Specific Modulation of Protein Activity by Using a Bioorthogonal Reaction

Unnatural amino acids with bioorthogonal reactive groups have the potential to provide a rapid and specific mechanism for covalently inhibiting a protein of interest. Here, we use mutagenesis to insert an unnatural amino acid containing an azide group (Z) into the target protein at positions such that a “click” reaction with an alkyne modulator (X) will alter the function of the protein. This bioorthogonally reactive pair can engender specificity of X for the Z‐containing protein, even if the target is otherwise identical to another protein, allowing for rapid target validation in living cells. We demonstrate our method using inhibition of the Escherichia coli enzyme aminoacyl transferase by both active‐site occlusion and allosteric mechanisms. We have termed this a “clickable magic bullet” strategy, and it should be generally applicable to studying the effects of protein inhibition, within the limits of unnatural amino acid mutagenesis.     

Selenium dioxide reaction of substituted diphenacyl sulfides: generation of α -ketoacids

The attempted selenium dioxide oxidation of substituted diphenacyl sulfides in anticipation of further functionalization led to a series of α -ketoacids 3 via oxidation followed by C?S bond cleavage. Two minor products, 5 and 6, have also been isolated and a mechanistic pathway for the formation of 3, 5 and 6 has been proposed.     

Self-consistent 3-D numerical modeling of a uniformly doped nanoscale FinFET using interpolating wavelets

A three-dimensional numerical modeling of a uniformly doped nanoscale FinFET including quantum-mechanical effects has been developed. A self-consistent solution of 3D Poisson-Schr?dinger equation has been obtained using multiresolution approach to achieve adaptively refined mesh that can be used to get a solution with the same level of accuracy of a reference, but with a considerable lower number of points. To the best of our knowledge, this is the first approach for the self-consistent solution to surface potential computations of nanoscale FinFET device using interpolating wavelets. It performs an efficient computation by dynamically adjusting the computational mesh in order to obtain surface potential variations during simulation. This method allows non-uniform grids and scales the CPU time linearly with the number of mesh points. The exact potential profile, subthreshold swing (S) and threshold voltage (V _th) rolloff are estimated. The accuracy of the model has been verified with finite difference, finite element and experimental results. This method provides more accurate results than other existing methods.     

Synthesis,characterization and properties of photoresponsive polymers comprising photocrosslinkable pendant chalcone moieties

New methacrylate monomers, namely 4‐methacryloyloxyphenyl‐4′‐fluorostyryl ketone and 4‐methacryloyloxyphenyl‐4′‐ethylstyryl ketone comprising a free radical polymerizable group and a photocrosslinkable group, were synthesized by reacting the respective hydroxychalcones with methacryloyl chloride in the presence of triethylamine. The monomers were polymerized in the presence of ethyl methyl ketone (EMK) at 70 °C using benzoyl peroxide as the initiator. The chemical structures were characterized using various spectroscopic techniques: ultraviolet, Fourier transform infrared, ¹H NMR and ¹³C NMR. The thermal stability of the polymers was studied using thermogravimetric analysis in nitrogen atmosphere. Differential scanning calorimetry was used to determine the glass transition temperature of the homopolymers. Photocrosslinking of the synthesized homopolymers was investigated in solution. The two homopolymers were crosslinked within 10–15 min. After crosslinking, the homopolymers were insoluble in the same solvent. Copyright © 2006 Society of Chemical Industry     

Synthesis and characterization of aromatic/cycloaliphatic poly(amide‐ imide‐imide)s from bis(4‐amino‐ 3,5‐dimethylphenyl) cycloalkane derivatives

A series of novel aromatic diamines containing cycloaliphatic moieties was synthesized by the reaction of cycloalkanones like cyclohexanone and cycloheptanone with 2,6‐dimethylaniline. The tetrimide diacid was synthesized using the prepared diamine with 3,3′,4,4′‐benzophenonetetracarboxylic acid dianhydride/pyromellitic dianhydride and p‐aminobenzoic acid. The polymers were prepared by treating the tetrimide diacid with different aromatic diamines. The structures of the monomers and polymers were identified using elemental analysis and Fourier transform infrared, ¹H NMR and ¹³C NMR spectroscopy. The polymers show excellent solubility. The polymers are amorphous and have high optical transparency. They also show good thermal stability and their T_g value is found to be in the range 268–305 °C. Copyright © 2007 Society of Chemical Industry     

Synthesis and characterisation of organosoluble polyimides containing the anisyl moiety

A new type of diamine monomer containing the anisyl moiety was synthesized via a straight‐forward one‐step procedure. Anisaldehyde was reacted with 2,6‐dimethylaniline in the presence of dry HCl to attain bis(4‐amino‐3,5‐dimethylphenyl)anisylmethane. A series of organo‐soluble polyimides were prepared using the anisyl diamine and various aromatic dianhydrides via a two step method involving thermal imidization. All polyimides are soluble in strong polar solvents such as N‐methyl‐2‐pyrollidone, N,N‐Dimethylformamide, and N,N‐DimethylAcetamide. The polyimides show excellent thermal stability and good mechanical properties. The glass transition temperatures of the polyimides are in the range 265–294 °C. The tensile strengths are in the range 79–99 MPa and the temperatures at which 10 % weight loss occurs are in the range 460–496 °C. Copyright © 2004 Society of Chemical Industry     

Study of Magnetic and Electrical Properties of Poly(o-phenylenediamine)/Manganese Substituted ZnFe2O4 Nanocomposites

Journal of Inorganic and Organometallic Polymers and Materials - Different concentrations of ZnFe2O4 and manganese substituted ZnFe2O4 nanoparticles (10%, 20% and 30%) dispersed...     

Improvement of tea leaves fermentation with Aspergillus spp. pectinase

The pectinase enzymes isolated from Aspergillus spp., A. indicus, A. flavus and A. niveus were used for fermentation of tea leaves. The enzymes were purified and characterized. The effect of both crude enzyme preparation and purified pectinase enzymes on the improvement of tea leaf fermentation were determined in terms of theaflavin, thearubigin, high polymerized substances, total liquor colour, dry matter content and total soluble solids of the tea produced. The crude enzyme preparations obtained from ethanol precipitation were found to be more effective in improving tea leaf fermentation than the purified pectinase enzymes.