An atomic-level perspective of HMG-CoA-reductase: The target enzyme to treat hypercholesterolemia

Diana S. Gesto, Carlos M. S. Pereira, Nuno M. F. S. Cerqueira, Sérgio F. Sousa

Research output: Contribution to journalReview articlepeer-review

4 Citations (Scopus)


This review provides an updated atomic-level perspective regarding the enzyme 3-hydroxy-3-methylglutaryl coenzyme A reductase (HMG-CoAR), linking the more recent data on this enzyme with a structure/function interpretation. This enzyme catalyzes one of the most important steps in cholesterol biosynthesis and is regarded as one of the most important drug targets in the treatment of hypercholesterolemia. Taking this into consideration, we review in the present article several aspects of this enzyme, including its structure and biochemistry, its catalytic mechanism and different reported and proposed approaches for inhibiting this enzyme, including the commercially available statins or the possibility of using dimerization inhibitors.

Original languageEnglish
Article number3891
Issue number17
Publication statusPublished - Sep 2020


  • Biochemistry
  • Dimerization inhibitors
  • HMG-CoAR
  • Regulation
  • Statins
  • Structure


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