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[PMID]:28468238
[Au] Autor:Oka S; Kanagawa M; Doi Y; Schuster DM; Goodman MM; Yoshimura H
[Ad] Endereço:Research Center, Nihon Medi-Physics Co., Ltd., 3-1 Kitasode, Sodegaura, Chiba 299-0266, Japan. shuntaro_oka@nmp.co.jp.
[Ti] Título:Fasting Enhances the Contrast of Bone Metastatic Lesions in F-Fluciclovine-PET: Preclinical Study Using a Rat Model of Mixed Osteolytic/Osteoblastic Bone Metastases.
[So] Source:Int J Mol Sci;18(5), 2017 Apr 29.
[Is] ISSN:1422-0067
[Cp] País de publicação:Switzerland
[La] Idioma:eng
[Ab] Resumo:F-fluciclovine ( -1-amino-3- F-fluorocyclobutanecarboxylic acid) is an amino acid positron emission tomography (PET) tracer used for cancer staging (e.g., prostate and breast). Patients scheduled to undergo amino acid-PET are usually required to fast before PET tracer administration. However, there have been no reports addressing whether fasting improves fluciclovine-PET imaging. In this study, the authors investigated the influence of fasting on fluciclovine-PET using triple-tracer autoradiography with C-fluciclovine, [5,6-³H]-2-fluoro-2-deoxy-d-glucose (³H-FDG), and Tc-hydroxymethylene diphosphonate ( Tc-HMDP) in a rat breast cancer model of mixed osteolytic/osteoblastic bone metastases in which the animals fasted overnight. Lesion accumulation of each tracer was evaluated using the target-to-background (muscle) ratio. The mean ratios of C-fluciclovine in osteolytic lesions were 4.6 ± 0.8 and 2.8 ± 0.6, respectively, with and without fasting, while those for ³H-FDG were 6.9 ± 2.5 and 5.1 ± 2.0, respectively. In the peri-tumor bone formation regions (osteoblastic), where Tc-HMDP accumulated, the ratios of C-fluciclovine were 4.3 ± 1.4 and 2.4 ± 0.7, respectively, and those of ³H-FDG were 6.2 ± 3.8 and 3.3 ± 2.2, respectively, with and without fasting. These results suggest that fasting before F-fluciclovine-PET improves the contrast between osteolytic and osteoblastic bone metastatic lesions and background, as well as F-FDG-PET.
[Mh] Termos MeSH primário: Neoplasias Ósseas/diagnóstico por imagem
Neoplasias Ósseas/secundário
Osso e Ossos/diagnóstico por imagem
Ácidos Carboxílicos/análise
Meios de Contraste/análise
Ciclobutanos/análise
Tomografia por Emissão de Pósitrons/métodos
[Mh] Termos MeSH secundário: Animais
Neoplasias da Mama/diagnóstico por imagem
Linhagem Celular Tumoral
Jejum
Feminino
Fluordesoxiglucose F18/análise
Masculino
Ratos
Ratos Sprague-Dawley
Medronato de Tecnécio Tc 99m/análogos & derivados
Medronato de Tecnécio Tc 99m/análise
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Carboxylic Acids); 0 (Contrast Media); 0 (Cyclobutanes); 0Z5B2CJX4D (Fluorodeoxyglucose F18); 38R1Q0L1ZE (fluciclovine F-18); 72945-61-0 (technetium Tc 99m hydroxymethylene diphosphonate); X89XV46R07 (Technetium Tc 99m Medronate)
[Em] Mês de entrada:1802
[Cu] Atualização por classe:180221
[Lr] Data última revisão:
180221
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170505
[St] Status:MEDLINE


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[PMID]:28448885
[Au] Autor:Mansour MF; Zhu P; Van Schepdael A; Adams E
[Ad] Endereço:KU Leuven, University of Leuven, Department of Pharmaceutical and Pharmacological Sciences, Pharmaceutical Analysis, Leuven, Belgium; National Organization for Drug Control and Research, Giza, Egypt.
[Ti] Título:Development and validation of a liquid chromatographic method for the analysis of squaric acid dibutyl ester and its impurities.
[So] Source:J Pharm Biomed Anal;141:165-172, 2017 Jul 15.
[Is] ISSN:1873-264X
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:A simple, fast and selective stability indicating liquid chromatographic method has been described for the simultaneous determination of squaric acid dibutyl ester and its impurities. The chromatographic separation was achieved on a C column (250mm×4.6mm i.d., 5µm) using a mobile phase consisting of 0.15% phosphoric acid - acetonitrile - methanol (30:60:10, v/v/v). Isocratic elution was performed at a flow rate of 1.0mLmin . The analytes were detected by UV at 252nm. The method was validated according to the ICH guidelines and satisfactory results were obtained. The specificity of the developed method was tested using forced degradation solutions of the drug substance. Characterization of squaric acid dibutyl ester and its forced degradation products was achieved by coupling mass spectrometry (MS) to the liquid chromatographic (LC) system. The method was successfully applied for quality control purposes including assay and determination of related compounds as required by regulatory guidelines to ensure its safety and efficacy since no monograph is available in official compendia.
[Mh] Termos MeSH primário: Ciclobutanos/análise
[Mh] Termos MeSH secundário: Cromatografia Líquida de Alta Pressão
Cromatografia Líquida
Estabilidade de Medicamentos
Reprodutibilidade dos Testes
[Pt] Tipo de publicação:JOURNAL ARTICLE; VALIDATION STUDIES
[Nm] Nome de substância:
0 (Cyclobutanes); 4RTO57VG65 (squaric acid dibutyl ester)
[Em] Mês de entrada:1801
[Cu] Atualização por classe:180125
[Lr] Data última revisão:
180125
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170428
[St] Status:MEDLINE


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[PMID]:28807437
[Au] Autor:Magalhães ÁF; Graça VC; Calhelha RC; Ferreira ICFR; Santos PF
[Ad] Endereço:Chemistry Dep. and Chemistry Center - Vila Real (CQ-VR), University of Trás-os-Montes and Alto Douro, 5001-801 Vila Real, Portugal.
[Ti] Título:Aminosquaraines as potential photodynamic agents: Synthesis and evaluation of in vitro cytotoxicity.
[So] Source:Bioorg Med Chem Lett;27(18):4467-4470, 2017 09 15.
[Is] ISSN:1464-3405
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:The synthesis of several aminosquaraine cationic dyes displaying strong absorption within the so-called phototherapeutic window (650-850nm) is described. Their cytotoxicity, under dark and illuminated conditions, was tested against several human tumor cell lines (breast, lung, cervical and hepatocellular carcinomas) and non-tumor porcine liver primary cells. All compounds showed to inhibit the growth of the tumor cells upon irradiation more than in the absence of light, in more or less extension, clearly exhibiting photodynamic activity. The photosensitizing ability against some cell lines, together with the low toxicity for the non-tumor primary PLP2 cells displayed by some of the compounds synthetized, turns them into potential candidates as photosensitizers for PDT.
[Mh] Termos MeSH primário: Antineoplásicos/farmacologia
Ciclobutanos/farmacologia
Fenóis/farmacologia
Fármacos Fotossensibilizantes/farmacologia
[Mh] Termos MeSH secundário: Animais
Antineoplásicos/síntese química
Antineoplásicos/química
Linhagem Celular
Proliferação Celular/efeitos dos fármacos
Ciclobutanos/síntese química
Ciclobutanos/química
Relação Dose-Resposta a Droga
Ensaios de Seleção de Medicamentos Antitumorais
Seres Humanos
Estrutura Molecular
Fenóis/síntese química
Fenóis/química
Fotoquimioterapia
Fármacos Fotossensibilizantes/síntese química
Fármacos Fotossensibilizantes/química
Relação Estrutura-Atividade
Suínos
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Antineoplastic Agents); 0 (Cyclobutanes); 0 (Phenols); 0 (Photosensitizing Agents); 0 (squaraine)
[Em] Mês de entrada:1709
[Cu] Atualização por classe:171125
[Lr] Data última revisão:
171125
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170816
[St] Status:MEDLINE


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[PMID]:28797798
[Au] Autor:Tian LW; Feng Y; Tran TD; Shimizu Y; Pfeifer T; Vu HT; Quinn RJ
[Ad] Endereço:Griffith Institute for Drug Discovery, Griffith University, Brisbane QLD 4111, Australia.
[Ti] Título:Achyrodimer F, a tyrosyl-DNA phosphodiesterase I inhibitor from an Australian fungus of the family Cortinariaceae.
[So] Source:Bioorg Med Chem Lett;27(17):4007-4010, 2017 09 01.
[Is] ISSN:1464-3405
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Mass-guided isolation of the dichloromethane/methanol extracts from a specimen of teleomorphic fungus of the family Cortinariaceae resulted in the identification of a new dimeric cyclobutane metabolite, achyrodimer F (1), along with the monomers hispidin (2) and bisnoryangonin (3). Their structures were determined by NMR and MS data analyses. Density Function Theory (DFT) NMR calculations was employed to confirm the chemical structure of achyrodimer F. Compound 1 inhibited tyrosyl-DNA phosphodiesterase I with an IC value of 1µM.
[Mh] Termos MeSH primário: Agaricales/química
Ciclobutanos/farmacologia
Inibidores de Fosfodiesterase/farmacologia
Diester Fosfórico Hidrolases/metabolismo
Pironas/farmacologia
[Mh] Termos MeSH secundário: Austrália
Ciclobutanos/química
Ciclobutanos/isolamento & purificação
Relação Dose-Resposta a Droga
Seres Humanos
Estrutura Molecular
Inibidores de Fosfodiesterase/química
Inibidores de Fosfodiesterase/isolamento & purificação
Pironas/química
Pironas/isolamento & purificação
Relação Estrutura-Atividade
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Cyclobutanes); 0 (Phosphodiesterase Inhibitors); 0 (Pyrones); 0 (achyrodimer F); EC 3.1.4.- (Phosphoric Diester Hydrolases); EC 3.1.4.- (TDP1 protein, human)
[Em] Mês de entrada:1709
[Cu] Atualização por classe:171125
[Lr] Data última revisão:
171125
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170812
[St] Status:MEDLINE


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[PMID]:28724846
[Au] Autor:Al-Tahami BAM; Al-Safi Ismail AA; Sanip Z; Yusoff Z; Shihabudin TMT; Singh TSP; Rasool AHG
[Ad] Endereço:Pharmacology Vascular Laboratory, School of Medical Sciences, Universiti Sains Malaysia.
[Ti] Título:Metabolic and Inflammatory Changes with Orlistat and Sibutramine Treatment in Obese Malaysian Subjects.
[So] Source:J Nippon Med Sch;84(3):125-132, 2017.
[Is] ISSN:1347-3409
[Cp] País de publicação:Japan
[La] Idioma:eng
[Ab] Resumo:INTRODUCTION: Obesity is associated with numerous health problems, particularly metabolic and cardiovascular complications. This study aimed to assess the effects that, nine months of pharmacological intervention with orlistat or sibutramine, on obese Malaysians' body weight and compositions, metabolic profiles and inflammatory marker. METHODS: Seventy-six obese subjects were randomly placed into two groups. The first group received three daily 120 mg dosages of orlistat for nine months (n=39), and the second group received a once daily 10 or 15 mg dosage of sibutramine for nine months (n=37). Baseline measurements for weight, body mass index (BMI), waist circumference (WC), body fat percentage (BF), visceral fat (VF), adiponectin, fasting plasma glucose (FPG), fasting insulin, pancreatic B cell secretory capacity (HOMA%B), insulin sensitivity (HOMA%S), insulin resistance (HOMA-IR) and serum high sensitivity C-reactive protein (hs-CRP) were performed and repeated during the sixth and ninth months of treatment. RESULTS: Twenty-four subjects completed the trial in both groups. For both groups, weight, BMI, WC, BF, VF, HOMA-IR and hs-CRP were significantly lower at the end of the nine month intervention. However, there were no significant differences between the two groups for these parameters with nine months treatment. There was a significant decrease in FPG in orlistat group; while fasting insulin and HOMA%B reduced in sibutramine group. For both groups, there were also significant increases in adiponectin levels and HOMA%S at the end of the nine month intervention. CONCLUSION: Nine months of treatment with orlistat and sibutramine not only reduced weight but also significantly improved BMI, WC, BF, VF, FPG, adiponectin, fasting insulin, HOMA%B, HOMA%S, HOMA-IR and hs-CRP. These improvements could prove useful in the reduction of metabolic and cardiovascular risks in obese subjects.
[Mh] Termos MeSH primário: Ciclobutanos/administração & dosagem
Lactonas/administração & dosagem
Obesidade/tratamento farmacológico
Obesidade/metabolismo
[Mh] Termos MeSH secundário: Adiponectina/metabolismo
Adolescente
Adulto
Idoso
Grupo com Ancestrais do Continente Asiático
Glicemia/metabolismo
Distribuição da Gordura Corporal
Índice de Massa Corporal
Proteína C-Reativa/metabolismo
Doenças Cardiovasculares/etiologia
Doenças Cardiovasculares/prevenção & controle
Ciclobutanos/farmacologia
Jejum/sangue
Seres Humanos
Insulina/metabolismo
Resistência à Insulina
Gordura Intra-Abdominal/metabolismo
Lactonas/farmacologia
Malásia
Meia-Idade
Obesidade/complicações
Obesidade/fisiopatologia
Risco
Resultado do Tratamento
Circunferência da Cintura
Adulto Jovem
[Pt] Tipo de publicação:JOURNAL ARTICLE; RANDOMIZED CONTROLLED TRIAL
[Nm] Nome de substância:
0 (Adiponectin); 0 (Blood Glucose); 0 (Cyclobutanes); 0 (Insulin); 0 (Lactones); 9007-41-4 (C-Reactive Protein); 95M8R751W8 (orlistat); WV5EC51866 (sibutramine)
[Em] Mês de entrada:1710
[Cu] Atualização por classe:171031
[Lr] Data última revisão:
171031
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170721
[St] Status:MEDLINE
[do] DOI:10.1272/jnms.84.125


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[PMID]:28723805
[Au] Autor:Cao CL; Duan PY; Zhang WJ; Li L; Qu FZ; Sun B; Wang G
[Ad] Endereço:Department of Pancreatic and Biliary Surgery, The First Affiliated Hospital of Harbin Medical University, Harbin, Heilongjiang Province, China.
[Ti] Título:Acute pancreatitis induced by etoposide-lobaplatin combination chemotherapy used for the treatment of lung cancer: A case report and literature review.
[So] Source:Medicine (Baltimore);96(29):e7601, 2017 Jul.
[Is] ISSN:1536-5964
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:RATIONALE: Drug-induced pancreatitis (DIP) is a rare type of pancreatitis that is not usually observed in the clinical practice. It is generally difficult to distinguish from acute pancreatitis (AP) induced by other causes. PATIENT CONCERNS: Here, we report a 62-year-old Chinese female patient with "small cell lung cancer" as the initial presentation. Because the patient could not bear the surgical treatment, the chemotherapy composed of lobaplatin and etoposide was performed. Three days later, the patient displayed sudden abdominal pain, distension, nausea, and vomiting without obvious inducements. Laboratory tests showed that the levels of serum and urine amylase were enhanced; abdominal computed tomography (CT) result showed the enlargement of the pancreas, peripancreatic effusion, and a rough edge, which suggested the diagnosis of AP. The patient had no history of biliary tract disease, alcoholism, binge overeating, hyperlipidemia, and hereditary pancreatitis. DIAGNOSES: The patient was diagnosed with DIP. INTERVENTIONS: The chemotherapy was stopped at once and we performed fluid resuscitation, pain alleviation, prophylactic antibiotics, and nutritional support, etc on the patient. Later, the patient's clinical symptoms were obviously relieved, and she recovered successfully. OUTCOMES: The chemotherapy was continued, but later, the patient showed abdominal pain, distension, nausea, and vomiting again. The levels of serum amylase and urine amylase were enhanced again. Further imaging examination strongly indicated the recurrence of AP. LESSONS: We should raise awareness of the clinicians regarding DIP, thereby enabling its timely diagnosis and accurate treatment, as well as promoting the rational and safe use of drugs.
[Mh] Termos MeSH primário: Antineoplásicos/efeitos adversos
Ciclobutanos/efeitos adversos
Etoposídeo/efeitos adversos
Neoplasias Pulmonares/tratamento farmacológico
Compostos Organoplatínicos/efeitos adversos
Pancreatite/induzido quimicamente
Pancreatite/diagnóstico
[Mh] Termos MeSH secundário: Doença Aguda
Antineoplásicos/uso terapêutico
Ciclobutanos/uso terapêutico
Diagnóstico Diferencial
Quimioterapia Combinada/efeitos adversos
Etoposídeo/uso terapêutico
Feminino
Seres Humanos
Meia-Idade
Compostos Organoplatínicos/uso terapêutico
Carcinoma de Pequenas Células do Pulmão/tratamento farmacológico
[Pt] Tipo de publicação:CASE REPORTS; JOURNAL ARTICLE; REVIEW
[Nm] Nome de substância:
0 (Antineoplastic Agents); 0 (Cyclobutanes); 0 (Organoplatinum Compounds); 6PLQ3CP4P3 (Etoposide); OX5XK1JD8C (lobaplatin)
[Em] Mês de entrada:1708
[Cu] Atualização por classe:170808
[Lr] Data última revisão:
170808
[Sb] Subgrupo de revista:AIM; IM
[Da] Data de entrada para processamento:170721
[St] Status:MEDLINE
[do] DOI:10.1097/MD.0000000000007601


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[PMID]:28723799
[Au] Autor:Zhao GS; Liu Y; Zhang Q; Li C; Zhang YW; Ren ZZ; Zhou J; Zhang M
[Ad] Endereço:aDepartment of Interventional Therapy, Affiliated Zhongshan Hospital of Dalian University, Dalian, Liaoning bDepartment of Radiology, The First Affiliated Hospital of Xi'an Jiaotong University, Xi'an, Shaanxi cCentral Laboratory, Affiliated Zhongshan Hospital of Dalian University, Dalian, Liaoning dDepartment of Hepatobiliary Intervention, Beijing Tsinghua Changgung Hospital, Changping, Beijing, China.
[Ti] Título:Transarterial chemoembolization combined with Huaier granule for the treatment of primary hepatic carcinoma: Safety and efficacy.
[So] Source:Medicine (Baltimore);96(29):e7589, 2017 Jul.
[Is] ISSN:1536-5964
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:To evaluate the safety and efficacy of transarterial arterial chemoembolization (TACE) with gelatin sponge particles (GSPs-TACE) and Huaier granule to treat primary hepatic carcinoma (PHC).A series of 62 patients with PHC were included between June 2009 and December 2011, and randomly assigned to a control (n = 31) or an experimental group (n = 31). The control patients received TACE with 350 to 560 µm GSPs plus lobaplatin chemotherapy. Patients in the experimental group received TACE plus Huaier granule. Treatment safety and mid-to-long-term efficacy were evaluated.Follow-up ranged from 12 to 24 months with a mean of 28.7 months. The 6- and 12-month overall survivals were 100% and 93.5% in the experimental group and 90.3% and 80.6% in control group, respectively. The difference in overall survival at 12 months was significant (χ = 5.213, P < .05), but the difference in median survival in the experimental group (20.6 months) and control group (17.1 months) patients was not significant (χ = 0.745, P > .05). The number of TACE procedures in the experimental group (2.9 ±â€Š8.7) and control group (4.1 ±â€Š7.3) patients was significantly different (χ = 7.262, P < .05). The 6-month (87.1% vs. 73.3%, χ = 5.945) and 12-month (72.4% vs. 64.3%, χ = 6.384) tumor objective response rates in the experimental and control groups were significantly different (P < .05). There were no statistically significant differences in the occurrence of treatment-related adverse reactions in the 2 groups.Transarterial chemoembolization with GSPs and Huaier granule was safe and effective for treating PHC patients.
[Mh] Termos MeSH primário: Antineoplásicos/uso terapêutico
Carcinoma Hepatocelular/terapia
Quimioembolização Terapêutica
Misturas Complexas/uso terapêutico
Medicamentos de Ervas Chinesas/uso terapêutico
[Mh] Termos MeSH secundário: Idoso
Antineoplásicos/efeitos adversos
Carcinoma Hepatocelular/patologia
Quimioembolização Terapêutica/efeitos adversos
Terapia Combinada/efeitos adversos
Ciclobutanos/uso terapêutico
Medicamentos de Ervas Chinesas/efeitos adversos
Feminino
Seguimentos
Seres Humanos
Estimativa de Kaplan-Meier
Masculino
Meia-Idade
Gradação de Tumores
Compostos Organoplatínicos/uso terapêutico
Fatores de Tempo
Resultado do Tratamento
[Pt] Tipo de publicação:JOURNAL ARTICLE; RANDOMIZED CONTROLLED TRIAL
[Nm] Nome de substância:
0 (Antineoplastic Agents); 0 (Complex Mixtures); 0 (Cyclobutanes); 0 (Drugs, Chinese Herbal); 0 (Organoplatinum Compounds); 0 (huaier); OX5XK1JD8C (lobaplatin)
[Em] Mês de entrada:1708
[Cu] Atualização por classe:170808
[Lr] Data última revisão:
170808
[Sb] Subgrupo de revista:AIM; IM
[Da] Data de entrada para processamento:170721
[St] Status:MEDLINE
[do] DOI:10.1097/MD.0000000000007589


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[PMID]:28632393
[Au] Autor:Hsu HC; Tong S; Zhou Y; Elmes MW; Yan S; Kaczocha M; Deutsch DG; Rizzo RC; Ojima I; Li H
[Ad] Endereço:Cryo-EM Structural Biology Laboratory, Van Andel Research Institute , Grand Rapids, Michigan 49503, United States.
[Ti] Título:The Antinociceptive Agent SBFI-26 Binds to Anandamide Transporters FABP5 and FABP7 at Two Different Sites.
[So] Source:Biochemistry;56(27):3454-3462, 2017 Jul 11.
[Is] ISSN:1520-4995
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Human FABP5 and FABP7 are intracellular endocannabinoid transporters. SBFI-26 is an α-truxillic acid 1-naphthyl monoester that competitively inhibits the activities of FABP5 and FABP7 and produces antinociceptive and anti-inflammatory effects in mice. The synthesis of SBFI-26 yields several stereoisomers, and it is not known how the inhibitor binds the transporters. Here we report co-crystal structures of SBFI-26 in complex with human FABP5 and FABP7 at 2.2 and 1.9 Å resolution, respectively. We found that only (S)-SBFI-26 was present in the crystal structures. The inhibitor largely mimics the fatty acid binding pattern, but it also has several unique interactions. Notably, the FABP7 complex corroborates key aspects of the ligand binding pose at the canonical site previously predicted by virtual screening. In FABP5, SBFI-26 was unexpectedly found to bind at the substrate entry portal region in addition to binding at the canonical ligand-binding pocket. Our structural and binding energy analyses indicate that both R and S forms appear to bind the transporter equally well. We suggest that the S enantiomer observed in the crystal structures may be a result of the crystallization process selectively incorporating the (S)-SBFI-26-FABP complexes into the growing lattice, or that the S enantiomer may bind to the portal site more rapidly than to the canonical site, leading to an increased local concentration of the S enantiomer for binding to the canonical site. Our work reveals two binding poses of SBFI-26 in its target transporters. This knowledge will guide the development of more potent FABP inhibitors based upon the SBFI-26 scaffold.
[Mh] Termos MeSH primário: Analgésicos/metabolismo
Ciclobutanos/metabolismo
Ácidos Dicarboxílicos/metabolismo
Proteína 7 de Ligação a Ácidos Graxos/metabolismo
Proteínas de Ligação a Ácido Graxo/metabolismo
Modelos Moleculares
Proteínas Supressoras de Tumor/metabolismo
[Mh] Termos MeSH secundário: Analgésicos/química
Analgésicos/farmacologia
Animais
Anti-Inflamatórios não Esteroides/química
Anti-Inflamatórios não Esteroides/metabolismo
Anti-Inflamatórios não Esteroides/farmacologia
Apoproteínas/antagonistas & inibidores
Apoproteínas/química
Apoproteínas/genética
Apoproteínas/metabolismo
Sítios de Ligação
Domínio Catalítico
Biologia Computacional
Cristalografia por Raios X
Ciclobutanos/química
Ciclobutanos/farmacologia
Ácidos Dicarboxílicos/química
Ácidos Dicarboxílicos/farmacologia
Proteína 7 de Ligação a Ácidos Graxos/antagonistas & inibidores
Proteína 7 de Ligação a Ácidos Graxos/química
Proteína 7 de Ligação a Ácidos Graxos/genética
Proteínas de Ligação a Ácido Graxo/antagonistas & inibidores
Proteínas de Ligação a Ácido Graxo/química
Proteínas de Ligação a Ácido Graxo/genética
Seres Humanos
Ligantes
Camundongos
Conformação Molecular
Simulação de Acoplamento Molecular
Simulação de Dinâmica Molecular
Conformação Proteica
Proteínas Recombinantes
Estereoisomerismo
Proteínas Supressoras de Tumor/antagonistas & inibidores
Proteínas Supressoras de Tumor/química
Proteínas Supressoras de Tumor/genética
[Pt] Tipo de publicação:COMPARATIVE STUDY; JOURNAL ARTICLE
[Nm] Nome de substância:
0 (1-naphthyl alpha-truxillate); 0 (Analgesics); 0 (Anti-Inflammatory Agents, Non-Steroidal); 0 (Apoproteins); 0 (Cyclobutanes); 0 (Dicarboxylic Acids); 0 (FABP5 protein, human); 0 (FABP7 protein, human); 0 (Fatty Acid-Binding Protein 7); 0 (Fatty Acid-Binding Proteins); 0 (Ligands); 0 (Recombinant Proteins); 0 (Tumor Suppressor Proteins)
[Em] Mês de entrada:1707
[Cu] Atualização por classe:171102
[Lr] Data última revisão:
171102
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170621
[St] Status:MEDLINE
[do] DOI:10.1021/acs.biochem.7b00194


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[PMID]:28571975
[Au] Autor:Friães S; Silva AM; Boto RE; Ferreira D; Fernandes JR; Souto EB; Almeida P; Ferreira LFV; Reis LV
[Ad] Endereço:Department of Chemistry and CQ-VR, UTAD, Quinta de Prados, 5001-801 Vila Real, Portugal; Centre for Research and Technology of Agro-Environmental and Biological Sciences, CITAB, UTAD, Quinta de Prados, 5001-801 Vila Real, Portugal.
[Ti] Título:Synthesis, spectroscopic characterization and biological evaluation of unsymmetrical aminosquarylium cyanine dyes.
[So] Source:Bioorg Med Chem;25(14):3803-3814, 2017 Jul 15.
[Is] ISSN:1464-3391
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:New unsymmetrical aminosquarylium cyanine dyes were synthesized and their potential as photosensitizers evaluated. New dyes, derived from benzothiazole and quinoline, were prepared by nucleophilic substitution of the corresponding O-methylated, the key intermediate that was obtained by methylation with CF SO CH of the related zwitterionic unsymmetrical dye, with ammonia and methylamine, respectively. All three news dyes herein described displayed intense and narrow bands in the Vis/NIR region (693-714nm) and their singlet oxygen formation quantum yields ranged from 0.03 to 0.05. In vitro toxicity, in Caco-2 and HepG2 cells, indicated that dark toxicity was absent for concentrations up to 5µM (for the less active dye) or up to 1µM (for the two more active dyes). The three dyes present potential as photosensitizers, differing in irradiation conditions and period of incubation in the presence of irradiated dye. The less active dye needs a longer irradiation period to exhibit phototoxicity which is only evident after longer period of contact with cells (24h). However, the remaining two more active dyes produce higher phototoxicity, even at shorter incubation periods (1h), with shorter irradiation time (7min). Although in different extents, these dyes show promising in vitro results as photosensitizers.
[Mh] Termos MeSH primário: Carbocianinas/química
Ciclobutanos/química
Corantes Fluorescentes/síntese química
Fenóis/química
Fármacos Fotossensibilizantes/síntese química
[Mh] Termos MeSH secundário: Células CACO-2
Carbocianinas/síntese química
Carbocianinas/farmacologia
Sobrevivência Celular/efeitos dos fármacos
Sobrevivência Celular/efeitos da radiação
Ciclobutanos/síntese química
Ciclobutanos/toxicidade
Corantes Fluorescentes/química
Corantes Fluorescentes/farmacologia
Células Hep G2
Seres Humanos
Luz
Fenóis/síntese química
Fenóis/toxicidade
Fármacos Fotossensibilizantes/química
Fármacos Fotossensibilizantes/farmacologia
Oxigênio Singlete/metabolismo
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Carbocyanines); 0 (Cyclobutanes); 0 (Fluorescent Dyes); 0 (Phenols); 0 (Photosensitizing Agents); 0 (squaraine); 17778-80-2 (Singlet Oxygen)
[Em] Mês de entrada:1710
[Cu] Atualização por classe:171002
[Lr] Data última revisão:
171002
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170603
[St] Status:MEDLINE


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[PMID]:28489121
[Au] Autor:Lucchetta RC; Riveros BS; Pontarolo R; Radominski RB; Otuki MF; Fernandez-Llimos F; Correr CJ
[Ad] Endereço:Laboratory of Clinical Services and Evidence in Health, Pharmacy Department, Universidade Federal do Paraná (UFPR), Curitiba, PR, Brazil.
[Ti] Título:Diethylpropion and mazindol: An end to the discussion?
[So] Source:Rev Assoc Med Bras (1992);63(3):203-206, 2017 Mar.
[Is] ISSN:1806-9282
[Cp] País de publicação:Brazil
[La] Idioma:eng
[Ab] Resumo:Antiobesity pharmacotherapy remains the main point of disagreement among both scientists and regulators. This is probably due to small sample sizes, high levels of heterogeneity, and low methodological quality. For many years, Brazil was one of the largest consumers of appetite suppressants worldwide, with evidence of irrational use of this drug class. Therefore, the country was the scene of a debate that divided the Brazilian Health Surveillance Agency (Anvisa - Agência Nacional de Vigilância Sanitária) and medical societies over the maintenance record of diethylpropion, mazindol and fenproporex. In this context, this commentary presents new arguments to contribute to the discussion, as well as recommendations for future studies.
[Mh] Termos MeSH primário: Depressores do Apetite/uso terapêutico
Dietilpropiona/uso terapêutico
Mazindol/uso terapêutico
Obesidade/tratamento farmacológico
[Mh] Termos MeSH secundário: Anfetaminas/uso terapêutico
Brasil
Ciclobutanos/uso terapêutico
Aprovação de Drogas
Seres Humanos
Medição de Risco/tendências
Resultado do Tratamento
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Amphetamines); 0 (Appetite Depressants); 0 (Cyclobutanes); C56709M5NH (Mazindol); Q94YYU22B8 (Diethylpropion); W0194S5FOA (fenproporex); WV5EC51866 (sibutramine)
[Em] Mês de entrada:1708
[Cu] Atualização por classe:170829
[Lr] Data última revisão:
170829
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170511
[St] Status:MEDLINE



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