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optoelectronic devices.Aberrant hedgehog (Hh) signaling is implicated in the development of a variety of cancers. Smoothened (Smo) protein is a bottleneck in the Hh signal transduction. The regulation of the Hh signaling pathway to target the Smo receptor is a practical approach for development of anticancer agents. We report herein the design and synthesis of a series of 2-methoxybenzamide derivatives as Hh signaling pathway inhibitors. The pharmacological data demonstrated that compound 21 possessed potent Hh pathway inhibition with a nanomolar IC50 value, and it prevented Shh-induced Smo from entering the primary cilium. Furthermore, mutant Smo was effectively suppressed via compound 21. The in vitro antiproliferative activity of compound 21 against a drug-resistant cell line gave encouraging results.Chemical reactions are powerful molecular recognition machines. This power has been recently harnessed to build actual instances of each class of experimentally realizable computing automata, using exclusively small-molecule chemistry (i.e. without requiring biomolecules). The most powerful of them, a programmable Turing machine, uses the Belousov-Zhabotinsky oscillatory chemistry, and accepts/rejects input sequences through a dual oscillatory and thermodynamic output signature. The time interval between the aliquots representing each letter of the input is the parameter that determines the time it takes to run the computation. Here, we investigate this critical performance parameter, and its effect not only on the computation speed, but also on the robustness of the accept/reject oscillatory and thermodynamic criteria. Our work demonstrates that the time interval is a non-trivial design parameter, whose choice should be made with great care. The guidelines we provide can be used in the optimization of the speed, robustness, and energy efficiency of chemical automata computations.Owing to the high sensitivity, fast responsiveness and high specificity, immunoassays using surface-enhanced Raman scattering (SERS) as the readout signal displayed great potential in disease diagnosis. In this study, we developed a SERS-immunoassay method for the detection of human immunoglobulin G (HIgG). Upon involving well-ordered AuA on a SERSIA substrate, the LSPR effect was further enhanced to generate a strong and uniform Raman signal through the formation of sandwich structure with the addition of target HIgG and SERSIA tag. Optimization of the assay provided a wide linear range (0.1-200 μg mL-1) and low limit of detection (0.1 μg mL-1). In addition, the SERS-immunoassay method displayed excellent specificity and was homogeneous, which guaranteed the practical use of this method in the quantitative detection of HIgG. To validate this assay, human serum was analysed, which demonstrated the potential advantages of SERS-immunoassay technology in clinical diagnostics.To enhance the photocatalytic water splitting performance of 2D ReS2, we theoretically propose a feasible strategy to engineer its band structure by applying strain or an electric field. Our calculated results show that the strains greatly tune the electronic structure of ReS2 especially band gap and band edge positions, because the strains significantly alter the crystal structure and then cause rearrangement of the surface charge. However, electric fields have little influence on band gap but obviously affect the band edge positions. This is because the electric fields have little effect on the crystal structure of ReS2 but easily produce an in-plane electric dipole moment. The shifts in band edge position mainly arise from competition between the surface charge and the in-plane electric dipole. For an applied strain, the shifts are dominated by rearrangement of surface charge; for an applied electric field, the shifts are determined by an induced electric dipole moment. Importantly, functionalized ReS2 with a bi-axial strain of -4% or an electronic field of -0.1 V Å-1 may be good candidates for water-splitting photocatalysts owing to their suitable band edge positions for water splitting, ideal band gaps, good stability, reduced electron-hole recombination and high carrier mobility. We hope our findings will stimulate experimental efforts to develop new photocatalysts based on functionalized ReS2.Zinc oxide (ZnO) is a II-VI group semiconductor with a wide direct bandgap and is an important material for various fields of industry and high-technological applications. The effects of thickness, annealing process in N2 and air, optical properties, and morphology of ZnO thin-films are studied. A low-cost sol-gel spin-coating technique is used in this study for the simple synthesis of eco-friendly ZnO multilayer films deposited on (100)-oriented silicon substrates ranging from 150 to 600 nm by adjusting the spin coating rate. The ZnO sol-gel thin-films using precursor solutions of molarity 0.75 M exhibit an average optical transparency above 98%, with an optical band gap energy of 3.42 eV. The c-axis (002) orientation of the ZnO thin-films annealed at 400 °C were mainly influenced by the thickness of the multilayer, which is of interest for piezoelectric applications. These results demonstrate that a low-temperature method can be used to produce an eco-friendly, cost-effective ZnO sol-gel that is compatible with a complementary metal-oxide-semiconductor (CMOS) and integrated-circuits (IC).Traumatic optic neuropathy (TON) describes an injury to the optic nerve following either blunt or penetrating trauma, and remains an important cause of vision loss. No generalized treatment of TON has been established so far to restore the injured optic nerve. We developed an adherent drug-encapsulated bi-layered depot (DBP) as a dual drug vehicle for local treatment to protect the residual retinal ganglion cells (RGCs) and regenerate axons following optic nerve damage. The inner layer of the depot was prepared by co-electrospinning poly(d,l-lactide-co-glycolide acid) (PLGA 75 25) and collagen (COL) with the hydrophobic corticosteroid triamcinolone acetonide (TA) loaded. The outer layer was made of PLGA and the hydrophilic neuroprotective agent Fasudil (FA). The DBP showed suitable morphology, hydrophilicity and mechanical properties, and slowly released TA and FA in vitro by undergoing time-dependent degradation and swelling. All depots showed good biocompatibility with L929 mouse fibroblasts, and DBP was helpful in maintaining the morphology of RGCs in vitro. In addition, direct implantation of DBP at the injured optic nerve in a rat model mitigated inflammation and the death of RGCs, and increased the expression of nerve growth-related protein GAP-43. Therefore, DBP maybe a promising local therapy against TON in future.Water was magnetized via an external magnetic field and employed, for the first time, as a solvent in green preparation of 3,4-dihydropyrimidin-2(1H)-ones by the one-pot three-component condensation reaction using boric acid as a catalyst. Shorter reaction times, higher yields, and cleaner reaction profiles were some advantages of using magnetic water.Detection of NO2 plays an important role in various safety applications. However, sensitive and reversible sensing of NO2 remains a challenge. Here we demonstrate the use of poly(3,4-ethylenedioxythiophene) (PEDOT) conducting polymer percolation networks for chemiresistive sensing of NO2. By adjusting the electrochemical polymerisation and doping conditions of the polymer, we show control over the relative contributions of oxidised and over-oxidised PEDOT to the sensing behaviour. Reversible NO2 sensors using only PEDOT as the sensor material are demonstrated. By operating the sensor near the electrical percolation threshold, a higher sensitivity is achieved compared to more traditional thin film based chemiresistive sensors. A limit of detection of 907 ± 102 ppb was achieved.Butelase-1, an asparaginyl endopeptidase or legumain, is the prototypical and fastest known Asn/Asp-specific peptide ligase. It is highly useful for engineering and macrocyclization of peptides and proteins. However, certain biochemical properties and applications of naturally occurring and recombinant butelase-1 remain unexplored. Here we report methods to increase the yield of natural and bacterial expressed recombinant butelase-1 and how they can be used to improve the stability and activity of two important industrial enzymes, lipase and phytase, by end-to-end circularization. First, the yield of natural butelase-1 was increased 3-fold to 15 mg kg-1 by determining its highest distribution which is found in young tissues, such as shoots. The yield of recombinantly-produced soluble butelase-1 was improved by promoting cytoplasmic disulfide folding, codon changes, and truncation of the N-terminal pro-domain. Natural and recombinant butelase-1 displayed similar ligase activity, physical stability, and salt tolerance. Furthermore, the processing and glycosylation sites of natural and recombinant butelase-1 were determined by proteomic analysis. Storage conditions for both forms of butelase-1, frozen or lyophilized, were also optimized. Cyclization of lipase and phytase mediated by either soluble or immobilized butelase-1 was highly efficient and simple, and resulted in increased thermal stability and enhanced enzymatic activity. Overall, improved production of butelase-1 can be exploited to improve the biocatalytic efficacy of lipase and phytase by end-to-end cyclization. In turn, ligase-improved enzymes could be a general and environmentally friendly strategy for producing more stable and efficient industrial enzymes.Hydrazine (N2H4) is one of the commonly used chemical reagents in numerous industries and applications but its toxicity to humans poses a need to develop simple visual detection methods. Herein, we demonstrate a novel dual-mode system to detect and simultaneously consume hydrazine in vapour and solution by using a small photoresponsive molecule that has altered optical response (both colourimetric and fluorescent) after reacting with hydrazine.In this study, gel polymer electrolytes (GPEs) were prepared using polyacrylonitrile (PAN) polymer, ethylene carbonate (EC), propylene carbonate (PC) plasticizers and different compositions of tetrapropylammonium iodide (TPAI) salt. Linear sweep voltammetry (LSV) and electrochemical impedance spectroscopy (EIS) measurements were done using non-blocking Pt-electrode symmetric cells. The limiting current (J lim), apparent diffusion coefficient of triiodide ions and exchange current were found to be 12.76 mA cm-2, 23.41 × 10-7 cm2 s-1 and 11.22-14.24 mA cm-2, respectively, for the GPE containing 30% TPAI. These values are the highest among the GPEs with different TPAI contents. To determine the ionic conductivity, the EIS technique was employed with blocking electrodes. The GPE containing 30% TPAI exhibited the lowest bulk impedance, R b (22 Ω), highest ionic conductivity (3.62 × 10-3 S cm-1) and lowest activation energy. find more Fourier transform infrared (FTIR) spectroscopy and X-ray diffraction (XRD) techniques were utilized for structural characterization. Functional group interactions among PAN, EC, PC and TPAI were studied in the FTIR spectra of the GPEs. An up-shift of the XRD peak indicates the polymer-salt interaction and possible complexation of the cation (TPA+ ion) with the lone pair of electrons containing site -C[triple bond, length as m-dash]N at the N atom in the host polymer matrix. On the other hand, computational study shows that TPAI-PAN based GPE possesses the lowest frontier orbital bandgap, which coincided with the enhanced electrochemical and electrocatalytic performance of GPE. The dye-sensitized solar cell (DSSC) fabricated with these GPEs showed that the J SC (19.75 mA cm-2) and V OC (553.8 mV) were the highest among the GPEs and hence the highest efficiency, η (4.76%), was obtained for the same electrolytes.
Read More: https://www.selleckchem.com/products/c1632.html
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