Base de dados : MEDLINE
Pesquisa : G02.805 [Categoria DeCS]
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  1 / 80699 MEDLINE  
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[PMID]:29346419
[Au] Autor:Holcomb J; Doughan M; Spellmon N; Lewis B; Perry E; Zhang Y; Nico L; Wan J; Chakravarthy S; Shang W; Miao Q; Stemmler T; Yang Z
[Ad] Endereço:Department of Biochemistry and Molecular Biology, Wayne State University School of Medicine, Detroit, Michigan, United States of America.
[Ti] Título:SAXS analysis of a soluble cytosolic NgBR construct including extracellular and transmembrane domains.
[So] Source:PLoS One;13(1):e0191371, 2018.
[Is] ISSN:1932-6203
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:The Nogo-B receptor (NgBR) is involved in oncogenic Ras signaling through directly binding to farnesylated Ras. It recruits farnesylated Ras to the non-lipid-raft membrane for interaction with downstream effectors. However, the cytosolic domain of NgBR itself is only partially folded. The lack of several conserved secondary structural elements makes this domain unlikely to form a complete farnesyl binding pocket. We find that inclusion of the extracellular and transmembrane domains that contain additional conserved residues to the cytosolic region results in a well folded protein with a similar size and shape to the E.coli cis-isoprenyl transferase (UPPs). Small Angle X-ray Scattering (SAXS) analysis reveals the radius of gyration (Rg) of our NgBR construct to be 18.2 Å with a maximum particle dimension (Dmax) of 61.0 Å. Ab initio shape modeling returns a globular molecular envelope with an estimated molecular weight of 23.0 kD closely correlated with the calculated molecular weight. Both Kratky plot and pair distribution function of NgBR scattering reveal a bell shaped peak which is characteristic of a single globularly folded protein. In addition, circular dichroism (CD) analysis reveals that our construct has the secondary structure contents similar to the UPPs. However, this result does not agree with the currently accepted topological orientation of NgBR which might partition this construct into three separate domains. This discrepancy suggests another possible NgBR topology and lends insight into a potential molecular basis of how NgBR facilitates farnesylated Ras recruitment.
[Mh] Termos MeSH primário: Receptores de Superfície Celular/química
[Mh] Termos MeSH secundário: Sequência de Aminoácidos
Sítios de Ligação
Membrana Celular/metabolismo
Dicroísmo Circular
Citosol/metabolismo
Peso Molecular
Estrutura Secundária de Proteína
Receptores de Superfície Celular/metabolismo
Espalhamento a Baixo Ângulo
Homologia de Sequência de Aminoácidos
Solubilidade
Difração de Raios X
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, N.I.H., EXTRAMURAL; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (NUS1 protein, human); 0 (Receptors, Cell Surface)
[Em] Mês de entrada:1803
[Cu] Atualização por classe:180309
[Lr] Data última revisão:
180309
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:180119
[St] Status:MEDLINE
[do] DOI:10.1371/journal.pone.0191371


  2 / 80699 MEDLINE  
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[PMID]:29268131
[Au] Autor:Duroux R; Agouridas L; Renault N; El Bakali J; Furman C; Melnyk P; Yous S
[Ad] Endereço:Univ. Lille, Inserm, CHU Lille, UMR-S1172 - JPArc - Centre de Recherche Jean-Pierre AUBERT Neurosciences et Cancer, F-59000 Lille, France.
[Ti] Título:Antagonists of the adenosine A receptor based on a 2-arylbenzoxazole scaffold: Investigation of the C5- and C7-positions to enhance affinity.
[So] Source:Eur J Med Chem;144:151-163, 2018 Jan 20.
[Is] ISSN:1768-3254
[Cp] País de publicação:France
[La] Idioma:eng
[Ab] Resumo:We have recently reported a series of 2-furoyl-benzoxazoles as potential A adenosine receptor (A R) antagonists. Two hits were identified with interesting pharmacokinetic properties but were find to bind the hA R receptor in the micromolar-range. Herein, in order to enhance affinity toward the hA R, we explored the C5- and C7-position of hits 1 and 2 based on docking studies. These modifications led to compounds with nanomolar-range affinity (e.g. 6a, Ki = 40 nM) and high antagonist activity (e.g. 6a, IC = 70.6 nM). Selected compounds also exhibited interesting in vitro DMPK (Drug Metabolism and Pharmacokinetics) properties including high solubility and low cytotoxicity. Therefore, the benzoxazole ring appears as a highly effective scaffold for the design of new A antagonists.
[Mh] Termos MeSH primário: Antagonistas do Receptor A2 de Adenosina/química
Antagonistas do Receptor A2 de Adenosina/farmacologia
Benzoxazóis/química
Benzoxazóis/farmacologia
Receptor A2A de Adenosina/metabolismo
[Mh] Termos MeSH secundário: Antagonistas do Receptor A2 de Adenosina/metabolismo
Antagonistas do Receptor A2 de Adenosina/farmacocinética
Benzoxazóis/metabolismo
Benzoxazóis/farmacocinética
Células CACO-2
Linhagem Celular Tumoral
Desenho de Drogas
Seres Humanos
Microssomos Hepáticos/metabolismo
Solubilidade
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Adenosine A2 Receptor Antagonists); 0 (Benzoxazoles); 0 (Receptor, Adenosine A2A)
[Em] Mês de entrada:1803
[Cu] Atualização por classe:180309
[Lr] Data última revisão:
180309
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:171222
[St] Status:MEDLINE


  3 / 80699 MEDLINE  
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[PMID]:29175399
[Au] Autor:Stubbings WA; Harrad S
[Ad] Endereço:School of Geography, Earth, & Environmental Sciences, University of Birmingham, Birmingham, B15 2TT, UK. Electronic address: william.a.stubbings@gmail.com.
[Ti] Título:Leaching of TCIPP from furniture foam is rapid and substantial.
[So] Source:Chemosphere;193:720-725, 2018 Feb.
[Is] ISSN:1879-1298
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:A series of laboratory experiments were conducted, in which waste furniture polyurethane foam samples containing tris (1-chloro-2-propyl) phosphate (TCIPP) were contacted with a range of leaching fluids, formulated to simulate the composition of landfill leachate. Leaching was examined under a number of different scenarios, such as: dissolved humic matter concentration, pH, and temperature, as well as the effect of agitation, and waste:leaching fluid contact duration. In addition to single batch (no replenishment of leaching fluid), serial batch (draining of leachate and replenishment with fresh leaching fluid at various time intervals) experiments were conducted. Leaching of TCIPP from PUF appears to be a first order process. Concentrations of TCIPP in leachate generated by the experiments in this study ranged from 13 mg L to 130 mg L . In serial batch leaching experiments, >95% of TCIPP was depleted from PUF after 168 h total contact with leaching fluid. Our experiments indicate leaching is potentially a very significant pathway of TCIPP emissions to the environment.
[Mh] Termos MeSH primário: Poluição Ambiental
Retardadores de Chama/toxicidade
Decoração de Interiores e Mobiliário
Organofosfatos/química
Poliuretanos/toxicidade
Poluentes Químicos da Água/química
[Mh] Termos MeSH secundário: Cinética
Solubilidade
Soluções/química
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Flame Retardants); 0 (Organophosphates); 0 (Polyurethanes); 0 (Solutions); 0 (Water Pollutants, Chemical); 9009-54-5 (polyurethane foam)
[Em] Mês de entrada:1803
[Cu] Atualização por classe:180309
[Lr] Data última revisão:
180309
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:171128
[St] Status:MEDLINE


  4 / 80699 MEDLINE  
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[PMID]:28886495
[Au] Autor:Chen XM; Zhao Y; Ma YY; Zhu LJ; Yang TX; Wei ZM; Dong YL; Wei QB
[Ad] Endereço:College of Life Science, Northeast Agricultural University, Harbin 150030, China.
[Ti] Título:Assessing the environmental impact of phenanthrene in different types of land use based on the binding characteristics with dissolved organic matter.
[So] Source:Ecotoxicol Environ Saf;147:394-400, 2018 Jan.
[Is] ISSN:1090-2414
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:The binding characteristics of phenanthrene with dissolved organic matter (DOM) were studied by the excitation emission matrix fluorescence spectroscopy with parallel factor analysis in four types of land use which derived from forest (F), meadow (M), cropland (C), and greenhouse (G). The results showed that the humification degree and binding characteristics of phenanthrene with DOM were distinct differences in the four soils. The binding capacities of humic-like components with phenanthrene were stronger than those of protein-like components. The log K derived from the Stern-Volmer equation significantly correlated with the humification degree of DOM (p < 0.05) in different types of land use. Besides, correlation analysis demonstrated that the potential binding index (Fk) obtained from the modified Stern-Volmer model was a more accurate parameter to describe the combination degree of DOM with phenanthrene than log K, which presented a decrease order of C > F > M > G. Therefore, the environmental impact of phenanthrene in different types of land use could be assessed deeply based on the Fk and DOM concentration.
[Mh] Termos MeSH primário: Monitoramento Ambiental/métodos
Substâncias Húmicas/análise
Fenantrenos/análise
Poluentes do Solo/análise
Solo/química
[Mh] Termos MeSH secundário: Agricultura
China
Análise Fatorial
Florestas
Pradaria
Modelos Teóricos
Solubilidade
Espectrometria de Fluorescência/métodos
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Humic Substances); 0 (Phenanthrenes); 0 (Soil); 0 (Soil Pollutants); 448J8E5BST (phenanthrene)
[Em] Mês de entrada:1803
[Cu] Atualização por classe:180309
[Lr] Data última revisão:
180309
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170909
[St] Status:MEDLINE


  5 / 80699 MEDLINE  
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[PMID]:28465176
[Au] Autor:Nasabi M; Labbafi M; Mousavi ME; Madadlou A
[Ad] Endereço:Department of Food Science and Engineering, Razi Food Chemistry Lab, Faculty of Agricultural Engineering and Technology, University of Tehran, Karaj, Iran.
[Ti] Título:Effect of salts and nonionic surfactants on thermal characteristics of egg white proteins.
[So] Source:Int J Biol Macromol;102:970-976, 2017 Sep.
[Is] ISSN:1879-0003
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:Effect of salts (Sodium chloride (NaCl), Sodium sulfate (Na SO ), Ammonium sulfate ((NH ) SO ), and nonionic surfactants (glycerol, tween20, tween80) on thermal properties of egg white proteins as a whole were investigated. Egg white solutions with additive (0, 0.5 and 1%) were collected after 0, 1 and 2min heat treatment. Physico-chemical properties of egg white proteins were evaluated by measuring heat coagulation time, solubility and turbidity of solution. Adding glycerol caused the most significant decrease in turbidity and increase in heat coagulation time and solubility of egg white, although Sodium Chloride had the least positive impact on physico-chemical properties of egg white under heat treatment. The Fourier transform infrared (FT-IR) spectroscopy analysis of heat treated egg white proteins as a whole with additives demonstrated changes in secondary protein structure, which are presented regarding the shape, intensity and position of FT-IR band. Meanwhile, it showed a good correlation with the physico-chemical properties consequences. Generally, the effect of nonionic surfactants were more noticeable than that of salts in preventing of egg white proteins aggregation under heat treatment. By improving thermal stability of egg white proteins, its usage in thermal processing industry can be evolved.
[Mh] Termos MeSH primário: Proteínas do Ovo/química
Sais/farmacologia
Tensoativos/farmacologia
Temperatura Ambiente
[Mh] Termos MeSH secundário: Animais
Agregados Proteicos/efeitos dos fármacos
Solubilidade
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Egg Proteins); 0 (Protein Aggregates); 0 (Salts); 0 (Surface-Active Agents)
[Em] Mês de entrada:1803
[Cu] Atualização por classe:180309
[Lr] Data última revisão:
180309
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170504
[St] Status:MEDLINE


  6 / 80699 MEDLINE  
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[PMID]:28968940
[Au] Autor:Li Z; Wang P; Menzies NW; Kopittke PM
[Ad] Endereço:The University of Queensland, School of Agriculture and Food Sciences, St. Lucia, Queensland, 4072, Australia.
[Ti] Título:Defining appropriate methods for studying toxicities of trace metals in nutrient solutions.
[So] Source:Ecotoxicol Environ Saf;147:872-880, 2018 Jan.
[Is] ISSN:1090-2414
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:The use of inappropriate experimental conditions for examining trace metal phytotoxicity results in data of questionable value. The present study aimed to identify suitable parameters for study of phytotoxic metals in nutrient solutions. First, the literature was reviewed to determine the concentration of six metals (Cd, Cu, Hg, Ni, Pb, and Zn) from solution of contaminated soils. Next, the effects of pH, P, Cl, NO , and four Fe-chelators were investigated by using thermodynamic modelling and by examining changes in root elongation rate of soybean (Glycine max cv. Bunya). The literature review identified that the solution concentrations of metals in soils were low, ranging from (µM) 0.069-11Cd, 0.19-15.8 Cu, 0.000027-0.000079 Hg, 1.0-8.7 Ni, 0.004-0.55 Pb, and 0.4-36.3 Zn. For studies in nutrient solution, pH should generally be low given its effects on solubility and speciation, as should the P concentration due to the formation of insoluble phosphate salts. The concentrations of Cl, NO , and various chelators also influence metal toxicity through alteration of metal speciation. The nutrient solutions used to study metal toxicity should consider environmentally-relevant conditions especially for metal concentrations, with concentrations of other components added at levels that do not substantially alter metal toxicity.
[Mh] Termos MeSH primário: Monitoramento Ambiental/métodos
Hidroponia
Metais Pesados/toxicidade
Feijão de Soja/efeitos dos fármacos
Oligoelementos/toxicidade
[Mh] Termos MeSH secundário: Metais Pesados/análise
Modelos Teóricos
Raízes de Plantas/efeitos dos fármacos
Raízes de Plantas/crescimento & desenvolvimento
Solubilidade
Soluções
Feijão de Soja/crescimento & desenvolvimento
Termodinâmica
Oligoelementos/análise
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Metals, Heavy); 0 (Solutions); 0 (Trace Elements)
[Em] Mês de entrada:1803
[Cu] Atualização por classe:180308
[Lr] Data última revisão:
180308
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:171004
[St] Status:MEDLINE


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[PMID]:28826031
[Au] Autor:Tran HN; Viet PV; Chao HP
[Ad] Endereço:Department of Environmental Engineering, Chung Yuan Christian University, Chungli 32023, Taiwan.
[Ti] Título:Surfactant modified zeolite as amphiphilic and dual-electronic adsorbent for removal of cationic and oxyanionic metal ions and organic compounds.
[So] Source:Ecotoxicol Environ Saf;147:55-63, 2018 Jan.
[Is] ISSN:1090-2414
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:A hydrophilic Y zeolite was primarily treated with sodium hydroxide to enhance its cation exchange capacity (Na-zeolite). The organo-zeolite (Na-H-zeolite) was prepared by a modification process of the external surface of Na-zeolite with a cationic surfactant (hexadecyltrimethylammonium; HDTMA). Three adsorbents (i.e., pristine zeolite, Na-zeolite, and Na-H-zeolite) were characterized with nitrogen adsorption/desorption isotherms, scanning electron microscopy coupled with energy dispersive X-ray spectroscopy, cation exchange capacities, and zeta potential. Results demonstrated that HDTMA can be adsorbed on the surface of Na-zeolite to form patchy bilayers. The adsorption capacity of several hazardous pollutants (i.e., Pb , Cu , Ni , Cr O , propylbenzene, ethylbenzene, toluene, benzene, and phenol) onto Na-H-zeolite was investigated in a single system and multiple-components. Adsorption isotherm was measured to further understand the effects of the modification process on the adsorption behaviors of Na-H-zeolite. Adsorption performances indicated that Na-H-zeolite can simultaneously adsorb the metal cations (on the surface not covered by HDTMA), oxyanions (on the surface covered by HDTMA). Na-H-zeolite also exhibited both hydrophilic and hydrophobic surfaces to uptake organic compounds with various water solubilities (from 55 to 75,000mg/L). It was experimentally concluded that Na-H-zeolite is a potential dual-electronic and amphiphilic adsorbent for efficiently removing a wide range of potentially toxic pollutants from aquatic environments.
[Mh] Termos MeSH primário: Metais Pesados/análise
Compostos Orgânicos/análise
Tensoativos/química
Poluentes Químicos da Água/análise
Purificação da Água/métodos
Zeolitas/química
[Mh] Termos MeSH secundário: Adsorção
Ânions
Cátions
Interações Hidrofóbicas e Hidrofílicas
Metais Pesados/química
Modelos Teóricos
Compostos Orgânicos/química
Óxidos
Solubilidade
Propriedades de Superfície
Poluentes Químicos da Água/química
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Anions); 0 (Cations); 0 (Metals, Heavy); 0 (Organic Chemicals); 0 (Oxides); 0 (Surface-Active Agents); 0 (Water Pollutants, Chemical); 1318-02-1 (Zeolites)
[Em] Mês de entrada:1803
[Cu] Atualização por classe:180308
[Lr] Data última revisão:
180308
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170822
[St] Status:MEDLINE


  8 / 80699 MEDLINE  
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[PMID]:28450206
[Au] Autor:Deng J; Staufenbiel S; Hao S; Wang B; Dashevskiy A; Bodmeier R
[Ad] Endereço:College of Pharmacy, Freie Universität Berlin, Kelchstr. 31, 12169 Berlin, Germany.
[Ti] Título:Development of a discriminative biphasic in vitro dissolution test and correlation with in vivo pharmacokinetic studies for differently formulated racecadotril granules.
[So] Source:J Control Release;255:202-209, 2017 Jun 10.
[Is] ISSN:1873-4995
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:The purpose of this study was to discriminate the release behavior from three differently formulated racecadotril (BCS II) granules and to establish an in vitro-in vivo correlation. Three granule formulations of the lipophilic drug were prepared with equivalent composition but prepared with different manufacturing processes (dry granulation, wet granulation with or without binder). In vitro release of the three granules was investigated using a biphasic dissolution system (phosphate buffer pH6.8 and octanol) and compared to the conventional single phase USP II dissolution test performed under sink and non-sink conditions. In vivo studies with each granule formulation were performed in rats. Interestingly, the granule formulations exhibited pronouncedly different behavior in the different dissolution systems depending on different wetting and dissolution conditions. Single phase USP II dissolution tests lacked discrimination. In contrast, remarkable discrimination between the granule formulations was observed in the octanol phase of biphasic dissolution system with a rank order of release from granules prepared by wet granulation with binder>wet granulation without binder>dry granulation. This release order correlated well with the wettability of these granules. An excellent correlation was also established between in vitro release in the octanol phase of the biphasic test and in vivo data (R =0.999). Compared to conventional dissolution methods, the biphasic method provides great potential to discriminate between only minor formulation and process changes within the same dosage form for poorly soluble drugs.
[Mh] Termos MeSH primário: Tiorfano/análogos & derivados
[Mh] Termos MeSH secundário: Animais
Química Farmacêutica
Liberação Controlada de Fármacos
Masculino
Modelos Teóricos
Ratos Sprague-Dawley
Solubilidade
Tiorfano/sangue
Tiorfano/química
Tiorfano/farmacocinética
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
76K53XP4TO (racecadotril); B79L7B5X3Z (Thiorphan)
[Em] Mês de entrada:1803
[Cu] Atualização por classe:180308
[Lr] Data última revisão:
180308
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170429
[St] Status:MEDLINE


  9 / 80699 MEDLINE  
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[PMID]:29180866
[Au] Autor:Lapin NA; Vergara LA; Mackeyev Y; Newton JM; Dilliard SA; Wilson LJ; Curley SA; Serda RE
[Ad] Endereço:Michael E DeBakey Department of Surgery, Baylor College of Medicine.
[Ti] Título:Biotransport kinetics and intratumoral biodistribution of malonodiserinolamide-derivatized [60]fullerene in a murine model of breast adenocarcinoma.
[So] Source:Int J Nanomedicine;12:8289-8307, 2017.
[Is] ISSN:1178-2013
[Cp] País de publicação:New Zealand
[La] Idioma:eng
[Ab] Resumo:[60]Fullerene is a highly versatile nanoparticle (NP) platform for drug delivery to sites of pathology owing to its small size and both ease and versatility of chemical functionalization, facilitating multisite drug conjugation, drug targeting, and modulation of its physicochemical properties. The prominent and well-characterized role of the enhanced permeation and retention (EPR) effect in facilitating NP delivery to tumors motivated us to explore vascular transport kinetics of a water-soluble [60]fullerene derivatives using intravital microscopy in an immune competent murine model of breast adenocarcinoma. Herein, we present a novel local and global image analysis of vascular transport kinetics at the level of individual tumor blood vessels on the micron scale and across whole images, respectively. Similar to larger nanomaterials, [60]fullerenes displayed rapid extravasation from tumor vasculature, distinct from that in normal microvasculature. Temporal heterogeneity in fullerene delivery to tumors was observed, demonstrating the issue of nonuniform delivery beyond spatial dimensions. Trends in local region analysis of fullerene biokinetics by fluorescence quantification were in agreement with global image analysis. Further analysis of intratumoral vascular clearance rates suggested a possible enhanced penetration and retention effect of the fullerene compared to a 70 kDa vascular tracer. Overall, this study demonstrates the feasibility of tracking and quantifying the delivery kinetics and intratumoral biodistribution of fullerene-based drug delivery platforms, consistent with the EPR effect on short timescales and passive transport to tumors.
[Mh] Termos MeSH primário: Adenocarcinoma/tratamento farmacológico
Sistemas de Liberação de Medicamentos/métodos
Fulerenos/farmacocinética
Neoplasias Mamárias Experimentais/tratamento farmacológico
Nanopartículas/química
[Mh] Termos MeSH secundário: Animais
Difusão Dinâmica da Luz
Feminino
Fluorescência
Fulerenos/química
Microscopia Intravital/métodos
Cinética
Camundongos Endogâmicos BALB C
Microscopia Eletrônica de Varredura
Imagem Molecular/métodos
Solubilidade
Distribuição Tecidual
Água/química
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Fullerenes); 059QF0KO0R (Water)
[Em] Mês de entrada:1803
[Cu] Atualização por classe:180305
[Lr] Data última revisão:
180305
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:171129
[St] Status:MEDLINE
[do] DOI:10.2147/IJN.S138641


  10 / 80699 MEDLINE  
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[PMID]:29291441
[Au] Autor:Otvagin VF; Nyuchev AV; Kuzmina NS; Grishin ID; Gavryushin AE; Romanenko YV; Koifman OI; Belykh DV; Peskova NN; Shilyagina NY; Balalaeva IV; Fedorov AY
[Ad] Endereço:Lobachevsky State University of Nizhny Novgorod, Gagarina Av. 23, Nizhny Novgorod 603950, Russian Federation.
[Ti] Título:Synthesis and biological evaluation of new water-soluble photoactive chlorin conjugate for targeted delivery.
[So] Source:Eur J Med Chem;144:740-750, 2018 Jan 20.
[Is] ISSN:1768-3254
[Cp] País de publicação:France
[La] Idioma:eng
[Ab] Resumo:A new water-soluble conjugate, consisting of a chlorin-based photosensitizing part, and a 4-arylaminoquinazoline moiety with high potential affinity to an epidermal growth factor receptors (EGFR) and vascular endothelial growth factor receptors (VEGFR), suitable for photodynamic therapy (PDT), was synthesized starting from methylpheophorbide-a in seven steps. An increased accumulation of this compound in A431 cells with high level of EGFR expression, in comparison with CHO and HeLa cells with low EGFR expression was observed. The prepared conjugate exhibits dark and photoinduced cytotoxicity at micromolar concentrations with IC /IC ratio of 11-18. In tumor-bearing mice, the conjugate preferentially accumulates in the tumor tissue.
[Mh] Termos MeSH primário: Sistemas de Liberação de Medicamentos
Fármacos Fotossensibilizantes/farmacologia
Porfirinas/farmacologia
Quinazolinas/farmacologia
[Mh] Termos MeSH secundário: Animais
Células CHO
Linhagem Celular Tumoral
Cricetulus
Relação Dose-Resposta a Droga
Células HeLa
Seres Humanos
Camundongos
Camundongos Endogâmicos BALB C
Estrutura Molecular
Fotoquimioterapia
Fármacos Fotossensibilizantes/síntese química
Fármacos Fotossensibilizantes/química
Porfirinas/química
Quinazolinas/química
Solubilidade
Relação Estrutura-Atividade
Fator A de Crescimento do Endotélio Vascular/biossíntese
Água/química
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Photosensitizing Agents); 0 (Porphyrins); 0 (Quinazolines); 0 (Vascular Endothelial Growth Factor A); 059QF0KO0R (Water); 2683-84-3 (chlorin)
[Em] Mês de entrada:1803
[Cu] Atualização por classe:180302
[Lr] Data última revisão:
180302
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:180102
[St] Status:MEDLINE



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