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What sites on HMG-CoA reductase does Lipitor bind to? HMG-CoA reductase catalyzes the conversion of HMG-CoA to mevalonate, the first committed step in cholesterol synthesis. Lipitor binds directly to the active site of the enzyme, blocking substrate access. Lipitor binds to the HMG-binding portion of the active site through hydrogen bonds and polar interactions with residues Ser565, Lys735, and Glu559.
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