assess cytotoxicity. With its favorable metabolic stability, minimal toxicity, anti-fibrotic properties, and enhanced efficacy, MDMG-935P is an invaluable tool for investigating hyperoxaluria and metabolic liver diseases.
MDMG-935P is a potent dual, noncompetitive inhibitor of glycolate oxidase (GO) and lactate dehydrogenase A (LDHA), targeting catalytic binding sites with an IC50 of 9 µM for hLDHA and demonstrating robust in vitro oxalate reduction. It selectively modulates key pathways involved in oxalate overproduction and upregulates fatty acid oxidation genes, such as CPT1α, showing significant efficacy in reducing liver triglycerides, oxalate levels, and hepatic fibrosis in MASH mouse models at an oral dose of 10 mg/kg. In vitro, Agxt1−/− mouse hepatocytes are employed to model primary hyperoxaluria, and HEK-293 cells are used to assess cytotoxicity. With its favorable metabolic stability, minimal toxicity, anti-fibrotic properties, and enhanced efficacy, MDMG-935P is an invaluable tool for investigating hyperoxaluria and metabolic liver diseases.
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Maria Dolores Moya-Garzon et al.
European journal of medicinal chemistry, 237, 114396-114396 (2022-05-03)
The synthesis and biological evaluation of double glycolate oxidase/lactate dehydrogenase inhibitors containing a salicylic acid moiety is described. The target compounds are obtained in an easily scalable two-step synthetic procedure. These compounds showed low micromolar IC50 values against the two
Sandeep Das et al.
Nature metabolism, 6(10), 1939-1962 (2024-09-28)
The incidence of metabolic dysfunction-associated steatohepatitis (MASH) is on the rise, and with limited pharmacological therapy available, identification of new metabolic targets is urgently needed. Oxalate is a terminal metabolite produced from glyoxylate by hepatic lactate dehydrogenase (LDHA). The liver-specific
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