Publication:
Biocatalyzed Synthesis of Statins: A Sustainable Strategy for the Preparation of Valuable Drugs

dc.contributor.authorHoyos Vidal, Pilar
dc.contributor.authorPace, Vittorio
dc.contributor.authorAlcántara León, Andrés Rafael
dc.date.accessioned2023-06-17T12:37:50Z
dc.date.available2023-06-17T12:37:50Z
dc.date.issued2019-03-14
dc.description.abstractStatins, inhibitors of 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase, are the largest selling class of drugs prescribed for the pharmacological treatment of hypercholesterolemia and dyslipidaemia. Statins also possess other therapeutic effects, called pleiotropic, because the blockade of the conversion of HMG-CoA to (R)-mevalonate produces a concomitant inhibition of the biosynthesis of numerous isoprenoid metabolites (e.g., geranylgeranyl pyrophosphate (GGPP) or farnesyl pyrophosphate (FPP)). Thus, the prenylation of several cell signalling proteins (small GTPase family members: Ras, Rac, and Rho) is hampered, so that these molecular switches, controlling multiple pathways and cell functions (maintenance of cell shape, motility, factor secretion, differentiation, and proliferation) are regulated, leading to beneficial effects in cardiovascular health, regulation of the immune system, anti-inflammatory and immunosuppressive properties, prevention and treatment of sepsis, treatment of autoimmune diseases, osteoporosis, kidney and neurological disorders, or even in cancer therapy. Thus, there is a growing interest in developing more sustainable protocols for preparation of statins, and the introduction of biocatalyzed steps into the synthetic pathways is highly advantageous—synthetic routes are conducted under mild reaction conditions, at ambient temperature, and can use water as a reaction medium in many cases. Furthermore, their high selectivity avoids the need for functional group activation and protection/deprotection steps usually required in traditional organic synthesis. Therefore, biocatalysis provides shorter processes, produces less waste, and reduces manufacturing costs and environmental impact. In this review, we will comment on the pleiotropic effects of statins and will illustrate some biotransformations nowadays implemented for statin synthesis.
dc.description.departmentDepto. de Química en Ciencias Farmacéuticas
dc.description.facultyFac. de Farmacia
dc.description.refereedTRUE
dc.description.sponsorshipMinisterio de Economía y Competitividad (MINECO)
dc.description.statuspub
dc.eprint.idhttps://eprints.ucm.es/id/eprint/67097
dc.identifier.doi10.3390/catal9030260
dc.identifier.issn2073-4344
dc.identifier.officialurlhttps://doi.org/10.3390/catal9030260
dc.identifier.relatedurlhttps://www.mdpi.com/2073-4344/9/3/260
dc.identifier.urihttps://hdl.handle.net/20.500.14352/12659
dc.issue.number3
dc.journal.titleCatalysts
dc.language.isoeng
dc.page.initial260
dc.publisherMDPI
dc.relation.projectIDCTQ2015-66206-C2-1-R
dc.rightsAtribución 3.0 España
dc.rights.accessRightsopen access
dc.rights.urihttps://creativecommons.org/licenses/by/3.0/es/
dc.subject.keywordbiocatalysis
dc.subject.keywordbiotransformations
dc.subject.keywordstatins
dc.subject.keywordpleiotropic effects
dc.subject.ucmQuímica farmaceútica
dc.subject.unesco2390 Química Farmacéutica
dc.titleBiocatalyzed Synthesis of Statins: A Sustainable Strategy for the Preparation of Valuable Drugs
dc.typejournal article
dc.volume.number9
dspace.entity.typePublication
relation.isAuthorOfPublicationc0d1193e-3161-4c69-af69-830b32f61932
relation.isAuthorOfPublication.latestForDiscoveryc0d1193e-3161-4c69-af69-830b32f61932
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