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. 2011 Aug 15;204(4):609–616. doi: 10.1093/infdis/jir303

Figure 3.

Figure 3.

Ceestatin inhibits 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) synthase. A, HMG-CoA synthase assay, demonstrating dose-dependent inhibition of enzymatic activity by ceestatin. The IC50 of ceestatin is ∼2 μmol/L. Maximum enzymatic inhibition is achieved by ceestatin at 5 μmol/L. B, Ceestatin (SM_A14B5) inhibits recombinant human HMG-CoA synthase in an irreversible fashion, with a t½ of ∼61 minutes. SM_A6B5_P200 is the parent compound from which ceestatin was derived [9]. It also demonstrates irreversible inhibition of HMG-CoA synthase. Cerulenin is a known powerful irreversible inhibitor of HMG-CoA synthase.