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1.
Opt Express ; 32(7): 12476-12495, 2024 Mar 25.
Artículo en Inglés | MEDLINE | ID: mdl-38571069

RESUMEN

Multi-band terahertz (THz) absorbers have recently gained attention due to their favorable application prospects in communication, imaging, detection, and other fields. However, many multi-band THz absorbers are tuned by a single method, which limits their tuning effect. To address this issue, we propose a multi-band THz absorber that can be co-modulated by thermal and electrical methods. Our proposed absorber uses vanadium dioxide (VO2) to achieve this co-modulation. When VO2 is insulating, the frequency of the absorbing peaks originating from the lateral Fabry-Pérot resonance mode can be changed by adjusting the VO2 width. When VO2 is a conductor, the quality factor of the absorbing peak based on the inductor-capacitor resonance mode can be tuned by adjusting the width of VO2. By varying the top dielectric layer thickness, the frequency of the absorbing peaks can be tuned over a wide range. For devices with two or three layers of graphene nanoribbons-dielectric stacks, a modulation effect similar to that of varying dielectric layer thickness in a single-layer graphene device can be achieved simply by applying a 1 eV Fermi energy to graphene nanoribbons in different layers. By combining thermal and electrical modulation, the two or three-layer stacked device can be dynamically switched between four or six absorbing states, and a wider range of dynamic peak frequency modulation can be realized. Furthermore, the performance of the absorber does not deteriorate significantly at an incident angle of up to 70°. Our proposed thermal-electrical switchable wide-angle multi-band THz absorber provides a reference for the design, fabrication, and application of high-performance THz absorbers in different fields.

2.
Opt Express ; 30(3): 3893-3902, 2022 Jan 31.
Artículo en Inglés | MEDLINE | ID: mdl-35209638

RESUMEN

A multi-band terahertz (THz) absorber based on graphene sheet and nanoribbons is proposed and investigated. In the studied frequency range, five absorption peaks are observed, with four originate from lateral Fabry-Perot resonance (LFPR) and one originates from guided-mode resonance (GMR). The LFPR and GMR peaks behave differently when geometric parameters are adjusted, which makes independent tuning possible. When period increases, the GMR peak red shifts and the frequencies of LFPR peaks remain almost unchanged. On the contrary, as nanoribbon width increases, the frequency of GMR remains almost unchanged while that of LFPRs decrease significantly. With increasing top dielectric layer thickness, the LFPR peaks blue shift while the GMR peak red shifts. In addition, the absorber has the merit of multi-band high absorptivity and frequency stability under large angle oblique incidence. The proposed terahertz absorber may benefit the areas of medical imaging, sensing, non-destructive testing, THz communications and other applications.

3.
Front Chem ; 10: 973961, 2022.
Artículo en Inglés | MEDLINE | ID: mdl-36034655

RESUMEN

The application of the active colloids is strongly related to their self-propulsion velocity, which is controlled by the generated anisotropic concentration field. We investigated the effect of this anisotropy on velocity induced by numerical treatments and size of Janus colloids. The far-field approximation is effective in estimating the velocity, even though it neglects the shape effect on the anisotropy of the concentration field. If the surface mobility contrast between the active and the inert part is moderate, the spherical approximation is feasible for sphere-like Janus colloids. Legendre expansion of the concentration field causes artificial anisotropy. Raising the order of the expansion can suppress this effect, but also distorts the concentration field at the top of active part. Thus, the order of the expansion should be chosen carefully depending on the goal of the study. Based on the verified Legendre expansion method and ionic-diffusiophoresis model, we show that due to the size-effect on both the concentration field and the surface mobility, increasing size of colloids can lower the self-propulsion velocity. Our finding is consistent with previous experimental observations without fitting parameter, shedding new light on the self-propulsion mechanism of chemically-driven active colloids. We further show a velocity reversal at high overall ζ potential induced by increasing size, providing a new way for controlling the dynamics of acitve colloids.

4.
Exp Cell Res ; 316(2): 258-71, 2010 Jan 15.
Artículo en Inglés | MEDLINE | ID: mdl-19732767

RESUMEN

The PSMD14 (POH1, also known as Rpn11/MPR1/S13/CepP1) protein within the 19S complex (19S cap; PA700) is responsible for substrate deubiquitination during proteasomal degradation. The role of PSMD14 in cell proliferation and senescence was explored using siRNA knockdown in carcinoma cell lines. Our results reveal that down-regulation of PSMD14 by siRNA transfection had a considerable impact on cell viability causing cell arrest in the G0-G1 phase, ultimately leading to senescence. The molecular events associated with decreased cell proliferation, cell cycle arrest and senescence include down-regulation of cyclin B1-CDK1-CDC25C, down-regulation of cyclin D1 and up-regulation of p21(/Cip) and p27(/Kip1). Most notably, phosphorylation of the retinoblastoma protein was markedly reduced in PSMD14 knockdown cells. A comparative study with PSMB5, a subunit of the 20S proteasome, revealed that PSMB5 and PSMD14 have different effects on cell cycle, senescence and associated molecular events. These data support the view that the 19S and 20S subunits of the proteasome have distinct biological functions and imply that targeting 19S and 20S would have distinct molecular consequences on tumor cells.


Asunto(s)
Ciclo Celular/genética , Senescencia Celular/genética , Complejo de la Endopetidasa Proteasomal/deficiencia , Transactivadores/deficiencia , Proteína Quinasa CDC2/genética , Proteína Quinasa CDC2/metabolismo , Línea Celular Tumoral , Proliferación Celular , Supervivencia Celular/genética , Ciclina B1/genética , Ciclina B1/metabolismo , Ciclina D1/genética , Ciclina D1/metabolismo , Proteínas Inhibidoras de las Quinasas Dependientes de la Ciclina/genética , Proteínas Inhibidoras de las Quinasas Dependientes de la Ciclina/metabolismo , ADN/análisis , Células Epiteliales/citología , Células Epiteliales/metabolismo , Fibroblastos/citología , Fibroblastos/metabolismo , Fase G1/genética , Expresión Génica/genética , Células HeLa , Humanos , Fosforilación/genética , Complejo de la Endopetidasa Proteasomal/genética , Complejo de la Endopetidasa Proteasomal/metabolismo , ARN Interferente Pequeño/genética , Fase de Descanso del Ciclo Celular/genética , Proteína de Retinoblastoma/genética , Proteína de Retinoblastoma/metabolismo , Sulfotransferasas/metabolismo , Transactivadores/genética , Transactivadores/metabolismo , Transfección , Proteínas Ubiquitinadas/metabolismo , Regulación hacia Arriba/genética , beta-Galactosidasa/metabolismo , Fosfatasas cdc25/genética , Fosfatasas cdc25/metabolismo
5.
Bioorg Med Chem Lett ; 19(19): 5657-60, 2009 Oct 01.
Artículo en Inglés | MEDLINE | ID: mdl-19699641

RESUMEN

A 43-member 1,2-dioxolane library was synthesized by coupling a 1,2-dioxolane-3-acetic acid derivative to a range of amines. Ten compounds had EC(50)s30nM against Plasmodium falciparum 3D7 and Dd2 strains, and another 15 compounds had EC(50)s50nM against both 3D7 and Dd2. The library was then subjected to a range of in vitro DMPK assays, which revealed that side chains with a heteroatom were required for favorable solubility, LogD and membrane permeability. CYP450 inhibition was isoform dependent, with 2C19 and 3A4 particularly susceptible, and the majority of compounds tested against rat and human microsomes were metabolized rapidly.


Asunto(s)
Antimaláricos/síntesis química , Antimaláricos/metabolismo , Inhibidores Enzimáticos del Citocromo P-450 , Dioxolanos/síntesis química , Dioxolanos/metabolismo , Plasmodium falciparum/efectos de los fármacos , Animales , Antimaláricos/farmacología , Sistema Enzimático del Citocromo P-450/metabolismo , Dioxolanos/farmacología , Humanos , Microsomas Hepáticos/metabolismo , Isoformas de Proteínas/antagonistas & inhibidores , Isoformas de Proteínas/metabolismo , Ratas , Bibliotecas de Moléculas Pequeñas
6.
ACS Appl Mater Interfaces ; 11(35): 31943-31953, 2019 Sep 04.
Artículo en Inglés | MEDLINE | ID: mdl-31407886

RESUMEN

Improving the reversibility of conversion reaction is a promising way to enhance the lithium-ion storage capability of SnO2-based anodes. Herein, we report ferrocene as a novel additive to improve the Li-ion storage performance of the SnO2/graphene (SnO2/G) composite. Through a simple mixing method, ferrocene can be uniformly dispersed into the SnO2/G electrode. It is found that the ferrocene additive can effectively suppress the agglomeration of Sn/SnO2 and retain the nanoscale Sn/Li2O interface. Furthermore, metallic Fe is formed from ferrocene in the discharge process and acts as a catalyst to promote the reversible conversion between Sn/Li2O and SnO2. As a result, the SnO2/G electrode with the addition of 10 wt % ferrocene (10%Fc-SnO2/G) exhibits a superior Li-ion storage performance. It displays a reversible capacity of up to 1084.5 mAh g-1 at 0.1 A g-1 after 150 cycles with a good rate capability (752 mAh g-1 at 1 A g-1). In addition, the 10%Fc-SnO2/G electrode can retain a capacity of 787.2 mAh g-1 at 0.5 A g-1 after 220 cycles. This work demonstrates the promising additive of ferrocene in enhancing the reversible capacity of SnO2-based anodes for lithium-ion batteries.

7.
SLAS Discov ; 24(2): 111-120, 2019 02.
Artículo en Inglés | MEDLINE | ID: mdl-30589598

RESUMEN

SLC6A19 (B0AT1) is a neutral amino acid transporter, the loss of function of which results in Hartnup disease. SLC6A19 is also believed to have an important role in amino acid homeostasis, diabetes, and weight control. A small-molecule inhibitor of human SLC6A19 (hSLC6A19) was identified using two functional cell-based assays: a fluorescence imaging plate reader (FLIPR) membrane potential (FMP) assay and a stable isotope-labeled neutral amino acid uptake assay. A diverse collection of 3440 pharmacologically active compounds from the Microsource Spectrum and Tocriscreen collections were tested at 10 µM in both assays using MDCK cells stably expressing hSLC6A19 and its obligatory subunit, TMEM27. Compounds that inhibited SLC6A19 activity in both assays were further confirmed for activity and selectivity and characterized for potency in functional assays against hSLC6A19 and related transporters. A single compound, cinromide, was found to robustly, selectively, and reproducibly inhibit SLC6A19 in all functional assays. Structurally related analogs of cinromide were tested to demonstrate structure-activity relationship (SAR). The assays described here are suitable for carrying out high-throughput screening campaigns to identify modulators of SLC6A19.


Asunto(s)
Sistemas de Transporte de Aminoácidos Neutros/antagonistas & inhibidores , Bioensayo/métodos , Sistemas de Transporte de Aminoácidos Neutros/metabolismo , Animales , Línea Celular , Fluorescencia , Humanos , Marcaje Isotópico , Potenciales de la Membrana , Xenopus laevis
8.
PLoS One ; 7(3): e33823, 2012.
Artículo en Inglés | MEDLINE | ID: mdl-22457791

RESUMEN

Increased metabolism is a requirement for tumor cell proliferation. To understand the dependence of tumor cells on fatty acid metabolism, we evaluated various nodes of the fatty acid synthesis pathway. Using RNAi we have demonstrated that depletion of fatty-acid synthesis pathway enzymes SCD1, FASN, or ACC1 in HCT116 colon cancer cells results in cytotoxicity that is reversible by addition of exogenous fatty acids. This conditional phenotype is most pronounced when SCD1 is depleted. We used this fatty-acid rescue strategy to characterize several small-molecule inhibitors of fatty acid synthesis, including identification of TOFA as a potent SCD1 inhibitor, representing a previously undescribed activity for this compound. Reference FASN and ACC inhibitors show cytotoxicity that is less pronounced than that of TOFA, and fatty-acid rescue profiles consistent with their proposed enzyme targets. Two reference SCD1 inhibitors show low-nanomolar cytotoxicity that is offset by at least two orders of magnitude by exogenous oleate. One of these inhibitors slows growth of HCT116 xenograft tumors. Our data outline an effective strategy for interrogation of on-mechanism potency and pathway-node-specificity of fatty acid synthesis inhibitors, establish an unambiguous link between fatty acid synthesis and cancer cell survival, and point toward SCD1 as a key target in this pathway.


Asunto(s)
Apoptosis/fisiología , Ácidos Grasos Monoinsaturados/metabolismo , Neoplasias/patología , Estearoil-CoA Desaturasa/antagonistas & inhibidores , Línea Celular Tumoral , Humanos , Estearoil-CoA Desaturasa/fisiología
9.
Bioorg Med Chem Lett ; 13(24): 4463-6, 2003 Dec 15.
Artículo en Inglés | MEDLINE | ID: mdl-14643347

RESUMEN

Ureas of 5-aminopyrazole and 2-aminothiazole emerged as lead compounds from a high-throughput screen assaying the growth of Staphylococcus aureus. Structure-activity relationships were developed for each compound series. Several compounds were also tested for activity against drug resistant strains of S. aureus in vivo.


Asunto(s)
Antibacterianos/síntesis química , Bacterias Grampositivas/efectos de los fármacos , Pirazoles/síntesis química , Pirazoles/farmacología , Tiazoles/síntesis química , Tiazoles/farmacología , Urea/análogos & derivados , Urea/síntesis química , Antibacterianos/química , Antibacterianos/farmacología , Resistencia a la Meticilina , Pruebas de Sensibilidad Microbiana , Conformación Molecular , Estructura Molecular , Pirazoles/química , Staphylococcus aureus/efectos de los fármacos , Relación Estructura-Actividad , Tiazoles/química , Urea/química , Urea/farmacología
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