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Design, synthesis, ...
Design, synthesis, and docking of highly hypolipidemic agents: Schizosaccharomyces pombe as a new model for evaluating α-asarone-based HMG-CoA reductase inhibitors
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Argüelles, Nancy (author)
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- Sánchez-Sandoval, Maria E. (author)
- Gothenburg University,Göteborgs universitet,Core Facilities, Bioinformatics,Core Facilities, Bioinformatics
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Mendieta, Aarón (author)
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Villa-Tanaca, Lourdes (author)
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Garduño-Siciliano, Leticia (author)
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Jiménez, Fabiola (author)
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Cruz, María del Carmen (author)
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Medina-Franco, José L. (author)
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Chamorro-Cevallos, Germán (author)
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Tamariz, Joaquín (author)
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(creator_code:org_t)
- Elsevier BV, 2010
- 2010
- English.
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In: Bioorganic and Medicinal Chemistry. - : Elsevier BV. - 0968-0896. ; 18, s. 4238-4248
- Related links:
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https://gup.ub.gu.se...
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https://doi.org/10.1...
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Abstract
Subject headings
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- A series of α-asarone-based analogues was designed by conducting docking experiments with published crystal structures of human HMG-CoA reductase. Indeed, synthesis and evaluation of this series showed a highly hypocholesterolemic in vivo activity in a murine model, as predicted by previous docking studies. In agreement with this model, the polar groups attached to the benzene ring could play a key role in the enzyme binding and probably also in its biological activity, mimicking the HMG-moiety of the natural substrate. The hypolipidemic action mechanism of these compounds was investigated by developing a simple, efficient, and novel model for determining HMG-CoA reductase inhibition. The partial purification of the enzyme from Schizosaccharomyces pombe allowed for testing of α-asarone- and fibrate-based analogues, resulting in positive and significant inhibitory activity. © 2010 Elsevier Ltd. All rights reserved.
Subject headings
- MEDICIN OCH HÄLSOVETENSKAP -- Medicinsk bioteknologi (hsv//swe)
- MEDICAL AND HEALTH SCIENCES -- Medical Biotechnology (hsv//eng)
Keyword
- Alpha-asarone
- Docking
- HMG-CoA reductase
- Hypocholesterolemic activity
- Schizosaccharomyces pombe
Publication and Content Type
- ref (subject category)
- art (subject category)
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