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[PMID]:29390377
[Au] Autor:Trifan A; Stanciu C; Gheorghe L; Iacob S; Curescu M; Cijevschi Prelipcean C; Stefanescu G; Girleanu I; Chiriac S; Mihai C; Brisc C; Goldis A; Sporea I; Miftode E; Bataga S; Rogoveanu I; Preda C; Caruntu FA; Singeap AM
[Ad] Endereço:"Grigore T. Popa" University of Medicine and Pharmacy Iasi.
[Ti] Título:Efficacy and safety of paritaprevir/ritonavir, ombitasvir, and dasabuvir with ribavirin for the treatment of HCV genotype 1b compensated cirrhosis in patients aged 70 years or older.
[So] Source:Medicine (Baltimore);96(50):e9271, 2017 Dec.
[Is] ISSN:1536-5964
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Advanced age has been a major limitation of interferon-based treatment for chronic hepatitis C virus (HCV) infection because of its poor response and tolerability. Direct-acting antiviral (DAA) drug regimens are safe and highly effective, allowing administration of treatment also in elderly. This study aims to assess the efficacy and safety of paritaprevir/ritonavir, ombitasvir, and dasabuvir (PrOD) with ribavirin for the treatment of patients aged ≥70 years with HCV genotype 1b compensated cirrhosis.A total of 1008 patients with HCV genotype 1b compensated cirrhosis were prospectively treated with PrOD + ribavirin for 12 weeks, between December 2015 and July 2016. Sustained virologic response 12 weeks after the end of treatment (SVR12), adverse effects (AEs), comorbidities, discontinuation, and death rates were recorded. Efficacy and safety of therapy were assessed in patients aged ≥70 years and compared with data from patients <70 years.There were 117 patients aged ≥70 years, preponderantly females (58.9%), mean age 73.3 ±â€Š2.8 years (range 70-82), and 37 (31.6%) were treatment-experienced. Comorbidities were reported in 60.6% of patients ≥70 years and in 39.8% of those <70 years (P < .001). SVR12 rates based on intention-to-treat and per-protocol analyses were 97.4% and 100%, respectively, in patients ≥70 years, compared to 97.8% and 99.6%, respectively, in patients <70 years (P = ns and P = ns). Severe AEs were reported in 4 (3.4%) patients ≥70 years, compared to 23 (2.6%) in those <70 years (P = ns). One death was recorded in a patient aged 79 years (0.9%) and 6 deaths (0.8%) in those <70 years (P = ns).Treatment with PrOD + ribavirin in patients 70 years of age or older with HCV genotype 1b compensated cirrhosis proved as effective, safe, and well tolerated, as it did in younger patients.
[Mh] Termos MeSH primário: Antivirais/uso terapêutico
Hepatite C Crônica/tratamento farmacológico
Cirrose Hepática/tratamento farmacológico
Cirrose Hepática/virologia
[Mh] Termos MeSH secundário: Idoso
Idoso de 80 Anos ou mais
Anilidas/uso terapêutico
Carbamatos/uso terapêutico
Farmacorresistência Viral
Quimioterapia Combinada
Feminino
Genótipo
Seres Humanos
Compostos Macrocíclicos/uso terapêutico
Masculino
Estudos Prospectivos
Ribavirina/uso terapêutico
Ritonavir/uso terapêutico
Sulfonamidas/uso terapêutico
Resposta Viral Sustentada
Uracila/análogos & derivados
Uracila/uso terapêutico
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (ABT-267); 0 (ABT-333); 0 (ABT-450); 0 (Anilides); 0 (Antiviral Agents); 0 (Carbamates); 0 (Macrocyclic Compounds); 0 (Sulfonamides); 49717AWG6K (Ribavirin); 56HH86ZVCT (Uracil); O3J8G9O825 (Ritonavir)
[Em] Mês de entrada:1802
[Cu] Atualização por classe:180301
[Lr] Data última revisão:
180301
[Sb] Subgrupo de revista:AIM; IM
[Da] Data de entrada para processamento:180203
[St] Status:MEDLINE
[do] DOI:10.1097/MD.0000000000009271


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[PMID]:29324623
[Au] Autor:Hussar DA
[Ad] Endereço:Remington Professor of Pharmacy Philadelphia College of Pharmacy University of the Sciences Philadelphia, Pa.
[Ti] Título:New Drugs 2018, part 1.
[So] Source:Nursing;48(2):36-44, 2018 Feb.
[Is] ISSN:1538-8689
[Cp] País de publicação:United States
[La] Idioma:eng
[Mh] Termos MeSH primário: Aprovação de Drogas
[Mh] Termos MeSH secundário: Anticorpos Monoclonais/uso terapêutico
Anticorpos Neutralizantes/uso terapêutico
Antipirina/análogos & derivados
Antipirina/uso terapêutico
Benzamidas/uso terapêutico
Benzimidazóis/uso terapêutico
Carbamatos/uso terapêutico
Combinação de Medicamentos
Compostos Heterocíclicos de 4 ou mais Anéis/uso terapêutico
Seres Humanos
Compostos Macrocíclicos/uso terapêutico
Naltrexona/análogos & derivados
Naltrexona/uso terapêutico
Peptídeos Natriuréticos/uso terapêutico
Piridinas/uso terapêutico
Quinoxalinas/uso terapêutico
Sofosbuvir/uso terapêutico
Sulfonamidas/uso terapêutico
Estados Unidos
United States Food and Drug Administration
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (ABT-493); 0 (Antibodies, Monoclonal); 0 (Antibodies, Neutralizing); 0 (Benzamides); 0 (Benzimidazoles); 0 (Carbamates); 0 (Drug Combinations); 0 (Heterocyclic Compounds, 4 or More Rings); 0 (Macrocyclic Compounds); 0 (Natriuretic Peptides); 0 (Pyridines); 0 (Quinoxalines); 0 (Sulfonamides); 0 (bezlotoxumab); 0 (naldemedine); 0 (pibrentasvir); 0 (voxilaprevir); 5S6W795CQM (Naltrexone); 74RWP7W0J9 (betrixaban); 7IK8Z952OK (plecanatide); KCU0C7RS7Z (velpatasvir); S798V6YJRP (phenylmethylpyrazolone); T3CHA1B51H (Antipyrine); WJ6CA3ZU8B (Sofosbuvir)
[Em] Mês de entrada:1802
[Cu] Atualização por classe:180223
[Lr] Data última revisão:
180223
[Sb] Subgrupo de revista:N
[Da] Data de entrada para processamento:180112
[St] Status:MEDLINE
[do] DOI:10.1097/01.NURSE.0000529803.83288.e1


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[PMID]:29288939
[Au] Autor:Cheong JE; Zaffagni M; Chung I; Xu Y; Wang Y; Jernigan FE; Zetter BR; Sun L
[Ad] Endereço:Center for Drug Discovery and Translational Research, Beth Israel Deaconess Medical Center, Harvard Medical School, Boston, MA 02215, USA.
[Ti] Título:Synthesis and anticancer activity of novel water soluble benzimidazole carbamates.
[So] Source:Eur J Med Chem;144:372-385, 2018 Jan 20.
[Is] ISSN:1768-3254
[Cp] País de publicação:France
[La] Idioma:eng
[Ab] Resumo:Metastases account for more than 90% of all cancer deaths and respond poorly to most therapies. There remains an urgent need for new therapeutic modalities for the treatment of advanced metastatic cancers. The benzimidazole methylcarbamate drugs, commonly used as anti-helmitics, have been suggested to have anticancer activity, but progress has been stalled by their poor water solubility and poor suitability for systemic delivery to disseminated cancers. We synthesized and characterized the anticancer activity of novel benzimidazoles containing an oxetane or an amine group to enhance solubility. Among them, the novel oxetanyl substituted compound 18 demonstrated significant cytotoxicity toward a variety of cancer cell types including prostate, lung, and ovarian cancers with strong activity toward highly aggressive cancer lines (IC : 0.9-3.8 µM). Compound 18 achieved aqueous solubility of 361 µM. In a mouse xenograft model of a highly metastatic human prostate cancer, compound 18 (30 mg/kg) significantly inhibited the growth of established tumors (T/C: 0.36) without noticeable toxicity.
[Mh] Termos MeSH primário: Antineoplásicos/farmacologia
Benzimidazóis/farmacologia
Carbamatos/farmacologia
Água/química
[Mh] Termos MeSH secundário: Animais
Antineoplásicos/síntese química
Antineoplásicos/química
Benzimidazóis/síntese química
Benzimidazóis/química
Carbamatos/síntese química
Carbamatos/química
Proliferação Celular/efeitos dos fármacos
Sobrevivência Celular/efeitos dos fármacos
Relação Dose-Resposta a Droga
Seres Humanos
Masculino
Camundongos
Simulação de Acoplamento Molecular
Estrutura Molecular
Neoplasias Experimentais/tratamento farmacológico
Neoplasias Experimentais/patologia
Solubilidade
Relação Estrutura-Atividade
Células Tumorais Cultivadas
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Antineoplastic Agents); 0 (Benzimidazoles); 0 (Carbamates); 059QF0KO0R (Water)
[Em] Mês de entrada:1802
[Cu] Atualização por classe:180223
[Lr] Data última revisão:
180223
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:171231
[St] Status:MEDLINE


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[PMID]:29325476
[Au] Autor:Chamorro-de-Vega E; Gimenez-Manzorro A; Rodriguez-Gonzalez CG; Escudero-Vilaplana V; De Lorenzo-Pinto A; Iglesias-Peinado I; Herranz-Alonso A; Sanjurjo Saez M; GRUviC Study Group
[Ad] Endereço:a Pharmacy Department , Hospital General Universitario Gregorio Marañón, Instituto de Investigación Sanitaria del Hospital Gregorio Marañón , Madrid , Spain.
[Ti] Título:Twelve weeks of ombitasvir/paritaprevir/r and dasabuvir without ribavirin is effective and safe in the treatment of patients with HCV genotype 1b infection and compensated cirrhosis: results from a real-world cohort study.
[So] Source:Expert Opin Drug Saf;17(3):235-241, 2018 Mar.
[Is] ISSN:1744-764X
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:OBJECTIVE: To explore the effectiveness and safety of ombitasvir/paritaprevir/ritonavir and dasabuvir (OBV/PTV/r+DSV) for 12 weeks without ribavirin in adults with chronic HCV genotype 1b infection and compensated cirrhosis. METHODS: Observational study of a prospective cohort of adult patients with HCV genotype 1b infection and compensated cirrhosis who received 12 weeks of OBV/PTV/r and DSV without ribavirin. Effectiveness was assessed by recording the percentage of patients achieving sustained virological response at week 12 post-treatment (SVR12). Safety outcomes were based on the incidence of adverse events. RESULTS: Seventy-eight patients were included. The SVR12 rate was 96.1% (95%CI 89.2-99.2). Adverse events were recorded in 78.0% of patients. Of these, 97.7% were grade 1/2. One patient discontinued treatment prematurely owing to adverse events. Eighty-six interactions were detected in 43 patients (55.1%). Overall, 81.4% of interactions required close monitoring, alteration of drug dosage, or timing of administration. In 7.0% of cases, the interactions arose from contraindications that required the suspension of the concomitant drug. In 11.6% of cases, medicinal plants or foods were withdrawn. CONCLUSIONS: The simplified regimen of OBV/PTV/r+DSV administered for 12 weeks is effective and safe in patients with chronic HCV genotype 1b infection and compensated cirrhosis. No adverse reactions related to drug-drug interactions were recorded.
[Mh] Termos MeSH primário: Antivirais/administração & dosagem
Hepacivirus/genética
Hepatite C Crônica/tratamento farmacológico
Cirrose Hepática/tratamento farmacológico
[Mh] Termos MeSH secundário: Idoso
Anilidas/administração & dosagem
Anilidas/efeitos adversos
Antivirais/efeitos adversos
Carbamatos/administração & dosagem
Carbamatos/efeitos adversos
Estudos de Coortes
Interações Medicamentosas
Quimioterapia Combinada
Feminino
Genótipo
Hepatite C Crônica/virologia
Seres Humanos
Cirrose Hepática/virologia
Compostos Macrocíclicos/administração & dosagem
Compostos Macrocíclicos/efeitos adversos
Masculino
Meia-Idade
Estudos Prospectivos
Ritonavir/administração & dosagem
Ritonavir/efeitos adversos
Sulfonamidas/administração & dosagem
Sulfonamidas/efeitos adversos
Resultado do Tratamento
Uracila/administração & dosagem
Uracila/efeitos adversos
Uracila/análogos & derivados
[Pt] Tipo de publicação:JOURNAL ARTICLE; OBSERVATIONAL STUDY
[Nm] Nome de substância:
0 (ABT-267); 0 (ABT-333); 0 (ABT-450); 0 (Anilides); 0 (Antiviral Agents); 0 (Carbamates); 0 (Macrocyclic Compounds); 0 (Sulfonamides); 56HH86ZVCT (Uracil); O3J8G9O825 (Ritonavir)
[Em] Mês de entrada:1802
[Cu] Atualização por classe:180215
[Lr] Data última revisão:
180215
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:180113
[St] Status:MEDLINE
[do] DOI:10.1080/14740338.2018.1424829


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[PMID]:28468728
[Au] Autor:Zhou H; Xiao Q; Tan W; Zhan Y; Pistolozzi M
[Ad] Endereço:School of Bioscience & Bioengineering, South China University of Technology, Higher Education Mega Center, 510006, Guangzhou, People's Republic of China.
[Ti] Título:Quantitative estimation of cholinesterase-specific drug metabolism of carbamate inhibitors provided by the analysis of the area under the inhibition-time curve.
[So] Source:J Pharm Biomed Anal;144:167-174, 2017 Sep 10.
[Is] ISSN:1873-264X
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Several molecules containing carbamate groups are metabolized by cholinesterases. This metabolism includes a time-dependent catalytic step which temporary inhibits the enzymes. In this paper we demonstrate that the analysis of the area under the inhibition versus time curve (AUIC) can be used to obtain a quantitative estimation of the amount of carbamate metabolized by the enzyme. (R)-bambuterol monocarbamate and plasma butyrylcholinesterase were used as model carbamate-cholinesterase system. The inhibition of different concentrations of the enzyme was monitored for 5h upon incubation with different concentrations of carbamate and the resulting AUICs were analyzed. The amount of carbamate metabolized could be estimated with <15% accuracy (RE%) and ≤23% precision (RSD%). Since the knowledge of the inhibition kinetics is not required for the analysis, this approach could be used to determine the amount of drug metabolized by cholinesterases in a selected compartment in which the cholinesterase is confined (e.g. in vitro solutions, tissues or body fluids), either in vitro or in vivo.
[Mh] Termos MeSH primário: Inibidores da Colinesterase/farmacologia
[Mh] Termos MeSH secundário: Biocatálise
Carbamatos
Colinesterases
Cinética
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Carbamates); 0 (Cholinesterase Inhibitors); EC 3.1.1.8 (Cholinesterases)
[Em] Mês de entrada:1802
[Cu] Atualização por classe:180205
[Lr] Data última revisão:
180205
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170505
[St] Status:MEDLINE


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[PMID]:29240834
[Au] Autor:Ufarté L; Laville E; Duquesne S; Morgavi D; Robe P; Klopp C; Rizzo A; Pizzut-Serin S; Potocki-Veronese G
[Ad] Endereço:LISBP, Université de Toulouse, CNRS, INRA, INSA, Toulouse, France.
[Ti] Título:Discovery of carbamate degrading enzymes by functional metagenomics.
[So] Source:PLoS One;12(12):e0189201, 2017.
[Is] ISSN:1932-6203
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Bioremediation of pollutants is a major concern worldwide, leading to the research of new processes to break down and recycle xenobiotics and environment contaminating polymers. Among them, carbamates have a very broad spectrum of uses, such as toxinogenic pesticides or elastomers. In this study, we mined the bovine rumen microbiome for carbamate degrading enzymes. We isolated 26 hit clones exhibiting esterase activity, and were able to degrade at least one of the targeted polyurethane and pesticide carbamate compounds. The most active clone was deeply characterized. In addition to Impranil, this clone was active on Tween 20, pNP-acetate, butyrate and palmitate, and on the insecticide fenobucarb. Sequencing and sub-cloning of the best target revealed a novel carboxyl-ester hydrolase belonging to the lipolytic family IV, named CE_Ubrb. This study highlights the potential of highly diverse microbiota such as the ruminal one for the discovery of promiscuous enzymes, whose versatility could be exploited for industrial uses.
[Mh] Termos MeSH primário: Carbamatos/metabolismo
Metagenômica
[Mh] Termos MeSH secundário: Animais
Bovinos
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Carbamates)
[Em] Mês de entrada:1801
[Cu] Atualização por classe:180116
[Lr] Data última revisão:
180116
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:171215
[St] Status:MEDLINE
[do] DOI:10.1371/journal.pone.0189201


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[PMID]:29239718
[Au] Autor:Ordeig L; Garcia-Cehic D; Gregori J; Soria ME; Nieto-Aponte L; Perales C; Llorens M; Chen Q; Riveiro-Barciela M; Buti M; Esteban R; Esteban JI; Rodriguez-Frias F; Quer J
[Ad] Endereço:1​Liver Unit, Liver Disease Laboratory-Viral Hepatitis, Internal Medicine Department, Vall d'Hebron Institut Recerca (VHIR)-Hospital Universitari Vall d'Hebron (HUVH), 08035, Barcelona, Spain.
[Ti] Título:New hepatitis C virus genotype 1 subtype naturally harbouring resistance-associated mutations to NS5A inhibitors.
[So] Source:J Gen Virol;99(1):97-102, 2018 Jan.
[Is] ISSN:1465-2099
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Hepatitis C virus (HCV) is a highly divergent virus currently classified into seven major genotypes and 86 subtypes (ICTV, June 2017), which can have differing responses to therapy. Accurate genotyping/subtyping using high-resolution HCV subtyping enables confident subtype identification, identifies mixed infections and allows detection of new subtypes. During routine genotyping/subtyping, one sample from an Equatorial Guinea patient could not be classified into any of the subtypes. The complete genomic sequence was compared to reference sequences by phylogenetic and sliding window analysis. Resistance-associated substitutions (RASs) were assessed by deep sequencing. The unclassified HCV genome did not belong to any of the existing genotype 1 (G1) subtypes. Sliding window analysis along the complete genome ruled out recombination phenomena suggesting that it belongs to a new HCV G1 subtype. Two NS5A RASs (L31V+Y93H) were found to be naturally combined in the genome which could limit treatment possibilities in patients infected with this subtype.
[Mh] Termos MeSH primário: Farmacorresistência Viral/genética
Genótipo
Hepacivirus/genética
Mutação
Filogenia
Proteínas não Estruturais Virais/genética
[Mh] Termos MeSH secundário: Anilidas/uso terapêutico
Antivirais/uso terapêutico
Benzimidazóis/uso terapêutico
Carbamatos/uso terapêutico
Guiné Equatorial
Feminino
Fluorenos/uso terapêutico
Expressão Gênica
Hepacivirus/classificação
Hepacivirus/efeitos dos fármacos
Hepatite C/tratamento farmacológico
Hepatite C/patologia
Hepatite C/virologia
Seres Humanos
Imidazóis/uso terapêutico
Testes de Sensibilidade Microbiana
Meia-Idade
Análise de Sequência de DNA
Sulfonamidas/uso terapêutico
Uracila/análogos & derivados
Uracila/uso terapêutico
[Pt] Tipo de publicação:CASE REPORTS; JOURNAL ARTICLE
[Nm] Nome de substância:
0 (ABT-267); 0 (ABT-333); 0 (Anilides); 0 (Antiviral Agents); 0 (BMS-790052); 0 (Benzimidazoles); 0 (Carbamates); 0 (Fluorenes); 0 (Imidazoles); 0 (NS-5 protein, hepatitis C virus); 0 (Sulfonamides); 0 (Viral Nonstructural Proteins); 013TE6E4WV (ledipasvir); 56HH86ZVCT (Uracil)
[Em] Mês de entrada:1712
[Cu] Atualização por classe:171229
[Lr] Data última revisão:
171229
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:171215
[St] Status:MEDLINE
[do] DOI:10.1099/jgv.0.000996


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[PMID]:27771531
[Au] Autor:Sartim AG; Moreira FA; Joca SRL
[Ad] Endereço:Department of Physical and Chemical, School of Pharmaceutical Science of Ribeirão Preto, University of São Paulo, Ribeirão Preto, SP, Brazil.
[Ti] Título:Involvement of CB and TRPV1 receptors located in the ventral medial prefrontal cortex in the modulation of stress coping behavior.
[So] Source:Neuroscience;340:126-134, 2017 Jan 06.
[Is] ISSN:1873-7544
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Cannabinoid type-1 (CB ) and transient receptor potential vanilloid type-1 (TRPV1) receptors may have opposite roles in modulating neural activity and, consequently, in regulating the stress response. These receptors are widely expressed in several brain structures, including the ventral medial prefrontal cortex (vmPFC). The functional consequences of the interaction between CB and TRPV1, however, have scarcely been explored. Therefore, we investigated if CB and TRPV1 receptors located in the vmPFC would be involved in the behavioral changes induced by the stress of the forced swim test (FST). Rats with cannulae implanted into the vmPFC were given the dual blocker of TRPV1 receptors and fatty acid amide hydrolase (FAAH), Arachidonyl serotonin (AA-5HT, 0.125/0.25/0.5nmol), TRPV1 antagonist, SB366791 (0.5/1/10nmol), FAAH inhibitor, URB597 (0.001/0.01/0.1/1nmol), or vehicle and were submitted to the FST, or to the open-field test. Another group received intra-vmPFC injection of SB366791 or vehicle, followed by a second injection of URB597 or vehicle, and was submitted to the FST. Lastly, a group received intra-vmPFC injection of a CB antagonist, in sub-effective dose or vehicle, followed by AA-5HT, SB366791 or vehicle. The results showed that AA-5HT, SB366791 and URB597 significantly reduced the immobility time without changing the locomotor activity. Furthermore, the co-administration of URB597 and SB366791 in sub-effective doses induced an antidepressant-like effect in the FST. Additionally, the antidepressant-like effect of AA-5HT was prevented by the CB antagonist. Together, these results suggest that both, CB and TRPV1 receptors located in the vmPFC are involved in the behavioral responses to stress, although in opposite ways.
[Mh] Termos MeSH primário: Adaptação Psicológica/fisiologia
Córtex Pré-Frontal/metabolismo
Receptor CB1 de Canabinoide/metabolismo
Estresse Psicológico/metabolismo
Canais de Cátion TRPV/metabolismo
[Mh] Termos MeSH secundário: Adaptação Psicológica/efeitos dos fármacos
Amidoidrolases/antagonistas & inibidores
Amidoidrolases/metabolismo
Anilidas/farmacologia
Animais
Antidepressivos/farmacologia
Ácidos Araquidônicos/farmacologia
Benzamidas/farmacologia
Carbamatos/farmacologia
Cinamatos/farmacologia
Masculino
Atividade Motora/efeitos dos fármacos
Atividade Motora/fisiologia
Neurotransmissores/farmacologia
Córtex Pré-Frontal/efeitos dos fármacos
Ratos Wistar
Serotonina/análogos & derivados
Serotonina/farmacologia
Canais de Cátion TRPV/antagonistas & inibidores
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Anilides); 0 (Antidepressive Agents); 0 (Arachidonic Acids); 0 (Benzamides); 0 (Carbamates); 0 (Cinnamates); 0 (Cnr1 protein, rat); 0 (N-(3-methoxyphenyl)-4-chlorocinnamanilide); 0 (Neurotransmitter Agents); 0 (Receptor, Cannabinoid, CB1); 0 (TRPV Cation Channels); 0 (Trpv1 protein, rat); 0 (arachidonyl serotonin); 0 (cyclohexyl carbamic acid 3'-carbamoylbiphenyl-3-yl ester); 333DO1RDJY (Serotonin); EC 3.5.- (Amidohydrolases); EC 3.5.1.- (fatty-acid amide hydrolase)
[Em] Mês de entrada:1711
[Cu] Atualização por classe:171224
[Lr] Data última revisão:
171224
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:161025
[St] Status:MEDLINE


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[PMID]:28456308
[Au] Autor:Mou X; Yuan GR; Jiang HB; Liu Z; Wang JJ
[Ad] Endereço:Key Laboratory of Entomology and Pest Control Engineering, College of Plant Protection, Southwest University, Chongqing 400716, People's Republic of China.
[Ti] Título:Functional characterization of two acetylcholinesterase genes in the brown citrus aphid, Aphis (Toxoptera) citricidus (Kirkaldy), using heterologous expression and RNA interference.
[So] Source:Pestic Biochem Physiol;138:76-83, 2017 May.
[Is] ISSN:1095-9939
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Acetylcholinesterase (AChE) is the primary target of organophosphate- and carbamate-based insecticides. We sequenced the full-length cDNAs of two AChE genes from the brown citrus aphid Aphis (Toxoptera) citricidus (Kirkaldy). These two genes, Tcace1 and Tcace2, which encode TcAChE1 and TcAChE2, respectively, had a shared amino acid identity of 29% and were highly similar to other insect ace1 and ace2 genes, respectively, having specific functional motifs. Potential differences in enzymatic function were characterized by the heterologous expression of the two genes using a baculovirus system in Sf9 insect cells. Both of the recombinant AChEs had high specific activities for three typical substrates, acetylthiocholine iodide, butyrylthiocholine iodide, and propinylthiocholine iodide. TcAChE1 had a lower Michaelis-Menten constant value and a higher maximal reaction velocity than recombinant TcAChE2, indicating a higher affinity for substrates and greater catalytic efficiency, respectively. Bioassays showed a greater sensitivity of recombinant TcAChE1 to the 10 tested insecticides. Silencing of Tcace1 and Tcace2 by RNA interference significantly increased the susceptibility of A. citricidus to malathion and carbaryl; however, silencing Tcace1 resulted in a higher mortality rate than silencing Tcace2. Additionally, the specific enzyme activity decreased more after silencing Tcace1 than after silencing Tcace2. Thus, TcAChE1 plays a major role in postsynaptic neurotransmission in A. citricidus.
[Mh] Termos MeSH primário: Acetilcolinesterase/metabolismo
Afídeos/enzimologia
Regulação Enzimológica da Expressão Gênica/fisiologia
[Mh] Termos MeSH secundário: Acetilcolinesterase/genética
Sequência de Aminoácidos
Animais
Afídeos/genética
Afídeos/metabolismo
Carbamatos/farmacologia
Clonagem Molecular
DNA Complementar
Resistência a Inseticidas/genética
Inseticidas/farmacologia
Organofosfatos/farmacologia
Filogenia
Interferência de RNA
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Carbamates); 0 (DNA, Complementary); 0 (Insecticides); 0 (Organophosphates); EC 3.1.1.7 (Acetylcholinesterase)
[Em] Mês de entrada:1711
[Cu] Atualização por classe:171128
[Lr] Data última revisão:
171128
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170501
[St] Status:MEDLINE


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[PMID]:28929747
[Au] Autor:Hopkins DH; Fraser NJ; Mabbitt PD; Carr PD; Oakeshott JG; Jackson CJ
[Ad] Endereço:Research School of Chemistry, Australian National University , Canberra, Australian Capital Territory 0200, Australia.
[Ti] Título:Structure of an Insecticide Sequestering Carboxylesterase from the Disease Vector Culex quinquefasciatus: What Makes an Enzyme a Good Insecticide Sponge?
[So] Source:Biochemistry;56(41):5512-5525, 2017 Oct 17.
[Is] ISSN:1520-4995
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Carboxylesterase (CBE)-mediated metabolic resistance to organophosphate and carbamate insecticides is a major problem for the control of insect disease vectors, such as the mosquito. The most common mechanism involves overexpression of CBEs that bind to the insecticide with high affinity, thereby sequestering them before they can interact with their target. However, the absence of any structure for an insecticide-sequestering CBE limits our understanding of the molecular basis for this process. We present the first structure of a CBE involved in sequestration, Cqestß2 , from the mosquito disease vector Culex quinquefasciatus. Lysine methylation was used to obtain the crystal structure of Cqestß2 , which adopts a canonical α/ß-hydrolase fold that has high similarity to the target of organophosphate and carbamate insecticides, acetylcholinesterase. Sequence similarity networks of the insect carboxyl/cholinesterase family demonstrate that CBEs associated with metabolic insecticide resistance across many species share a level of similarity that distinguishes them from a variety of other classes. This is further emphasized by the structural similarities and differences in the binding pocket and active site residues of Cqestß2 and other insect carboxyl/cholinesterases. Stopped-flow and steady-state inhibition studies support a major role for Cqestß2 in organophosphate resistance and a minor role in carbamate resistance. Comparison with another isoform associated with insecticide resistance, Cqestß1, showed both enzymes have similar affinity to insecticides, despite 16 amino acid differences between the two proteins. This provides a molecular understanding of pesticide sequestration by insect CBEs and could facilitate the design of CBE-specific inhibitors to circumvent this resistance mechanism in the future.
[Mh] Termos MeSH primário: Carboxilesterase/metabolismo
Culex/enzimologia
Proteínas de Insetos/metabolismo
Inseticidas/metabolismo
Modelos Moleculares
[Mh] Termos MeSH secundário: Substituição de Aminoácidos
Animais
Sítios de Ligação
Carbamatos/química
Carbamatos/metabolismo
Carboxilesterase/química
Carboxilesterase/genética
Domínio Catalítico
Cristalografia por Raios X
Proteínas de Insetos/química
Proteínas de Insetos/genética
Inseticidas/química
Cinética
Ligantes
Conformação Molecular
Mutação
Organofosfatos/química
Organofosfatos/metabolismo
Filogenia
Conformação Proteica
Dobramento de Proteína
Proteínas Recombinantes/química
Proteínas Recombinantes/metabolismo
Especificidade da Espécie
Umbeliferonas/química
Umbeliferonas/metabolismo
[Pt] Tipo de publicação:COMPARATIVE STUDY; JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Carbamates); 0 (Insect Proteins); 0 (Insecticides); 0 (Ligands); 0 (Organophosphates); 0 (Recombinant Proteins); 0 (Umbelliferones); EC 3.1.1.1 (Carboxylesterase)
[Em] Mês de entrada:1710
[Cu] Atualização por classe:171024
[Lr] Data última revisão:
171024
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170921
[St] Status:MEDLINE
[do] DOI:10.1021/acs.biochem.7b00774



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