Approaches for Designing new Potent Inhibitors of Farnesyl Pyrophosphate Synthase

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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 f...

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Autor principal: Rodriguez, J.B
Otros Autores: Falcone, B.N, Szajnman, S.H
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Publicado: Taylor and Francis Ltd 2016
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Biblioteca Central Dr. Luis F. Leloir (FCEN) de Universidad de Buenos Aires
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024 7 |2 scopus  |a 2-s2.0-84958535830 
024 7 |2 cas  |a hydroxyapatite, 1306-06-5, 51198-94-8; farnesyl diphosphate, 13058-04-3, 372-97-4; geranyltransferase, 37277-79-5, 50812-36-7; Antiparasitic Agents; Diphosphonates; Enzyme Inhibitors; farnesyl pyrophosphate; Geranyltranstransferase; Polyisoprenyl Phosphates; Sesquiterpenes 
040 |a Scopus  |b spa  |c AR-BaUEN  |d AR-BaUEN 
100 1 |a Rodriguez, J.B. 
245 1 0 |a Approaches for Designing new Potent Inhibitors of Farnesyl Pyrophosphate Synthase 
260 |b Taylor and Francis Ltd  |c 2016 
270 1 0 |m Rodriguez, J.B.; Departamento de Química Orgánica and UMYMFOR (CONICET-FCEyN), Facultad de Ciencias Exactas y Naturales, Universidad de Buenos Aires, Pabellón 2, Ciudad Universitaria, Argentina; email: jbr@qo.fcen.uba.ar 
506 |2 openaire  |e Política editorial 
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504 |a Jahnke, W., Bold, G., Marzinzik, A.L., A general strategy for targeting drugs to bone (2015) Angew Chem Int Ed., 54, pp. 14575-14579 
520 3 |a 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. © 2016 Taylor & Francis.  |l eng 
593 |a Departamento de Química Orgánica and UMYMFOR (CONICET-FCEyN), Facultad de Ciencias Exactas y Naturales, Universidad de Buenos Aires, Pabellón 2, Ciudad Universitaria, Buenos Aires, Argentina 
690 1 0 |a BISPHOSPHONATES 
690 1 0 |a BONE DISORDERS 
690 1 0 |a FARNESYL PYROPHOSPHATE SYNTHASE 
690 1 0 |a PARASITIC DISEASES 
690 1 0 |a TOXOPLASMA GONDII 
690 1 0 |a TRYPANOSOMA CRUZI 
690 1 0 |a ANTIPARASITIC AGENT 
690 1 0 |a BENZOINDOLE DERIVATIVE 
690 1 0 |a BISPHOSPHONIC ACID DERIVATIVE 
690 1 0 |a ENZYME 
690 1 0 |a ENZYME INHIBITOR 
690 1 0 |a FARNESYL PYROPHOSPHATE SYNTHASE 
690 1 0 |a FARNESYL PYROPHOSPHATE SYNTHASE INHIBITOR 
690 1 0 |a HYDROXYAPATITE 
690 1 0 |a QUINOLINE DERIVATIVE 
690 1 0 |a SALICYLIC ACID DERIVATIVE 
690 1 0 |a UNCLASSIFIED DRUG 
690 1 0 |a ANTIPARASITIC AGENT 
690 1 0 |a BISPHOSPHONIC ACID DERIVATIVE 
690 1 0 |a ENZYME INHIBITOR 
690 1 0 |a FARNESYL DIPHOSPHATE 
690 1 0 |a GERANYLTRANSFERASE 
690 1 0 |a ISOPRENOID PHOSPHATE 
690 1 0 |a SESQUITERPENE 
690 1 0 |a BINDING AFFINITY 
690 1 0 |a BINDING SITE 
690 1 0 |a BONE DISEASE 
690 1 0 |a BONE MINERAL 
690 1 0 |a CELL ORGANELLE 
690 1 0 |a DRUG ACTIVITY 
690 1 0 |a DRUG DESIGN 
690 1 0 |a DRUG MECHANISM 
690 1 0 |a DRUG POTENCY 
690 1 0 |a DRUG STRUCTURE 
690 1 0 |a DRUG TARGETING 
690 1 0 |a ENZYME ACTIVITY 
690 1 0 |a ENZYME INHIBITION 
690 1 0 |a HUMAN 
690 1 0 |a NONHUMAN 
690 1 0 |a PRIORITY JOURNAL 
690 1 0 |a PROTEIN STRUCTURE 
690 1 0 |a REVIEW 
690 1 0 |a X RAY CRYSTALLOGRAPHY 
690 1 0 |a ANTAGONISTS AND INHIBITORS 
690 1 0 |a BONE DISEASES 
690 1 0 |a METABOLISM 
690 1 0 |a MOLECULARLY TARGETED THERAPY 
690 1 0 |a PARASITIC DISEASES 
690 1 0 |a PARASITOLOGY 
690 1 0 |a PATHOLOGY 
690 1 0 |a ANTIPARASITIC AGENTS 
690 1 0 |a BONE DISEASES 
690 1 0 |a DIPHOSPHONATES 
690 1 0 |a DRUG DESIGN 
690 1 0 |a ENZYME INHIBITORS 
690 1 0 |a GERANYLTRANSTRANSFERASE 
690 1 0 |a HUMANS 
690 1 0 |a MOLECULAR TARGETED THERAPY 
690 1 0 |a PARASITIC DISEASES 
690 1 0 |a POLYISOPRENYL PHOSPHATES 
690 1 0 |a SESQUITERPENES 
650 1 7 |2 spines  |a MALARIA 
700 1 |a Falcone, B.N. 
700 1 |a Szajnman, S.H. 
773 0 |d Taylor and Francis Ltd, 2016  |g v. 11  |h pp. 307-320  |k n. 3  |p Expert Opin. Drug. Discov.  |x 17460441  |t Expert Opinion on Drug Discovery 
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856 4 0 |u https://doi.org/10.1517/17460441.2016.1143814  |y DOI 
856 4 0 |u https://hdl.handle.net/20.500.12110/paper_17460441_v11_n3_p307_Rodriguez  |y Handle 
856 4 0 |u https://bibliotecadigital.exactas.uba.ar/collection/paper/document/paper_17460441_v11_n3_p307_Rodriguez  |y Registro en la Biblioteca Digital 
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999 |c 77095 

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