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[PMID]:28463421
[Au] Autor:Wu C; Ichinose K; Choi YH; van Wezel GP
[Ad] Endereço:Molecular Biotechnology, Institute of Biology, Leiden University, Sylviusweg 72, 2333 BE, Leiden, The Netherlands.
[Ti] Título:Aromatic Polyketide GTRI-02 is a Previously Unidentified Product of the act Gene Cluster in Streptomyces coelicolor A3(2).
[So] Source:Chembiochem;18(14):1428-1434, 2017 07 18.
[Is] ISSN:1439-7633
[Cp] País de publicação:Germany
[La] Idioma:eng
[Ab] Resumo:The biosynthesis of aromatic polyketides derived from type II polyketide synthases (PKSs) is complex, and it is not uncommon that highly similar gene clusters give rise to diverse structural architectures. The act biosynthetic gene cluster (BGC) of the model actinomycete Streptomyces coelicolor A3(2) is an archetypal type II PKS. Here we show that the act BGC also specifies the aromatic polyketide GTRI-02 (1) and propose a mechanism for the biogenesis of its 3,4-dihydronaphthalen-1(2H)-one backbone. Polyketide 1 was also produced by Streptomyces sp. MBT76 after activation of the act-like qin gene cluster by overexpression of the pathway-specific activator. Mining of this strain also identified dehydroxy-GTRI-02 (2), which most likely originated from dehydration of 1 during the isolation process. This work shows that even extensively studied model gene clusters such as act of S. coelicolor can still produce new chemistry, offering new perspectives for drug discovery.
[Mh] Termos MeSH primário: Família Multigênica
Naftóis/metabolismo
Streptomyces coelicolor/genética
Streptomyces coelicolor/metabolismo
Tetra-Hidronaftalenos/metabolismo
[Mh] Termos MeSH secundário: Naftóis/química
Tetra-Hidronaftalenos/química
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (GTRI 02); 0 (Naphthols); 0 (Tetrahydronaphthalenes)
[Em] Mês de entrada:1710
[Cu] Atualização por classe:180122
[Lr] Data última revisão:
180122
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170503
[St] Status:MEDLINE
[do] DOI:10.1002/cbic.201700107


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[PMID]:28977599
[Au] Autor:Masoodi KZ; Eisermann K; Yang Z; Dar JA; Pascal LE; Nguyen M; O'Malley K; Parrinello E; Feturi FG; Kenefake AN; Nelson JB; Johnston PA; Wipf P; Wang Z
[Ad] Endereço:Department of Urology, University of Pittsburgh School of Medicine, Pittsburgh, Pennsylvania 15232.
[Ti] Título:Inhibition of Androgen Receptor Function and Level in Castration-Resistant Prostate Cancer Cells by 2-[(isoxazol-4-ylmethyl)thio]-1-(4-phenylpiperazin-1-yl)ethanone.
[So] Source:Endocrinology;158(10):3152-3161, 2017 Oct 01.
[Is] ISSN:1945-7170
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:The androgen receptor (AR) plays a critical role in the development of castration-resistant prostate cancer (CRPC) as well as in the resistance to the second-generation AR antagonist enzalutamide and the selective inhibitor of cytochrome P450 17A1 (CYP17A1) abiraterone. Novel agents targeting AR may inhibit the growth of prostate cancer cells resistant to enzalutamide and/or abiraterone. Through a high-throughput/high-content screening of a 220,000-member small molecule library, we have previously identified 2-[(isoxazol-4-ylmethyl)thio]-1-(4-phenylpiperazin-1-yl)ethanone (IMTPPE) (SID 3712502) as a novel small molecule capable of inhibiting AR transcriptional activity and protein level in C4-2 prostate cancer cells. In this study, we show that IMTPPE inhibits AR-target gene expression using real-time polymerase chain reaction, Western blot, and luciferase assays. IMTPPE inhibited proliferation of AR-positive, but not AR-negative, prostate cancer cells in culture. IMTPPE inhibited the transcriptional activity of a mutant AR lacking the ligand-binding domain (LBD), indicating that IMTPPE inhibition of AR is independent of the LBD. Furthermore, animal studies showed that IMTPPE inhibited the growth of 22Rv1 xenograft tumor, a model for enzalutamide-resistant prostate cancer. These findings suggest that IMTPPE is a potential lead compound for developing clinical candidates for the treatment of CRPC, including those resistant to enzalutamide.
[Mh] Termos MeSH primário: Antagonistas de Receptores de Andrógenos/farmacologia
Isoxazóis/farmacologia
Piperazinas/farmacologia
Neoplasias de Próstata Resistentes à Castração/química
Receptores Androgênicos/fisiologia
[Mh] Termos MeSH secundário: Animais
Sítios de Ligação/genética
Sítios de Ligação/fisiologia
Linhagem Celular Tumoral
Resistência a Medicamentos Antineoplásicos
Expressão Gênica/efeitos dos fármacos
Seres Humanos
Masculino
Camundongos
Camundongos Endogâmicos BALB C
Camundongos SCID
Feniltioidantoína/análogos & derivados
Regiões Promotoras Genéticas/efeitos dos fármacos
Isoformas de Proteínas/genética
Reação em Cadeia da Polimerase em Tempo Real
Receptores Androgênicos/análise
Receptores Androgênicos/genética
Tetra-Hidronaftalenos
Ensaios Antitumorais Modelo de Xenoenxerto
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (2-((isoxazol-4-ylmethyl)thio)-1-(4-phenylpiperazin-1-yl)ethanone); 0 (Androgen Receptor Antagonists); 0 (Isoxazoles); 0 (MDV 3100); 0 (Piperazines); 0 (Protein Isoforms); 0 (Receptors, Androgen); 0 (Tetrahydronaphthalenes); 2010-15-3 (Phenylthiohydantoin); A61RXM4375 (bexarotene)
[Em] Mês de entrada:1710
[Cu] Atualização por classe:171115
[Lr] Data última revisão:
171115
[Sb] Subgrupo de revista:AIM; IM
[Da] Data de entrada para processamento:171005
[St] Status:MEDLINE
[do] DOI:10.1210/en.2017-00408


  3 / 4115 MEDLINE  
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[PMID]:28858135
[Au] Autor:Fang BX; Wang LH; Liu HM; Chen FC; Liu J
[Ad] Endereço:aDepartment of Pharmacy, Dongfeng Hospital bDepartment of Pharmacy, Renmin Hospital, Hubei University of Medicine, Shiyan, Hubei, P.R. China.
[Ti] Título:Stability study of dezocine in 0.9% sodium chloride solutions for patient-controlled analgesia administration.
[So] Source:Medicine (Baltimore);96(35):e7979, 2017 Sep.
[Is] ISSN:1536-5964
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:BACKGROUND: Dezocine, a mixed agonist/antagonist of opioid receptors, has been used in iv patient-controlled analgesia (PCA) pumps for postoperative pain control. The aim of this study was to investigate the physicochemical stability of dezocine solutions in 0.9% sodium chloride for injection for PCA administration. METHODS: Solutions of dezocine (0.3, 0.45, or 0.6 mg/mL in 0.9% sodium chloride for injection) were stored in polyolefin bags and glass bottles. Their stabilities at storage conditions of 4°C for 14 days and 25°C for 72 hours were studied. For all preparations, physical characteristics (including pH, color, and presence of precipitates) were evaluated. Each preparation of dezocine was also analyzed using a stability-indicating high-performance liquid chromatography method. A solution was considered stable if it maintained at least 90% of its initial concentration. RESULTS: No notable changes in pH, color, or precipitation were observed in any of the prepared solutions over the testing period. All formulations maintained >97% of the initial dezocine concentration under the storage conditions evaluated. CONCLUSIONS: Dezocine solutions at 0.3, 0.45, or 0.6 mg/mL in 0.9% sodium chloride for PCA administration were stable for 72 hours at 25°C and for 14 days at 4°C when packaged in polyolefin bags or glass bottles and protected from light.
[Mh] Termos MeSH primário: Analgesia Controlada pelo Paciente
Analgésicos Opioides/química
Compostos Bicíclicos Heterocíclicos com Pontes/química
Estabilidade de Medicamentos
Tetra-Hidronaftalenos/química
[Mh] Termos MeSH secundário: Analgésicos Opioides/administração & dosagem
Compostos Bicíclicos Heterocíclicos com Pontes/administração & dosagem
Cromatografia Líquida de Alta Pressão
Armazenamento de Medicamentos/métodos
Seres Humanos
Concentração de Íons de Hidrogênio
Plásticos
Polienos
Solução Salina Hipertônica
Tetra-Hidronaftalenos/administração & dosagem
Fatores de Tempo
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Analgesics, Opioid); 0 (Bridged Bicyclo Compounds, Heterocyclic); 0 (Plastics); 0 (Polyenes); 0 (Saline Solution, Hypertonic); 0 (Tetrahydronaphthalenes); 83136-87-2 (PL 732); VHX8K5SV4X (dezocine)
[Em] Mês de entrada:1709
[Cu] Atualização por classe:171116
[Lr] Data última revisão:
171116
[Sb] Subgrupo de revista:AIM; IM
[Da] Data de entrada para processamento:170901
[St] Status:MEDLINE
[do] DOI:10.1097/MD.0000000000007979


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[PMID]:28818004
[Au] Autor:Geyer J; Bogan R
[Ad] Endereço:a Alabama Neurology & Sleep Medicine and Unosano, LLC , Tuscaloosa , AL , USA.
[Ti] Título:Identification and treatment of augmentation in patients with restless legs syndrome: practical recommendations.
[So] Source:Postgrad Med;129(7):667-675, 2017 Sep.
[Is] ISSN:1941-9260
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Restless legs syndrome (RLS) is a chronic disorder causing clinically significant discomfort to approximately 3% of adults. Although RLS was first identified centuries ago, our understanding of this disorder, its causes, and its treatments is still evolving. In particular, our knowledge of the potential negative effects of RLS treatments, including dopaminergic augmentation, continues to expand. Augmentation, which refers to a paradoxical treatment-related increase in RLS symptoms, has been associated with all three dopamine agonists approved for the treatment of RLS - rotigotine, pramipexole, and ropinirole. This review presents key information on prevention and treatment of dopaminergic augmentation from the recently published consensus-based guidelines issued by the International RLS Study Group task force in conjunction with the European RLS Study Group and the RLS Foundation for first-line treatment of RLS/Willis-Ekbom disease. If dopamine agonists are used to treat RLS, it is recommended that the dosage should be kept as low as possible without exceeding the maximum dose recommended for RLS treatment. As the frequency of augmentation with the rotigotine patch may only be slightly lower than that associated with pramipexole or ropinirole, medications that are effective and have little risk of augmentation, such as alpha-2-delta ligands, may be considered for initial RLS treatment. In addition, we present our clinical experience with treating patients with dopaminergic augmentation by highlighting 2 case studies and practical considerations when treating different patient populations. Applying current RLS augmentation diagnosis and treatment guidelines, as well as collecting detailed histories of worsening RLS symptoms, is critical for patient safety and effective management of RLS augmentation.
[Mh] Termos MeSH primário: Benzotiazóis/uso terapêutico
Agonistas de Dopamina/uso terapêutico
Indóis/uso terapêutico
Ligantes
Síndrome das Pernas Inquietas/diagnóstico
Síndrome das Pernas Inquietas/tratamento farmacológico
Tetra-Hidronaftalenos/uso terapêutico
[Mh] Termos MeSH secundário: Adulto
Idoso
Idoso de 80 Anos ou mais
Benzotiazóis/efeitos adversos
Agonistas de Dopamina/efeitos adversos
Feminino
Seres Humanos
Indóis/efeitos adversos
Masculino
Meia-Idade
Tetra-Hidronaftalenos/efeitos adversos
Resultado do Tratamento
[Pt] Tipo de publicação:CASE REPORTS; JOURNAL ARTICLE; REVIEW
[Nm] Nome de substância:
0 (Benzothiazoles); 0 (Dopamine Agonists); 0 (Indoles); 0 (Ligands); 0 (Tetrahydronaphthalenes)
[Em] Mês de entrada:1709
[Cu] Atualização por classe:170906
[Lr] Data última revisão:
170906
[Sb] Subgrupo de revista:AIM; IM
[Da] Data de entrada para processamento:170819
[St] Status:MEDLINE
[do] DOI:10.1080/00325481.2017.1360747


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[PMID]:28753292
[Au] Autor:Shibahara O; Watanabe M; Yamada S; Akehi M; Sasaki T; Akahoshi A; Hanada T; Hirano H; Nakatani S; Nishioka H; Takeuchi Y; Kakuta H
[Ad] Endereço:Division of Pharmaceutical Sciences, Okayama University Graduate School of Medicine, Dentistry and Pharmaceutical Sciences , 1-1-1, Tsushima-Naka, Kita-Ku, Okayama 700-8530, Japan.
[Ti] Título:Synthesis of C-Labeled RXR Partial Agonist 1-[(3,5,5,8,8-Pentamethyl-5,6,7,8-tetrahydronaphthalen-2-yl)amino]benzotriazole-5-carboxylic Acid (CBt-PMN) by Direct [ C]Carbon Dioxide Fixation via Organolithiation of Trialkyltin Precursor and PET Imaging Thereof.
[So] Source:J Med Chem;60(16):7139-7145, 2017 Aug 24.
[Is] ISSN:1520-4804
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:The retinoid X receptor (RXR) partial agonist 1-[(3,5,5,8,8-pentamethyl-5,6,7,8-tetrahydronaphthalen-2-yl)amino]benzotriazole-5-carboxylic acid (1; CBt-PMN, E = 75%, EC = 143 nM) is a candidate for treatment of central nervous system (CNS) diseases such as Alzheimer's and Parkinson's diseases based on reports that RXR-full agonist 4-[1-(3,5,5,8,8-pentamethyl-5,6,7,8-tetrahydro-2-naphthyl)ethynyl]benzoic acid (bexarotene) shows therapeutic effects on these disease in rodent models. Here, we synthesized carbon-11-labeled ([ C]1) as a tracer for positron emission tomography (PET) and used it in a PET imaging study to examine the brain uptake and biodistribution of 1. We found that CO fixation after tin-lithium exchange at -20 °C afforded [ C]1. This methodology may also be useful for synthesizing CO H-PET tracer derivatives of other compounds bearing π-rich heterocyclic rings. A PET/CT imaging study of [ C]1 in mice indicated 1 is distributed to the brain and is thus a candidate for treatment of CNS diseases.
[Mh] Termos MeSH primário: Compostos Radiofarmacêuticos/síntese química
Compostos Radiofarmacêuticos/farmacologia
Receptores X Retinoide/agonistas
Tetra-Hidronaftalenos/síntese química
Tetra-Hidronaftalenos/farmacologia
Triazóis/síntese química
Triazóis/farmacologia
[Mh] Termos MeSH secundário: Animais
Autorradiografia
Encéfalo/diagnóstico por imagem
Encéfalo/metabolismo
Dióxido de Carbono/química
Radioisótopos de Carbono
Agonismo Parcial de Drogas
Lítio/química
Masculino
Camundongos Endogâmicos ICR
Compostos Orgânicos de Estanho/química
Tomografia por Emissão de Pósitrons
Compostos Radiofarmacêuticos/administração & dosagem
Tetra-Hidronaftalenos/administração & dosagem
Triazóis/administração & dosagem
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (1-((3,5,5,8,8-pentamethyl-5,6,7,8-tetrahydronaphthalen-2-yl)amino)benzotriazole-5-carboxylic acid); 0 (Carbon Radioisotopes); 0 (Organotin Compounds); 0 (Radiopharmaceuticals); 0 (Retinoid X Receptors); 0 (Tetrahydronaphthalenes); 0 (Triazoles); 142M471B3J (Carbon Dioxide); 9FN79X2M3F (Lithium)
[Em] Mês de entrada:1709
[Cu] Atualização por classe:170926
[Lr] Data última revisão:
170926
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170729
[St] Status:MEDLINE
[do] DOI:10.1021/acs.jmedchem.7b00817


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[PMID]:28672694
[Au] Autor:Ribeiro H; Ramos S; Homem V; Santos L
[Ad] Endereço:LEPABE - Laboratory for Process Engineering, Environment, Biotechnology and Energy, Faculty of Engineering, University of Porto, Rua Dr. Roberto Frias, 4200-465 Porto, Portugal.
[Ti] Título:Can coastline plant species be used as biosamplers of emerging contaminants? - UV-filters and synthetic musks as case studies.
[So] Source:Chemosphere;184:1134-1140, 2017 Oct.
[Is] ISSN:1879-1298
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Personal care products, an important class of emerging contaminants, have been frequently detected in different environmental matrices. Included in this category are synthetic musks compounds (SMCs) and UV-filters. Their occurrence in the coastal environment has been poorly studied. Therefore, this work aimed to verify whether five coastline plant species (Carpobrotus edulis, Cakile maritima, Medicago marina, Elymus farctus borealis-atlanticus and Euphorbia paralias) have the ability to accumulate 11 SMCs (cashmeran, celestolide, phantolide, galaxolide, tonalide, exaltolide, musk moskene, tibetene, ambrette, xylene and ketone) and 2 organic UVB filters (3-(4'-methylbenzylidene) camphor and octocrylene), functioning as biosamplers. To accomplish this task, a QuEChERS technique ("Quick, Easy, Cheap, Effective, Rugged, and Safe") was employed to extract the target compounds from the plant material collected in 15 beaches of Matosinhos and Vila Nova de Gaia (Portugal). The resulting extracts were analysed by gas chromatography-mass spectrometry. Limits of detection ranged from 0.02 ng g for celestolide and tonalide to 1.32 ng g for musk ambrette. The obtained recoveries were around 93% and relative standard deviation was generally less than 15%. SMCs were detected at levels ranging from 1.56 to 350 ng g dw and UV-filters from 2.9 to 264 ng g dw. Galaxolide and 3-(4'-methylbenzylidene) camphor were the synthetic musk and UV-filter detected in higher concentrations, respectively. Plants with higher water content accumulate better SMCs (hottentot-fig), while those with higher lipid content retain better the UV-filters (sea spurge).
[Mh] Termos MeSH primário: Monitoramento Ambiental
Ácidos Graxos Monoinsaturados/análise
Água do Mar/química
Protetores Solares/análise
Poluentes Químicos da Água/análise
[Mh] Termos MeSH secundário: Benzopiranos
Dinitrobenzenos
Cromatografia Gasosa-Espectrometria de Massas/métodos
Indanos
Portugal
Receptores Proteína Tirosina Quinases
Receptores Colinérgicos
Tetra-Hidronaftalenos
Xilenos/análise
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Benzopyrans); 0 (Dinitrobenzenes); 0 (Fatty Acids, Monounsaturated); 0 (Indans); 0 (Receptors, Cholinergic); 0 (Sunscreening Agents); 0 (Tetrahydronaphthalenes); 0 (Water Pollutants, Chemical); 0 (Xylenes); 095I377U8F (musk); 14170060AT (galaxolide); 1Q49IC9FAW (moskene); 21145-77-7 (acetyl methyl tetramethyl tetralin); 83-66-9 (musk ambrette (artificial)); BZR4438MY4 (6,7-dihydro-1,1,2,3,3-pentamethyl-4-(5H)indanone); EC 2.7.10.1 (MUSK protein, human); EC 2.7.10.1 (Receptor Protein-Tyrosine Kinases)
[Em] Mês de entrada:1710
[Cu] Atualização por classe:171005
[Lr] Data última revisão:
171005
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170705
[St] Status:MEDLINE


  7 / 4115 MEDLINE  
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[PMID]:28642153
[Au] Autor:Miro Estruch I; Melchers D; Houtman R; de Haan LHJ; Groten JP; Louisse J; Rietjens IMCM
[Ad] Endereço:Division of Toxicology, Wageningen University, Stippeneng 4, 6708 WE Wageningen, The Netherlands. Electronic address: ignacio.miroestruch@wur.nl.
[Ti] Título:Characterization of the differential coregulator binding signatures of the Retinoic Acid Receptor subtypes upon (ant)agonist action.
[So] Source:Biochim Biophys Acta;1865(9):1195-1206, 2017 09.
[Is] ISSN:0006-3002
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:Retinoic Acid Receptor alpha (RARα/NR1B1), Retinoic Acid Receptor beta (RARß/NR1B2) and Retinoic Acid Receptor gamma (RARγ/NR1B3) are transcription factors regulating gene expression in response to retinoids. Within the RAR genomic pathways, binding of RARs to coregulators is a key intermediate regulatory phase. However, ligand-dependent interactions between the wide variety of coregulators that may be present in a cell and the different RAR subtypes are largely unknown. The aim of this study is to characterize the coregulator binding profiles of RARs in the presence of the pan-agonist all-trans-Retinoic Acid (AtRA); the subtype-selective agonists Am80 (RARα), CD2314 (RARß) and BMS961 (RARγ); and the antagonist Ro415253. To this end, we used a microarray assay for coregulator-nuclear receptor interactions to assess RAR binding to 154 motifs belonging to >60 coregulators. The results revealed a high number of ligand-dependent RAR-coregulator interactions among all RAR variants, including many binding events not yet described in literature. Next, this work confirmed a greater ligand-independent activity of RARß compared to the other RAR subtypes based on both higher basal and lower ligand-driven coregulator binding. Further, several coregulator motifs showed selective binding to a specific RAR subtype. Next, this work showed that subtype-selective agonists can be successfully discriminated by using coregulator binding assays. Finally this study demonstrated the possible applications of a coregulator binding assay as a tool to discriminate between agonistic/antagonistic actions of ligands. The RAR-coregulator interactions found will be of use to direct further studies to better understand the mechanisms driving the eventual actions of retinoids.
[Mh] Termos MeSH primário: Receptores do Ácido Retinoico/química
Receptor alfa de Ácido Retinoico/química
[Mh] Termos MeSH secundário: Motivos de Aminoácidos
Antracenos/farmacologia
Benzoatos/farmacologia
Sítios de Ligação
Análise Serial de Proteínas
Ligação Proteica
Domínios Proteicos
Receptores do Ácido Retinoico/agonistas
Receptores do Ácido Retinoico/antagonistas & inibidores
Proteínas Recombinantes/metabolismo
Elementos de Resposta
Receptor alfa de Ácido Retinoico/agonistas
Receptor alfa de Ácido Retinoico/antagonistas & inibidores
Retinoides/farmacologia
Relação Estrutura-Atividade
Tetra-Hidronaftalenos/farmacologia
Tiofenos/farmacologia
Tretinoína/farmacologia
[Pt] Tipo de publicação:COMPARATIVE STUDY; JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Anthracenes); 0 (BMS 961); 0 (Benzoates); 0 (CD2314); 0 (Receptors, Retinoic Acid); 0 (Recombinant Proteins); 0 (Retinoic Acid Receptor alpha); 0 (Retinoids); 0 (Ro 415253); 0 (Tetrahydronaphthalenes); 0 (Thiophenes); 0 (retinoic acid receptor beta); 0 (retinoic acid receptor gamma); 08V52GZ3H9 (tamibarotene); 5688UTC01R (Tretinoin)
[Em] Mês de entrada:1710
[Cu] Atualização por classe:171027
[Lr] Data última revisão:
171027
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170624
[St] Status:MEDLINE


  8 / 4115 MEDLINE  
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[PMID]:28641286
[Au] Autor:Cao H; Bissinger R; Umbach AT; Gawaz M; Lang F
[Ad] Endereço:Department of Internal Medicine III, Tuebingen, Germany.
[Ti] Título:Effect of Bexarotene on Platelet Activation and Apoptosis.
[So] Source:Cell Physiol Biochem;42(2):838-847, 2017.
[Is] ISSN:1421-9778
[Cp] País de publicação:Switzerland
[La] Idioma:eng
[Ab] Resumo:BACKGROUND/AIMS: The retinoid X receptor (RXRs) stimulator Bexarotene ((4-[1-(3,5,5,8,8-pentamethyl-5,6,7,8-tetrahydro-2-naphthyl)ethynyl] benzoic acid) is used for the treatment of several malignancies. Bexarotene is at least in part effective by stimulation of apoptosis of tumor cells. Moreover, Bexarotene triggers eryptosis, the suicidal death of erythrocytes. Similar to erythrocytes, blood platelets lack nuclei but are nevertheless able to enter an apoptosis-like phenotype, characterized by caspase activation, cell shrinkage and cell membrane scrambling with phospha-tidylserine translocation to the cell surface. Platelet apoptosis is triggered by increase of cytosolic Ca2+-activity ([Ca2+]i), which further leads to degranulation and integrin activation. Platelet activation and apoptosis could be elicited by thrombin or collagen related peptide (CRP). The present study explored whether treatment of platelets with bexarotene modifies platelet activation and apoptosis following exposure to thrombin or CRP. METHODS: Platelets isolated from wild-type mice were exposed for 30 minutes to bexarotene (6 µg/ml) without or with an additional treatment with thrombin (0.01 U/ml) or CRP (2 µg/ml or 5 µg/ml). Flow cytometry was employed to estimate cytosolic Ca2+-activity ([Ca2+]i) from Fluo-3 fluorescence, platelet degranulation from P-selectin abundance, integrin activation from αIIbß3 integrin abundance, caspase activity utilizing an Active Caspase-3 Staining kit, phosphatidylserine abundance from annexin-V-binding, and relative platelet volume from forward scatter. RESULTS: In the absence of thrombin or CRP, the administration of bexarotene slightly but significantly increased [Ca2+]i, but did not significantly modify P-selectin abundance, activated αIIbß3 integrin, annexin-V-binding, cell volume, or caspase activity. Exposure of platelets to thrombin or CRP was followed by significant increase of [Ca2+]i, P-selectin abundance, active αIIbß3 integrin, annexin-V-binding, and caspase activity. The effects of thrombin on [Ca2+]i, annexin-V-binding, cell volume, and caspase activity as well as the effects of CRP on [Ca2+]i, P-selectin abundance, activated αIIbß3 integrin, annexin-V-binding, cell volume, and caspase activity were significantly augmented in the presence of bexarotene. CONCLUSIONS: Bexarotene sensitizes blood platelets for thrombin and/or CRP induced activation and apoptosis.
[Mh] Termos MeSH primário: Apoptose/efeitos dos fármacos
Ativação Plaquetária/efeitos dos fármacos
Tetra-Hidronaftalenos/administração & dosagem
Trombina/metabolismo
[Mh] Termos MeSH secundário: Animais
Plaquetas/efeitos dos fármacos
Plaquetas/metabolismo
Cálcio/metabolismo
Colágeno/metabolismo
Eritrócitos/metabolismo
Citometria de Fluxo
Hemólise/efeitos dos fármacos
Seres Humanos
Camundongos
Ativação Plaquetária/genética
Complexo Glicoproteico GPIIb-IIIa de Plaquetas
Espécies Reativas de Oxigênio/metabolismo
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Platelet Glycoprotein GPIIb-IIIa Complex); 0 (Reactive Oxygen Species); 0 (Tetrahydronaphthalenes); 9007-34-5 (Collagen); A61RXM4375 (bexarotene); EC 3.4.21.5 (Thrombin); SY7Q814VUP (Calcium)
[Em] Mês de entrada:1708
[Cu] Atualização por classe:170804
[Lr] Data última revisão:
170804
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170623
[St] Status:MEDLINE
[do] DOI:10.1159/000478627


  9 / 4115 MEDLINE  
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[PMID]:28590734
[Au] Autor:Moraux T; Dumarçay S; Gérardin P; Gérardin-Charbonnier C
[Ad] Endereço:Laboratoire d'Études et de Recherche sur le Matériau Bois, EA4370 USC INRA, Université de Lorraine, Faculté des Sciences et Technologies , Boulevard des Aiguillettes, 54506 VandÅ“uvre-lès-Nancy, France.
[Ti] Título:Derivatives of the Lignan 7'-Hydroxymatairesinol with Antioxidant Properties and Enhanced Lipophilicity.
[So] Source:J Nat Prod;80(6):1783-1790, 2017 Jun 23.
[Is] ISSN:1520-6025
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:The lignan 7'-hydroxymatairesinol (1), extracted from the knotwoods of fir (Abies alba), spruce (Picea abies), and Douglas fir (Pseudotsuga menziesii), exhibited unexpected reactivity when esterification reactions were attempted on the hydroxy group at position C-7'. To circumvent the rapid intramolecular cyclization procedure, leading quantitatively to the lignan conidendrin (7), a simple strategy for 7'-esterification of 1 under mild conditions (three steps, up to 80% overall yield) was developed. Compared to hydroxymatairesinol (1) (log K' = 1.49), the derivatives (2-5) had increased lipophilicity with log K' > 3.1, as determined by a UHPLC method. Compounds 1-5 exhibited potent antioxidant properties in the same range as the standards ascorbic acid and α-tocopherol (IC = 20-25 µM) and higher than that of BHT using a DPPH radical-scavenging assay.
[Mh] Termos MeSH primário: Antioxidantes/química
Antioxidantes/farmacologia
Lignanas/química
Lignanas/farmacologia
Picea/química
Pinus/química
Tetra-Hidronaftalenos/química
Tetra-Hidronaftalenos/farmacologia
[Mh] Termos MeSH secundário: Compostos de Bifenilo/farmacologia
Estrutura Molecular
Ressonância Magnética Nuclear Biomolecular
Picratos/farmacologia
Estereoisomerismo
alfa-Tocoferol
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Antioxidants); 0 (Biphenyl Compounds); 0 (Lignans); 0 (Picrates); 0 (Tetrahydronaphthalenes); 0 (hydroxymatairesinol); 518-55-8 (conidendrin); DFD3H4VGDH (1,1-diphenyl-2-picrylhydrazyl); H4N855PNZ1 (alpha-Tocopherol)
[Em] Mês de entrada:1708
[Cu] Atualização por classe:170830
[Lr] Data última revisão:
170830
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170608
[St] Status:MEDLINE
[do] DOI:10.1021/acs.jnatprod.6b01124


  10 / 4115 MEDLINE  
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[PMID]:28534193
[Au] Autor:Tsuji M
[Ad] Endereço:Institute of Molecular Function, 2-105-14 Takasu, Misato-shi, Saitama, 341-0037, Japan. motonori@molfunction.com.
[Ti] Título:Antagonist-perturbation mechanism for activation function-2 fixed motifs: active conformation and docking mode of retinoid X receptor antagonists.
[So] Source:J Comput Aided Mol Des;31(6):577-585, 2017 Jun.
[Is] ISSN:1573-4951
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:HX531, which contains a dibenzodiazepine skeleton, is one of the first retinoid X receptor (RXR) antagonists. Functioning via RXR-PPARγ heterodimer, this compound is receiving a lot of attention as a therapeutic drug candidate for diabetic disease controlling differentiation of adipose tissue. However, the active conformation of HX531 for RXRs is not well established. In the present study, quantum mechanics calculations and molecular mechanical docking simulations were carried out to precisely study the docking mode of HX531 with the human RXRα ligand-binding domain, as well as to provide a new approach to drug design using a structure-based perspective. It was suggested that HX531, which has the R configuration for the bent dibenzodiazepine plane together with the equatorial configuration for the N-methyl group attached to the nitrogen atom in the seven-membered diazepine ring, is a typical activation function-2 (AF-2) fixed motif perturbation type antagonist, which destabilizes the formation of AF-2 fixed motifs. On the other hand, the docking simulations supported the experimental result that LG100754 is an RXR homodimer antagonist and an RXR heterodimer agonist.
[Mh] Termos MeSH primário: Benzoatos/química
Compostos de Bifenilo/química
Receptores X Retinoide/agonistas
Receptores X Retinoide/antagonistas & inibidores
Retinoides/química
Tetra-Hidronaftalenos/química
[Mh] Termos MeSH secundário: Motivos de Aminoácidos
Sítios de Ligação
Seres Humanos
Simulação de Acoplamento Molecular
PPAR gama/agonistas
PPAR gama/química
Ligação Proteica
Conformação Proteica
Domínios Proteicos
Multimerização Proteica
Teoria Quântica
Receptores X Retinoide/química
Estereoisomerismo
Relação Estrutura-Atividade
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Benzoates); 0 (Biphenyl Compounds); 0 (LG 100754); 0 (PPAR gamma); 0 (Retinoid X Receptors); 0 (Retinoids); 0 (Tetrahydronaphthalenes); 0 (diazepinylbenzoic acid)
[Em] Mês de entrada:1711
[Cu] Atualização por classe:171108
[Lr] Data última revisão:
171108
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170524
[St] Status:MEDLINE
[do] DOI:10.1007/s10822-017-0025-6



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