Description
Hymeglusin (29066-42-0) is an inhibitor of eukaryotic mevalonate biosynthesis via inhibition of HMG-CoA synthase, IC50=0.12 μM.1 Acts via covalent modification of the active site Cys129.1,2 Inhibits cholesterol biosynthesis in rats (45% at 25 mg/Kg).1 Also inhibits bacterial HMG-CoA synthase.3 Inhibits dengue virus replication.4
References
[1] M D GREENSPAN. Inhibition of hydroxymethylglutaryl-coenzyme A synthase by L-659,699.[J]. Proceedings of the National Academy of Sciences of the United States of America, 1987, 84 21: 7488-7492. DOI:
10.1073/pnas.84.21.7488[2] HIROSHI TOMODA. Binding site for fungal β-lactone hymeglusin on cytosolic 3-hydroxy-3-methylglutaryl coenzyme A synthase[J]. Biochimica et biophysica acta. Molecular and cell biology of lipids, 2004, 1636 1: Pages 22-28. DOI:
10.1016/j.bbalip.2003.11.005[3] D. ANDREW SKAFF. Biochemical and Structural Basis for Inhibition of Enterococcus faecalis Hydroxymethylglutaryl-CoA Synthase, mvaS, by Hymeglusin[J]. Biochemistry Biochemistry, 2012, 51 23: 4713-4722. DOI:
10.1021/bi300037k[4] CHRISTOPHER ROTHWELL . Cholesterol biosynthesis modulation regulates dengue viral replication[J]. Virology, 2009, 389 1: Pages 8-19. DOI:
10.1016/j.virol.2009.03.025
