999 resultados para G
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for selectively targeting cancer cells. Herein, we report the design and evolution of a new kind of carbazole-based benzimidazole dimers for their efficient telomerase inhibition activity. Spectroscopic titrations reveal the ligands high affinity toward the G4 DNA with significantly higher selectivity over duplex-DNA. The electrophoretic mobility shift assay shows that the ligands efficiently promote the formation of 04 DNA even at a lower concentration of the stabilizing K+ ions. The TRAP-LIG assay demonstrates the ligand's potential telomerase inhibition activity and also establishes that the activity proceeds via G4 DNA stabilization. An efficient nuclear internalization of the ligands in several common cancer cells (HeLa, HT1080, and A549) also enabled differentiation between normal HFF cells in co-cultures of cancer and normal ones. The ligands induce significant apoptotic response and antiproliferative activity toward cancer cells selectively when compared to the normal cells.
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In this study, fluoranthene-based derivatives with a high thermal stability were synthesized for applications in organic electroluminescent devices. The two derivatives synthesized in this study, bis(4-(7,9,10-triphenylfluoranthen-8-yl)phenyl)sulfane (TPFDPS) and 2,8-bis(7,9,10-triphenylfluoranthen-8-yl)dibenzob,d]thiophene (TPFDBT), were characterized by cyclic voltammetry, differential scanning calorimetry (DSC) and thermogravimetric analysis (TGA). TPFDPS exhibits a high T-g of 210 degrees C while TPFDBT is crystalline in nature. Both the derivatives are thermally stable up to 500 degrees C. The charge transport studies reveal predominant electron transport properties. Subsequently, we fabricated blue OLEDs with 2-tert-butyl-9,10-bis-(beta-naphthyl)-anthracene (TBADN) as the emitting layer to demonstrate the applications of these molecules as an electron transporting layer.
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We report the temperature-dependent photoluminescence (PL) properties of polymeric graphite-like carbon nitride (g-C3N4) and a methodology for the determination of quantum efficiency along with the activation energy. The PL is shown to originate from three different pathways of transitions: sigma*-LP, pi*-LP, and pi*-pi, respectively. The overall activation energy is found to be similar to 73.58 meV which is much lower than the exciton binding energy reported theoretically but ideal for highly sensitive wide-range temperature sensing. The quantum yield derived from the PL data is 23.3%, whereas the absolute quantum yield is 5.3%. We propose that the temperature-dependent PL can be exploited for the evaluation of the temperature dependency of quantum yield as well as for temperature sensing. Our analysis further indicates that g-C3N4 is well-suited for wide-range temperature sensing.
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A fuel optimal nonlinear sub-optimal guidance scheme is presented in this paper for soft landing of a lunar craft during the powered descent phase. The recently developed Generalized Model Predictive Static Programming (G-MPSP) is used to compute the required magnitude and angle of the thrust vector. Both terminal position and velocity vector are imposed as hard constraints, which ensures high position accuracy and facilitates initiation of vertical descent at the end of the powered descent phase. A key feature of the G-MPSP algorithm is that it converts the nonlinear dynamic programming problem into a low-dimensional static optimization problem (of the same dimension as the output vector). The control history update is done in closed form after computing a time-varying weighting matrix through a backward integration process. This feature makes the algorithm computationally efficient, which makes it suitable for on-board applications. The effectiveness of the proposed guidance algorithm is demonstrated through promising simulation results.
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The formation of telomeric G-quadruplexes has been shown to inhibit telomerase activity. Indeed, a number of small molecules capable of p-stacking with G-tetrads have shown the ability to inhibit telomerase activity through the stabilization of G-quadruplexes. Curcumin displays a wide spectrum of medicinal properties ranging from anti-bacterial, anti-viral, anti-protozoal, anti-fungal and anti-inflammatory to anti-cancer activity. We have investigated the interactions of curcumin and its structural analogues with the human telomeric sequence AG(3)(T(2)AG(3))(3) under molecular crowding conditions. Experimental studies indicated the existence of a AG(3)(T(2)AG(3))(3)/curcumin complex with binding affinity of 0.72 x 10(6) M-1 under molecular crowding conditions. The results from UV-visible absorption spectroscopy, a fluorescent TO displacement assay, circular dichroism and molecular docking studies, imply that curcumin and their analogues interact with G-quadruplex DNA via groove binding. While other analogs of curcumin studied here bind to G-quadruplexes in a qualitatively similar manner their affinities are relatively lower in comparison to curcumin. The Knoevenagel condensate, a methoxy-benzylidene derivative of curcumin, also exhibited significant binding to G-quadruplex DNA, although with two times decreased affinity. Our study establishes the potential of curcumin as a promising natural product for G-quadruplex specific ligands.
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G. N. Ramachandran is among the founding fathers of structural molecular biology. He made pioneering contributions in computational biology, modelling and what we now call bioinformatics. The triple helical coiled coil structure of collagen proposed by him forms the basis of much of collagen research at the molecular level. The Ramachandran map remains the simplest descriptor and tool for validation of protein structures. He has left his imprint on almost all aspects of biomolecular conformation. His contributions in the area of theoretical crystallography have been outstanding. His legacy has provided inspiration for the further development of structural biology in India. After a pause, computational biology and bioinformatics are in a resurgent phase. One of the two schools established by Ramachandran pioneered the development of macromolecular crystallography, which has now grown into an important component of modern biological research in India. Macromolecular NMR studies in the country are presently gathering momentum. Structural biology in India is now poised to again approach heights of the kind that Ramachandran conquered more than a generation ago.
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The formation of telomeric G-quadruplexes has been shown to inhibit telomerase activity. Indeed, a number of small molecules capable of p-stacking with G-tetrads have shown the ability to inhibit telomerase activity through the stabilization of G-quadruplexes. Curcumin displays a wide spectrum of medicinal properties ranging from anti-bacterial, anti-viral, anti-protozoal, anti-fungal and anti-inflammatory to anti-cancer activity. We have investigated the interactions of curcumin and its structural analogues with the human telomeric sequence AG(3)(T(2)AG(3))(3) under molecular crowding conditions. Experimental studies indicated the existence of a AG(3)(T(2)AG(3))(3)/curcumin complex with binding affinity of 0.72 x 10(6) M-1 under molecular crowding conditions. The results from UV-visible absorption spectroscopy, a fluorescent TO displacement assay, circular dichroism and molecular docking studies, imply that curcumin and their analogues interact with G-quadruplex DNA via groove binding. While other analogs of curcumin studied here bind to G-quadruplexes in a qualitatively similar manner their affinities are relatively lower in comparison to curcumin. The Knoevenagel condensate, a methoxy-benzylidene derivative of curcumin, also exhibited significant binding to G-quadruplex DNA, although with two times decreased affinity. Our study establishes the potential of curcumin as a promising natural product for G-quadruplex specific ligands.
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This paper reveals an early quasi-saturation (QS) effect attributed to the geometrical parameters in shallow trench isolation-type drain-extended MOS (STI-DeMOS) transistors in advanced CMOS technologies. The quasi-saturation effect leads to serious g(m) reduction in STI-DeMOS. This paper investigates the nonlinear resistive behavior of the drain-extended region and its impact on the particular behavior of the STI-DeMOS transistor. In difference to vertical DMOS or lateral DMOS structures, STI-DeMOS exhibits three distinct regions of the drain extension. A complete understanding of the physics in these regions and their impact on the QS behavior are developed in this paper. An optimization strategy is shown for an improved g(m) device in a state-of-the-art 28-nm CMOS technology node.
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In the present paper the rarefied gas how caused by the sudden change of the wall temperature and the Rayleigh problem are simulated by the DSMC method which has been validated by experiments both in global flour field and velocity distribution function level. The comparison of the simulated results with the accurate numerical solutions of the B-G-K model equation shows that near equilibrium the BG-K equation with corrected collision frequency can give accurate result but as farther away from equilibrium the B-G-K equation is not accurate. This is for the first time that the error caused by the B-G-K model equation has been revealed.
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Este experimento se realizó en la Granja Experimental Porcina (G.E.P), Cofradía, Masaya, con 82 cerdas del cuarto parto, 30 servidas a través de inseminación artificial (I.A) y 52 cerdas por monta natural (M.N); iniciando en mayo de 1,995 hasta mayo de 1,996 con el objetivo de evaluar los parámetros reproductivos y económicos en ambos sistemas de monta. Los dos grupos de cerdas reproductoras estaban compuestos por las razas LANDRACE, YORKSHIRE y DUROC. Las variables evaluadas fueron: Tasa de concepción (T.C) y tasa de parición (T.P), números de crías por partos (N.C.P), peso vivo promedio del lechón en la camada al nacer (P.V.L.C), relación beneficio-costo (B-C). Los resultados finales comprobados al 5% de significancia estadísticas fueron: T.P en I.A con 56.66% menor que en M.N con 76.92%, en N.C.P para I.A con 7.06, menor que en M.N de 8.725, P.V.L.C en I.A de 1.85 kg, similar a 1.74 kg, en MN. Para la relación B-C en I.A fue de 0.53 córdobas y para M.N de 0.56 córdobas.
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Durante la época de postrera del 2001 se establecieron dos ensayos en las localidades La Compañía y La Conquista pertenecientes al departamento de Carazo con el objetivo de evaluar el comportamiento de 34 genotipos de frijol común (Phaseolus vulgaris L.) y 2 genotipos de frijol tepari( Phaseolus acutifulius G.). en cuanto a caracteres de rendimiento y desarrollo. Estos materiales fueron proporcionados por el Centro Internacional de Agricultura Tropical (CIAT). El diseño utilizado fue de bloques incompleto con 3 repeticiones. Los resultados de campo se procesaron mediante el programa de sistema análisis estadístico (SAS), la prueba de rango múltiple de Tukey al 0.05 de error para las variables evaluadas y la correlación de Pearson. Las variables evaluadas días a floración, madurez fisiológica, peso de 100 granos, y rendimiento mostraron diferencias estadísticas entre genotipos en cada localidad. La variable granos por vaina, solamente en una localidad resultó significativa, la variable número de vainas por planta no fue significativa en ambas localidades, ningún genotipo supero en cuanto al rendimiento a las variedades utilizadas como testigos. Los genotipos que superaron en precocidad a madurez fisiológica a los testigos en las dos localidades son INB 37, INB 39 y G 40068. Los genotipos con mayores incidencia al virus del mosaico dorado (BGMV) fueron SEA 15, SEA 17, SEA 19, SEA 21. SEA 22 y G 1977, los de mayor incidencia a mancha angular (Isariopsis griseo/a Sacc.) fueron G 40068, G 40159 y PINTO VILLA.
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An immunosensor interface based on mixed hydrophobic self-assembled monolayers (SAMs) of methyl and carboxylic acid terminated thiols with covalently attached human Immunoglobulin G (hIgG), is investigated. The densely packed and organised SAMs were characterised by contact angle measurements and cyclic voltammetry. The effect of the non-ionic surfactant, Tween 20, in preventing nonspecific adsorption is addressed by ellipsometry during physical and covalent hIgG immobilization on pure and mixed SAMs, respectively. It is clearly demonstrated that nonspecific adsorption due to hydrophobic interactions of hIgG on methyl ended groups is totally inhibited, whereas electrostatic/hydrogen bonding interactions with the exposed carboxylic groups prevail in the presence of surfactant. Results of ellipsometry and Atomic Force Microscopy, reveal that the surface concentration of covalently immobilized hIgG is determined by the ratio of COOH/CH3-terminated thiols in SAM forming solution. Moreover, the ellipsometric data demonstrates that the ratio of bound anti-hIgG/hIgG depends on the density of hIgG on the surface and that the highest ratio is close to three. We also report the selectivity and high sensitivity achieved by chronoamperometry in the detection of adsorbed hIgG and the reaction with its antibody.
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El café (coffea arábiga L.) representa uno de los cultivos de mayor importancia en Nicaragua Este cultivo se ve afectado por nematodos fitoparasito de los géneros Meloidogyne Spp. Pratylenchus spp0, y Rotylenchulus spp. Se probó el efecto de combinaciones del nematicida counter 10 G y fertilizante N-P sobre los nematodos fitoparasito con un ensayo en el Centro Experimental del Café Mauricio López Munguía”, Masatepe entre los meses de abril y Octubre de 1986. El diseña utilizado fue en bifactorial en bloques completos al azar con cuatro repeticiones. Los tratamientos fueron al nematicida counter 10 G (terbufos) en dosis de 0; 017: 0.25 y 0, 32 gr de la planta; el fertilizante N-P de la fórmula 18-46 o en dosis de 0.5 y 10 gr/planta, aplicados sobre y en combinación lo que se Hizo un total de 12 tratamientos. la aplicación del nematicida se hizo una sola vez y el fertilizante en dos ocasiones d. A los 55 y 100 DDA se midió el numero de nematodos en el suelo (Meloidogyne spp., Rotylenchulus spp, y pratylenchus spp) nematodos en las raíces (Meloidogyne spp), altura de planta, Numero de hojas y peso de raíz. Los resultados de este ensayo demostraron qué el nematicida tuvo efecto sobre Rotylenchulus spp y Rotylenchulus spp. Pero no sobre Meloidogyne spp en el suelo y en la raíz: No se encontró ningún defecto del fertilizant4e sobre las poblaciones de nematodos. Las combinaciones de nematicida-fertilizante tuvieron un efecto de amplia variabilidad sobre las poblaciones de nematodos lo que dificulto la recomendación de una determinada combinación: La dosis de fertilizantes que resulto con los mejores promedios sobre las variables altura de la planta, Número de hojas y peso de raíz fue la de 5gr, /planta Se encontró una correlaciona negativa significativa entre el género Meloidogyne spp y la altura de la plata a los 55 DDA, no observándose estos mismos resultados a los 100 DDA: también se encontró una correlación positiva significativa entre el número de Meloidogyne spp, del suelo y de la raíz a los 55 y 100 DDA; entre pratylenchus y rotylenchulus a los 55 DDA y entere el número de Nódulos causados por Meloidogyne a los 55 DDA y el peso de la Raíz a los 100 DDA.