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dc.contributor.author Rodriguez, Juan Bautista
dc.contributor.author Falcone, Bruno Nicolas
dc.contributor.author Szajnman, Sergio Hernan
dc.date.available 2018-09-26T18:20:13Z
dc.date.issued 2016-02
dc.identifier.citation Rodriguez, Juan Bautista; Falcone, Bruno Nicolas; Szajnman, Sergio Hernan; Approaches for Designing new Potent Inhibitors of Farnesyl Pyrophosphate Synthase; Taylor & Francis; Expert Opinion On Drug Discovery; 11; 3; 2-2016; 307-320
dc.identifier.issn 1746-0441
dc.identifier.uri http://hdl.handle.net/11336/60934
dc.description.abstract Introduction: Farnesyl pyrophosphate synthase (FPPS) catalyzes the condensation of isopentenyl diphosphate with dimethylallyl diphosphate to give rise to one molecule of geranyl diphosphate, which on a further reaction with another molecule of isopentenyl diphosphate forms the 15-carbon isoprenoid farnesyl diphosphate. This molecule is the obliged precursor for the biosynthesis of sterols, ubiquinones, dolichols, heme A, and prenylated proteins. The blockade of FPPS prevents the synthesis of farnesyl diphosphate and the downstream essential products. Due to its crucial role in isoprenoid biosynthesis, this enzyme has been winnowed as a molecular target for the treatment of different bone disorders and to control parasitic diseases, particularly, those produced by trypanosomatids and Apicomplexan parasites.Areas covered: This article discusses some relevant structural features of farnesyl pyrophosphate synthase. It also discusses the precise mode of action of relevant modulators, including both bisphosphonate and non-bisphosphonate inhibitors and the recent advances made in the development of effective inhibitors of the enzymatic activity of this target enzyme.Expert opinion: Notwithstanding their lack of drug-like character, bisphosphonates are still the most advantageous class of inhibitors of the enzymatic activity of farnesyl pyrophosphate synthase. The poor drug-like character is largely compensated by the high affinity of the bisphosphonate moiety by bone mineral hydroxyapatite in humans. Several bisphosphonates are currently in use for the treatment of a variety of bone disorders. Currently, the great prospects that bisphosphonates behave as antiparasitic agents is due to their accumulation in acidocalcisomes, organelles with equivalent composition to bone mineral, hence facilitating their antiparasitic action.
dc.format application/pdf
dc.language.iso eng
dc.publisher Taylor & Francis
dc.rights info:eu-repo/semantics/restrictedAccess
dc.rights.uri https://creativecommons.org/licenses/by-nc-sa/2.5/ar/
dc.subject BISPHOSPHONATES
dc.subject BONE DISORDERS
dc.subject FARNESYL PYROPHOSPHATE SYNTHASE
dc.subject MALARIA
dc.subject PARASITIC DISEASES
dc.subject TOXOPLASMA GONDII
dc.subject TRYPANOSOMA CRUZI
dc.subject.classification Otras Ciencias Químicas
dc.subject.classification Ciencias Químicas
dc.subject.classification CIENCIAS NATURALES Y EXACTAS
dc.title Approaches for Designing new Potent Inhibitors of Farnesyl Pyrophosphate Synthase
dc.type info:eu-repo/semantics/article
dc.type info:ar-repo/semantics/artículo
dc.type info:eu-repo/semantics/publishedVersion
dc.date.updated 2018-09-04T19:01:17Z
dc.identifier.eissn 1746-045X
dc.journal.volume 11
dc.journal.number 3
dc.journal.pagination 307-320
dc.journal.pais Reino Unido
dc.journal.ciudad Oxford
dc.description.fil Fil: Rodriguez, Juan Bautista. Consejo Nacional de Investigaciones Científicas y Técnicas. Oficina de Coordinación Administrativa Ciudad Universitaria. Unidad de Microanálisis y Métodos Físicos en Química Orgánica. Universidad de Buenos Aires. Facultad de Ciencias Exactas y Naturales. Unidad de Microanálisis y Métodos Físicos en Química Orgánica; Argentina
dc.description.fil Fil: Falcone, Bruno Nicolas. Consejo Nacional de Investigaciones Científicas y Técnicas. Oficina de Coordinación Administrativa Ciudad Universitaria. Unidad de Microanálisis y Métodos Físicos en Química Orgánica. Universidad de Buenos Aires. Facultad de Ciencias Exactas y Naturales. Unidad de Microanálisis y Métodos Físicos en Química Orgánica; Argentina
dc.description.fil Fil: Szajnman, Sergio Hernan. Consejo Nacional de Investigaciones Científicas y Técnicas. Oficina de Coordinación Administrativa Ciudad Universitaria. Unidad de Microanálisis y Métodos Físicos en Química Orgánica. Universidad de Buenos Aires. Facultad de Ciencias Exactas y Naturales. Unidad de Microanálisis y Métodos Físicos en Química Orgánica; Argentina
dc.journal.title Expert Opinion On Drug Discovery
dc.relation.alternativeid info:eu-repo/semantics/altIdentifier/url/http://www.tandfonline.com/doi/full/10.1517/17460441.2016.1143814
dc.relation.alternativeid info:eu-repo/semantics/altIdentifier/doi/http://dx.doi.org/10.1517/17460441.2016.1143814
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info:eu-repo/semantics/restrictedAccess Excepto donde se diga explícitamente, este item se publica bajo la siguiente descripción: Creative Commons Attribution-NonCommercial-ShareAlike 2.5 Unported (CC BY-NC-SA 2.5)