Structural Mechanism for Statin Inhibition of HMG-CoA Reductase

@article{Istvan2001StructuralMF,
  title={Structural Mechanism for Statin Inhibition of HMG-CoA Reductase},
  author={Eva S. Istvan and Johann Deisenhofer},
  journal={Science},
  year={2001},
  volume={292},
  pages={1160 - 1164}
}
  • Eva S. Istvan, Johann Deisenhofer
  • Published 2001
  • Medicine, Chemistry
  • Science
  • HMG-CoA (3-hydroxy-3-methylglutaryl–coenzyme A) reductase (HMGR) catalyzes the committed step in cholesterol biosynthesis. Statins are HMGR inhibitors with inhibition constant values in the nanomolar range that effectively lower serum cholesterol levels and are widely prescribed in the treatment of hypercholesterolemia. We have determined structures of the catalytic portion of human HMGR complexed with six different statins. The statins occupy a portion of the binding site of HMG-CoA, thus… CONTINUE READING

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