Advances in drug design based on the amino acid approach: Taurine analogues for the treatment of CNS diseases
Autor(a) principal: | |
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Data de Publicação: | 2012 |
Outros Autores: | , , , , |
Tipo de documento: | Artigo |
Idioma: | eng |
Título da fonte: | Repositório Institucional da UNESP |
Texto Completo: | http://dx.doi.org/10.3390/ph5101128 http://hdl.handle.net/11449/73673 |
Resumo: | Amino acids are well known to be an important class of compounds for the maintenance of body homeostasis and their deficit, even for the polar neuroactive aminoacids, can be controlled by supplementation. However, for the amino acid taurine (2-aminoethanesulfonic acid) this is not true. Due its special physicochemical properties, taurine is unable to cross the blood-brain barrier. In addition of injured taurine transport systems under pathological conditions, CNS supplementation of taurine is almost null. Taurine is a potent antioxidant and anti-inflammatory semi-essential amino acid extensively involved in neurological activities, acting as neurotrophic factor, binding to GABA A/glycine receptors and blocking the excitotoxicity glutamate-induced pathway leading to be a neuroprotective effect and neuromodulation. Taurine deficits have been implicated in several CNS diseases, such as Alzheimer's, Parkinson's, epilepsy and in the damage of retinal neurons. This review describes the CNS physiological functions of taurine and the development of new derivatives based on its structure useful in CNS disease treatment.&; 2012 by the authors; licensee MDPI, Basel, Switzerland. |
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Advances in drug design based on the amino acid approach: Taurine analogues for the treatment of CNS diseasesAmino acidAnalogsCNSTaurine2 aminoethylmethylsulfone2 aminoethylphosphonic acid2 phthalimidoethanesulfonamide derivative4 aminobutyric acid A receptoracamprosatealcoholaminocyclohexaenesulfonic acidaniline 2 sulfinic acidanticonvulsive agentcysteic aciddimethyltaurineethanolamine sulfateglutaurineglycine receptorhomotaurinen methyl thiomorpholine 1,1 dioxiden pivaloyltaurinepiperidine 3 sulfinic acidtau 15taurepartaurinetaurine derivativetaurocholic acidtaurolidinetauropyronethiomorpholine 1,1 dioxidetrimethyltaurineunclassified drugvalproyltaurinamide derivativealcoholismAlzheimer diseaseamino acid substitutionanticonvulsant activitybipolar disorderblood brain barrierbrain edemabrain ischemiacentral nervous system diseasecentral nervous system tumorCLogPdigestive system cancerdose responsedrug designdrug efficacydrug potencydrug receptor bindingdrug structuredrug synthesisexcitotoxicityhumanhyperthermiahypothermialipophilicitylow drug doseneuromodulationneuroprotectionnonhumanParkinson diseaseretina diseasereviewseizurespinal cord compressionstatistical parametersstructure activity relationtoxicity testingAmino acids are well known to be an important class of compounds for the maintenance of body homeostasis and their deficit, even for the polar neuroactive aminoacids, can be controlled by supplementation. However, for the amino acid taurine (2-aminoethanesulfonic acid) this is not true. Due its special physicochemical properties, taurine is unable to cross the blood-brain barrier. In addition of injured taurine transport systems under pathological conditions, CNS supplementation of taurine is almost null. Taurine is a potent antioxidant and anti-inflammatory semi-essential amino acid extensively involved in neurological activities, acting as neurotrophic factor, binding to GABA A/glycine receptors and blocking the excitotoxicity glutamate-induced pathway leading to be a neuroprotective effect and neuromodulation. Taurine deficits have been implicated in several CNS diseases, such as Alzheimer's, Parkinson's, epilepsy and in the damage of retinal neurons. This review describes the CNS physiological functions of taurine and the development of new derivatives based on its structure useful in CNS disease treatment.&; 2012 by the authors; licensee MDPI, Basel, Switzerland.Lapdesf-Laboratory of Drug Design School of Pharmaceutical Sciences University of São Paulo State (UNESP), Rodovia Araraquara-Jaú Km1, CEP 14.801-902, Araraquara, SPLapdesf-Laboratory of Drug Design School of Pharmaceutical Sciences University of São Paulo State (UNESP), Rodovia Araraquara-Jaú Km1, CEP 14.801-902, Araraquara, SPUniversidade Estadual Paulista (Unesp)Chung, Man Chin [UNESP]Malatesta, Pedro [UNESP]Bosquesi, Priscila Longhin [UNESP]Yamasaki, Paulo Renato [UNESP]dos Santos, Jean Leandro [UNESP]Vizioli, Ednir Oliveira [UNESP]2014-05-27T11:27:06Z2014-05-27T11:27:06Z2012-10-23info:eu-repo/semantics/publishedVersioninfo:eu-repo/semantics/article1128-1146application/pdfhttp://dx.doi.org/10.3390/ph5101128Pharmaceuticals, v. 5, n. 10, p. 1128-1146, 2012.1424-8247http://hdl.handle.net/11449/7367310.3390/ph51011282-s2.0-848692066932-s2.0-84869206693.pdf97343336079754130000-0003-4141-0455Scopusreponame:Repositório Institucional da UNESPinstname:Universidade Estadual Paulista (UNESP)instacron:UNESPengPharmaceuticals1,293info:eu-repo/semantics/openAccess2024-04-17T18:28:59Zoai:repositorio.unesp.br:11449/73673Repositório InstitucionalPUBhttp://repositorio.unesp.br/oai/requestopendoar:29462024-08-05T15:02:18.309742Repositório Institucional da UNESP - Universidade Estadual Paulista (UNESP)false |
dc.title.none.fl_str_mv |
Advances in drug design based on the amino acid approach: Taurine analogues for the treatment of CNS diseases |
title |
Advances in drug design based on the amino acid approach: Taurine analogues for the treatment of CNS diseases |
spellingShingle |
Advances in drug design based on the amino acid approach: Taurine analogues for the treatment of CNS diseases Chung, Man Chin [UNESP] Amino acid Analogs CNS Taurine 2 aminoethylmethylsulfone 2 aminoethylphosphonic acid 2 phthalimidoethanesulfonamide derivative 4 aminobutyric acid A receptor acamprosate alcohol aminocyclohexaenesulfonic acid aniline 2 sulfinic acid anticonvulsive agent cysteic acid dimethyltaurine ethanolamine sulfate glutaurine glycine receptor homotaurine n methyl thiomorpholine 1,1 dioxide n pivaloyltaurine piperidine 3 sulfinic acid tau 15 taurepar taurine taurine derivative taurocholic acid taurolidine tauropyrone thiomorpholine 1,1 dioxide trimethyltaurine unclassified drug valproyltaurinamide derivative alcoholism Alzheimer disease amino acid substitution anticonvulsant activity bipolar disorder blood brain barrier brain edema brain ischemia central nervous system disease central nervous system tumor CLogP digestive system cancer dose response drug design drug efficacy drug potency drug receptor binding drug structure drug synthesis excitotoxicity human hyperthermia hypothermia lipophilicity low drug dose neuromodulation neuroprotection nonhuman Parkinson disease retina disease review seizure spinal cord compression statistical parameters structure activity relation toxicity testing |
title_short |
Advances in drug design based on the amino acid approach: Taurine analogues for the treatment of CNS diseases |
title_full |
Advances in drug design based on the amino acid approach: Taurine analogues for the treatment of CNS diseases |
title_fullStr |
Advances in drug design based on the amino acid approach: Taurine analogues for the treatment of CNS diseases |
title_full_unstemmed |
Advances in drug design based on the amino acid approach: Taurine analogues for the treatment of CNS diseases |
title_sort |
Advances in drug design based on the amino acid approach: Taurine analogues for the treatment of CNS diseases |
author |
Chung, Man Chin [UNESP] |
author_facet |
Chung, Man Chin [UNESP] Malatesta, Pedro [UNESP] Bosquesi, Priscila Longhin [UNESP] Yamasaki, Paulo Renato [UNESP] dos Santos, Jean Leandro [UNESP] Vizioli, Ednir Oliveira [UNESP] |
author_role |
author |
author2 |
Malatesta, Pedro [UNESP] Bosquesi, Priscila Longhin [UNESP] Yamasaki, Paulo Renato [UNESP] dos Santos, Jean Leandro [UNESP] Vizioli, Ednir Oliveira [UNESP] |
author2_role |
author author author author author |
dc.contributor.none.fl_str_mv |
Universidade Estadual Paulista (Unesp) |
dc.contributor.author.fl_str_mv |
Chung, Man Chin [UNESP] Malatesta, Pedro [UNESP] Bosquesi, Priscila Longhin [UNESP] Yamasaki, Paulo Renato [UNESP] dos Santos, Jean Leandro [UNESP] Vizioli, Ednir Oliveira [UNESP] |
dc.subject.por.fl_str_mv |
Amino acid Analogs CNS Taurine 2 aminoethylmethylsulfone 2 aminoethylphosphonic acid 2 phthalimidoethanesulfonamide derivative 4 aminobutyric acid A receptor acamprosate alcohol aminocyclohexaenesulfonic acid aniline 2 sulfinic acid anticonvulsive agent cysteic acid dimethyltaurine ethanolamine sulfate glutaurine glycine receptor homotaurine n methyl thiomorpholine 1,1 dioxide n pivaloyltaurine piperidine 3 sulfinic acid tau 15 taurepar taurine taurine derivative taurocholic acid taurolidine tauropyrone thiomorpholine 1,1 dioxide trimethyltaurine unclassified drug valproyltaurinamide derivative alcoholism Alzheimer disease amino acid substitution anticonvulsant activity bipolar disorder blood brain barrier brain edema brain ischemia central nervous system disease central nervous system tumor CLogP digestive system cancer dose response drug design drug efficacy drug potency drug receptor binding drug structure drug synthesis excitotoxicity human hyperthermia hypothermia lipophilicity low drug dose neuromodulation neuroprotection nonhuman Parkinson disease retina disease review seizure spinal cord compression statistical parameters structure activity relation toxicity testing |
topic |
Amino acid Analogs CNS Taurine 2 aminoethylmethylsulfone 2 aminoethylphosphonic acid 2 phthalimidoethanesulfonamide derivative 4 aminobutyric acid A receptor acamprosate alcohol aminocyclohexaenesulfonic acid aniline 2 sulfinic acid anticonvulsive agent cysteic acid dimethyltaurine ethanolamine sulfate glutaurine glycine receptor homotaurine n methyl thiomorpholine 1,1 dioxide n pivaloyltaurine piperidine 3 sulfinic acid tau 15 taurepar taurine taurine derivative taurocholic acid taurolidine tauropyrone thiomorpholine 1,1 dioxide trimethyltaurine unclassified drug valproyltaurinamide derivative alcoholism Alzheimer disease amino acid substitution anticonvulsant activity bipolar disorder blood brain barrier brain edema brain ischemia central nervous system disease central nervous system tumor CLogP digestive system cancer dose response drug design drug efficacy drug potency drug receptor binding drug structure drug synthesis excitotoxicity human hyperthermia hypothermia lipophilicity low drug dose neuromodulation neuroprotection nonhuman Parkinson disease retina disease review seizure spinal cord compression statistical parameters structure activity relation toxicity testing |
description |
Amino acids are well known to be an important class of compounds for the maintenance of body homeostasis and their deficit, even for the polar neuroactive aminoacids, can be controlled by supplementation. However, for the amino acid taurine (2-aminoethanesulfonic acid) this is not true. Due its special physicochemical properties, taurine is unable to cross the blood-brain barrier. In addition of injured taurine transport systems under pathological conditions, CNS supplementation of taurine is almost null. Taurine is a potent antioxidant and anti-inflammatory semi-essential amino acid extensively involved in neurological activities, acting as neurotrophic factor, binding to GABA A/glycine receptors and blocking the excitotoxicity glutamate-induced pathway leading to be a neuroprotective effect and neuromodulation. Taurine deficits have been implicated in several CNS diseases, such as Alzheimer's, Parkinson's, epilepsy and in the damage of retinal neurons. This review describes the CNS physiological functions of taurine and the development of new derivatives based on its structure useful in CNS disease treatment.&; 2012 by the authors; licensee MDPI, Basel, Switzerland. |
publishDate |
2012 |
dc.date.none.fl_str_mv |
2012-10-23 2014-05-27T11:27:06Z 2014-05-27T11:27:06Z |
dc.type.status.fl_str_mv |
info:eu-repo/semantics/publishedVersion |
dc.type.driver.fl_str_mv |
info:eu-repo/semantics/article |
format |
article |
status_str |
publishedVersion |
dc.identifier.uri.fl_str_mv |
http://dx.doi.org/10.3390/ph5101128 Pharmaceuticals, v. 5, n. 10, p. 1128-1146, 2012. 1424-8247 http://hdl.handle.net/11449/73673 10.3390/ph5101128 2-s2.0-84869206693 2-s2.0-84869206693.pdf 9734333607975413 0000-0003-4141-0455 |
url |
http://dx.doi.org/10.3390/ph5101128 http://hdl.handle.net/11449/73673 |
identifier_str_mv |
Pharmaceuticals, v. 5, n. 10, p. 1128-1146, 2012. 1424-8247 10.3390/ph5101128 2-s2.0-84869206693 2-s2.0-84869206693.pdf 9734333607975413 0000-0003-4141-0455 |
dc.language.iso.fl_str_mv |
eng |
language |
eng |
dc.relation.none.fl_str_mv |
Pharmaceuticals 1,293 |
dc.rights.driver.fl_str_mv |
info:eu-repo/semantics/openAccess |
eu_rights_str_mv |
openAccess |
dc.format.none.fl_str_mv |
1128-1146 application/pdf |
dc.source.none.fl_str_mv |
Scopus reponame:Repositório Institucional da UNESP instname:Universidade Estadual Paulista (UNESP) instacron:UNESP |
instname_str |
Universidade Estadual Paulista (UNESP) |
instacron_str |
UNESP |
institution |
UNESP |
reponame_str |
Repositório Institucional da UNESP |
collection |
Repositório Institucional da UNESP |
repository.name.fl_str_mv |
Repositório Institucional da UNESP - Universidade Estadual Paulista (UNESP) |
repository.mail.fl_str_mv |
|
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1808128220448423936 |