An Atomic-Level Perspective of HMG-CoA-Reductase: The Target Enzyme to Treat Hypercholesterolemia
1
UCIBIO, Departamento de Química, Faculdade de Ciências e Tecnologia, Universidade Nova de Lisboa, 2829-516 Caparica, Portugal
2
UCIBIO/REQUIMTE, BioSIM, Departamento de Biomedicina, Faculdade de Medicina da Universidade do Porto, Alameda Prof. Hernâni Monteiro, 4200-319 Porto, Portugal
*
Author to whom correspondence should be addressed.
Academic Editor: Pierluigi Plastina
Molecules 2020, 25(17), 3891; https://doi.org/10.3390/molecules25173891
Received: 31 July 2020 / Revised: 23 August 2020 / Accepted: 24 August 2020 / Published: 26 August 2020
(This article belongs to the Special Issue Lipids in Health and Disease)
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.
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Keywords:
HMG-CoAR; structure; biochemistry; regulation; statins; dimerization inhibitors.
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited
MDPI and ACS Style
Gesto, D.S.; Pereira, C.M.S.; Cerqueira, N.M.F.S.; Sousa, S.F. An Atomic-Level Perspective of HMG-CoA-Reductase: The Target Enzyme to Treat Hypercholesterolemia. Molecules 2020, 25, 3891. https://doi.org/10.3390/molecules25173891
AMA Style
Gesto DS, Pereira CMS, Cerqueira NMFS, Sousa SF. An Atomic-Level Perspective of HMG-CoA-Reductase: The Target Enzyme to Treat Hypercholesterolemia. Molecules. 2020; 25(17):3891. https://doi.org/10.3390/molecules25173891
Chicago/Turabian StyleGesto, Diana S.; Pereira, Carlos M.S.; Cerqueira, Nuno M.F.S.; Sousa, Sérgio F. 2020. "An Atomic-Level Perspective of HMG-CoA-Reductase: The Target Enzyme to Treat Hypercholesterolemia" Molecules 25, no. 17: 3891. https://doi.org/10.3390/molecules25173891
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