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Li Guangdi - - 2014
HIV-1 Gag amino acid substitutions associated with protease inhibitor (PI) treatment have mainly been reported in subtype B, while information on other subtypes is scarce. Using sequences from 11613 patients infected with different HIV-1 subtypes, we evaluated the prevalence of 93 Gag amino acid substitutions and their association with genotypic ...
Han Xin X School of Pharmaceutical Sciences, State Key Laboratory of Virology, Wuhan University, Wuhan, - - 2014
A series of non-nucleoside reverse transcriptase inhibitors derived from indole-based α-amino acids were designed and synthesized. Their inhibitory activities were detected by a TZM-bl cell assay on HIV virus type HIV-1IIIB. The comprehensive understanding of the SAR was obtained by utilizing the variation of the substituents of the indole-based α-amino ...
Cashin Kieran K Center for Biomedical Research, Burnet Institute, Melbourne, Australia; Department of Microbiology and Immunology, University of Melbourne, Melbourne, - - 2014
The ability to determine coreceptor usage of patient-derived human immunodeficiency virus type 1 (HIV-1) strains is clinically important, particularly for the administration of the CCR5 antagonist maraviroc. The envelope glycoprotein (Env) determinants of coreceptor specificity lie primarily within the gp120 V3 loop region, although other Env determinants have been shown ...
Meixenberger Karolin K HIV and Other Retroviruses, Robert Koch Institute, Berlin, - - 2014
Introduction: The aim of our study was to analyze the occurrence and evolution of HIV-1 integrase polymorphisms during the HIV-1 epidemic in Germany prior to the introduction of the first integrase inhibitor raltegravir in 2007. Materials and Methods: Plasma samples from drug-naïve HIV-1 infected individuals newly diagnosed between 1986 and ...
Oh Young Taek YT Department of Physiology and Biophysics, University of Southern California, Keck School of Medicine, Los Angeles, CA, - - 2013
We previously showed that a fall in plasma FFA level increases plasma corticosterone levels in rats by activating the hypothalamic-pituitary-adrenal (HPA) axis. In the present study, we tested whether this regulation is mediated by specific or all species of FFA. Nicotinic acid (NA; 30 μ mol/h) was infused in rats ...
Garrel Ghislaine - - 2013
Reproductive function is highly dependent on nutritional input. We recently provided evidence that the unsaturated ω6 fatty acid, linoleic acid (linoleic), interferes with transcription and secretion of the gonadotropin LH, highlighting the existence of a lipid sensing in pituitary gonadotropes. Here, we show using a combination of in vivo and ...
Mocking Roel J T - - 2013
Alterations in hypothalamic-pituitary-adrenal (HPA)-axis activity and fatty acid (FA)-metabolism have been observed in (recurrent) major depressive disorder (MDD). Through the pathophysiological roles of FAs in the brain and cardiovascular system, a hypothesized relationship between HPA-axis activity and FA-metabolism could form a possible missing link accounting for the association of HPA-axis ...
Miles Anna - - 2012
This study investigated the inter-rater and intra-rater reliability of subjective judgements of cough in patients following inhalation of citric acid. Eleven speech-language pathologists (SLPs) currently using cough reflex testing in their clinical practice (experienced raters) and 34 SLPs with no experience using cough reflex testing (inexperienced raters) were recruited to ...
Mishra Swati S Department of Biomedical Engineering, Rutgers, The State University of New Jersey, Piscataway, 08854, United - - 2012
The advancement of gene-based therapeutics to the clinic is limited by the ability to deliver physiologically relevant doses of nucleic acids to target tissues safely and effectively. Over the last couple of decades, researchers have successfully employed polymer and lipid based nanoassemblies to deliver nucleic acids for the treatment of ...
Yang Chuan - - 2012
A new series of acid- and urea-functionalized polycarbonate block copolymers were synthesized via organocatalytic living ring-opening polymerization using methoxy poly(ethylene glycol) (PEG) as a macroinitiator to form micelles as drug delivery carriers. The micelles were characterized for critical micelle concentration, particle size and size distribution, kinetic stability and loading capacity ...
Lichtenstein Bruce R - - 2012
As a prelude to engineering artificial energy conversion proteins emulating biology, we examine the inclusion of a synthetic naphthoquinone amino acid in a characterized host-guest protein and determine the effects of its quinone and hydroquinone forms on the helix-coil distribution.
Marchesan Silvia - - 2011
Change of chirality of the first N-terminal amino acid of tripeptides VFF and FFV from l to d results in self-assembled hydrogels at physiological pH from non-assembling l-analogues. Interestingly, changing the chirality of F yields very different nanostructures; nanotapes are observed for (D)VFF, twisted fibers for (D)FFV.
Azizian Homa - - 2012
Here, we report a structure-based virtual screening of the ZINC database (containing about five million compounds) by computational docking and the analysis of docking energy calculations followed by in vitro screening against H. pylori urease enzyme. One of the compounds selected showed urease inhibition in the low micromolar range. Barbituric ...
Ozcan Mehmet Musa - - 2011
Percentages of crude oil, protein, fibre and ash of grape seeds obtained from Turkish cultivars were of the ranges 5.40-10.79, 5.24-7.54, 17.6-27.1, and 1.2-2.6, respectively. The highest crude oil, crude protein and crude fibre were determined in Siyah pekmezlik, Karadimrit and Antep grape seeds. The energy values of seeds were ...
Hon Gloudina Maria - - 2011
The aim of this study was to investigate whether blood cell membrane monounsaturated fatty acids were associated with inflammation and disease outcome in patients with multiple sclerosis. The fatty acid composition in peripheral blood mononuclear cell and red blood cell membranes from 26 patients and 25 controls were determined by ...
Bowman T T Department of Food Science and Technology, Ohio State University, Columbus, OH 43210, - - 2012
Pumpkin (Cucurbita pepo and maxima) seeds are uniquely flavored and commonly consumed as a healthy roasted snack. The objective was to determine dominant volatiles in raw and roasted pumpkin seeds, and the effect of seed coat, moisture content, fatty acid ratio, total lipids, reducing sugars, and harvest year on volatile ...
Iqbal Javed J Department of Pharmaceutical Technology, Leopold-Franzens-University Innsbruck, Innsbruck, Austria. - - 2012
This study was aimed to synthesize polymeric excipients with improved mucoadhesive, cohesive and in situ-gelling properties to assure a prolonged retention time of dosage forms at a given target site, thereby achieving an increased uptake and improved oral bioavailability of certain challenging therapeutic agents such as peptides and proteins. Accordingly, ...
Li Wei - - 2012
Novel phenoxyalkylcarboxylic acid derivatives based on the natural scaffolds, flavonoids, or resveratrol were designed, synthesized, and evaluated for hypolipidaemic activity. Among the compounds, 30b lowered the triglycerides by 48.5% (P < 0.05) and total cholesterol by 44.2% (P < 0.05), respectively, and was more effective than the reference drug fenofibric acid in a Triton ...
Sanyal Anushree - - 2011
Fatty acid composition is an important determinant of seed oil quality. Overall, 72 QTL for 12 fatty acid traits that control seed oil composition were identified in four recombinant inbred line (RIL) populations (Ler-0 × Sha, Ler-0 × Col-4, Ler-2 × Cvi, Ler-0 × No-0) of Arabidopsis thaliana. The identified QTL explained 3.2-79.8% of the phenotypic variance; 33 ...
Khan Wahid - - 2011
In the past three decades, the use of polymeric materials has increased dramatically for biomedical applications. Many α-amino acids derived biodegradable polymers have also been intensely developed with the main goal to obtain bio-mimicking functional biomaterials. Polymers derived from α-amino acids may offer many advantages, as these polymers: (a) can ...
Schrumpf Mark A - - 2011
Polyglycolic acid and poly-L-lactic acid have become popular choices for bioabsorbable anchor fixation in the hand and wrist. We report a case of osteolysis, synovitis, and chondral erosion secondary to a poly-L-lactic acid suture anchor in the wrist.
Hilbold Benoît - - 2011
Hydrophobic photoaffinity labeling is a powerful strategy to identify hydrophobic segments within molecules, in particular membrane proteins. Here we report the design and synthesis of a novel family of fluorescent and photosensitive lipid tools, which have a common amino acid scaffold functionalized by three groups: (i) a first fatty acid ...
Xin Zhili - - 2011
Starting from literature examples of nonsteroidal anti-inflammatory drugs (NSAIDs)-type carboxylic acid γ-secretase modulators (GSMs) and using a scaffold design approach, we identified 4-aminomethylphenylacetic acid 4 with a desirable γ-secretase modulation profile. Scaffold optimization led to the discovery of a novel chemical series, represented by 6b, having improved brain penetration. Further ...
Yuan Qiang - - 2011
High-selectivity, uniform three-dimensional (3D) flower-like bismuth telluride (Bi(2)Te(3)) nanocrystals consisting of few-quintuple-layer nanoplatelets with a thickness down to 4.5 nm were synthesized for the first time by a facile, one-pot polyol method with acetic acid as the structure-director. Micrometre-sized 2D films and honeycomb-like spheres can be obtained using the uniform ...
Muranaka Kazuhiro - - 2011
The new carboxamide protecting group, 4-(tert-butyldimethylsiloxy)-2-methoxybenzyl (SiMB), has been developed. While this SiMB group can be removed using mild basic desilylation methods, it can also be deprotected under strongly acidic or oxidative conditions. An application of this group to not only simple carboxamide groups, as well as to more complex ...
Brownson Dale A C - - 2011
We investigate the electrochemical properties of CVD grown graphene towards the detection of various biologically prevalent analytes including l-ascorbic acid (AA), dopamine hydrochloride (DA), β-nicotinamide adenine dinucleotide (NADH), uric acid (UA) and epinephrine (EP). We find that the observed electrochemical response of the CVD-graphene towards these select analytes does not ...
Zhou Weimin - - 2011
Electrical conductivity was obtained in hybrid organic nanofibers fabricated with low-molecular-weight amphiphilic azopyridinium and dodecylbenzenesulfonic acid or its salt.
Li Xinming X Department of Chemistry, Brandeis University, Waltham, Massachusetts 02454, - - 2011
The integration of nucleobase, amino acid, and glycoside into a single molecule results in a novel class of supramolecular hydrogelators, which not only exhibit biocompatibility and biostability but also facilitate the entry of nucleic acids into cytosol and nuclei of cells. This work illustrates a simple way to generate an ...
André Christophe - - 2011
Constrained enantiopure bicyclic β-amino acids derived from the asymmetric Diels-Alder reaction of the (R)-benzyl-4-(3-acryloyloxy-4,4-dimethyl-2-oxopyrrolidin-1-yl)-benzoate and the 1-(benzyloxycarbonylamino)cyclohexadiene provide original templates for the construction of new rigid enantiopure 1,3-amino alcohols.
Chouaibi Moncef - - 2011
BACKGROUND: Zizyphus lotus seeds are an unutilized source of vegetable oil and protein and nothing has been reported on their physicochemical characteristics which would indicate the potential uses of these seeds. RESULTS: The percentage composition of the Zizyphus lotus seeds is (on a dry-weight basis): ash 1.05%, oil 32.92%, protein ...
Huang Meixia - - 2011
The purpose of this study was to prepare a propyl gallate (PrG) molecular imprinted polymer as a cartridge stuffing material to isolate antiplatelet active ingredients. A macroporous polymer was synthesized utilizing ethylene glycol dimethacrylate (EDMA) as the crosslinking agent, PrG as the template molecule and 4-vinylpyridine (4-Vpy) as the functional ...
Lockner Jonathan W JW Department of Chemistry, The Scripps Research Institute, 10550 North Torrey Pines Road, La Jolla, California 92037, - - 2011
Practical radical cyclizations using organoboronic acids and trifluoroborates take place in water, open to air, and in a scalable fashion employing catalytic silver nitrate and stoichiometric potassium persulfate. Both Pschorr-type cyclizations and tandem radical cyclization/trap cascades are described, illustrating the utility of these mild conditions for the generation of polycyclic ...
Roodhart Jeanine M L - - 2011
The development of resistance to chemotherapy is a major obstacle for lasting effective treatment of cancer. Here, we demonstrate that endogenous mesenchymal stem cells (MSCs) become activated during treatment with platinum analogs and secrete factors that protect tumor cells against a range of chemotherapeutics. Through a metabolomics approach, we identified ...
Félix Lanao Rosa P - - 2011
Apatitic calcium phosphate cements (CPC) are frequently used to fill bone defects due to their favourable clinical handling and excellent bone response, but their lack of degradability inhibits complete bone regeneration. In order to render these injectable CaP cements biodegradable, hollow microspheres made of poly (D,L-lactic-co-glycolic) acid (PLGA) have been ...
Meyers Marvin J - - 2011
Herein we report the identification of two new fatty acid amide hydrolase (FAAH) inhibitor lead series with FAAH k(inact)/K(i) potency values greater than 1500M(-1)s(-1). The two novel spirocyclic cores, 7-azaspiro[3.5]nonane and 1-oxa-8-azaspiro[4.5]decane, clearly distinguished themselves from the other spirocyclic cores on the basis of their superior potency for FAAH. Lead ...
Zanon Nathaly C M - - 2011
Preserving the enzyme structure in solid films is key for producing various bioelectronic devices, including biosensors, which has normally been performed with nanostructured films that allow for control of molecular architectures. In this paper, we investigate the adsorption of uricase onto Langmuir monolayers of stearic acid (SA), and their transfer ...
Robertson Megan L - - 2011
Poly(l-lactide) (PLLA) is a renewable resource polymer derived from plant sugars with several commercial applications. Broader implementation of the material is limited due to its inherent brittleness. We show that the addition of 5 wt % castor oil to PLLA significantly enhances the overall tensile toughness with minimal reductions in ...
Hieke Martina - - 2011
A novel set of dual γ-secretase/PPARγ modulators characterized by a 2-benzyl hexanoic acid scaffold is presented. Synthetic efforts were focused on the variation of the substitution pattern of the central benzene. Finally, we obtained a new class of 2,5-disubstituted 2-benzylidene hexanoic acid derivatives, which act as dual γ-secretase/PPARγ modulators in ...
Kohut Ananiy - - 2011
"Host-guest" interactions between amphiphilic invertible macromolecules based on PEG and sebacic acid, and cyclohexasilane (Si6H12) in acetonitrile (neither a solvent for cyclohexasilane, nor supporting micellization of amphiphilic invertible macromolecules) have been investigated. Despite the extended conformation of the AIP macromolecules and the absence of self-assembled polymeric domains, an AIP amphiphilicity ...
Walvoort Marthe T C - - 2011
With the aim to find an efficient synthetic procedure for the construction of 2,3-diamino-2,3-dideoxy-beta-D-mannuronic acids we evaluated three mannosyl donors: S-phenyl 4,6-di-O-acetyl-2,3-diazido mannopyranoside, S-phenyl 2,3-diazido-4,6-O-benzylidene mannopyranoside and S-phenyl 2,3-diazido mannopyranosyl methyl uronate. The first two mannosylating agents are rather unselective or slightly alpha-selective in their condensation with three different acceptors. ...
Barbanti Samuel H - - 2011
Porous bioresorbable polymers have been widely used as scaffolds in tissue engineering. Most of the bioresorbable scaffolds are aliphatic polyesters and the methods employed to prepare the porous morphology may vary. This work describes and evaluates the in vitro degradation of porous and dense scaffolds of poly(ε-caprolactone) (PCL) and poly(D,L: ...
Pálková Helena - - 2011
The effect of short alkyl chain cations on the modification of the structure, surface and textural properties of organo-montmorillonites upon their acid treatment was investigated. Samples prepared from Ca-SAz montmorillonite and tetramethylammonium (Me(4)N(+)-), tetraethylammonium (Et(4)N(+)-), tetrapropylammonium (Pr(4)N(+)-) and tetrabutylammonium (Bu(4)N(+)-) salts were treated in 6M HCl at 80°C for 2-8h ...
Li Yinli - - 2011
By using the layer-by-layer deposition method, we build three dimensional (3D) supramolecular nanostructures by stacking small molecular species on top of the first buffer layer, which can be utilized to fabricate novel 3D supramolecular functional nanostructures.
Ko Yoon-Joo - - 2011
Understanding and controlling aggregation structures of conjugated polymers (CPs) in aqueous solutions is critical to improving the physical and photophysical properties of CPs for biological applications. Here, we present spectroscopic evidence, including nuclear magnetic resonance (NMR) spectroscopic results, that different organic acid treatment induces different aggregation structures and photophysical properties ...
Potekhina N V - - 2011
Anionic phosphate-containing cell wall polymers of bacilli are represented by teichoic acids and poly(glycosyl 1-phosphates). Different locations of phosphodiester bonds in the main chain of teichoic acids as well as the nature and combination of the constituent structural elements underlie their structural diversity. Currently, the structures of teichoic acids of ...
Zall Andrea - - 2011
Modulation of γ-secretase activity holds potential for the treatment of Alzheimer's disease. Most NSAID-derived γ-secretase modulators feature a carboxylic acid, which may impair blood-brain barrier permeation. The structure activity relationship of 33 carbazoles featuring diverse carboxylic acid isosteres or metabolic precursors thereof was established in a cellular amyloid secretion assay. ...
Robertson Mark - - 2011
The synthesis of eleven novel antibacterial agents is reported. The structures are based on a C(2)-symmetric binaphthyl scaffold which holds two identical chains consisting of a short linker, a basic amino acid and a small hydrophobic side chain. Antibacterial activity is revealed for a number of derivatives down to an ...
Park Jason - - 2011
Biodegradable polymeric nanoparticles are widely recognized as efficacious drug delivery vehicles, yet the rational engineering of nanoparticle surfaces in order to improve biodistribution, reduce clearance, and/or improve targeting remains a significant challenge. We have previously demonstrated that an amphiphilic conjugate of avidin and palmitic acid can be used to modify ...
Natalini Benedetto - - 2011
The successful enantioseparation of five 6-desfluoroquinolones with three polysaccharide-based stationary phases (namely, the cellulose-based Chiralpak IB and the two amylose-based Chiralpak AD-H and Lux Amylose-2) is herein described. The investigated species differ for the nature of substituents and/or the position of the stereogenic centre on the quinolone scaffold. The effect ...
Touaibia M - - 2011
The caffeic acid scaffold, which is abundant in nature, is extremely versatile and is found in a number of biologically active molecules. The purpose of this review is to provide an overview of the pharmacological activity of synthetic caffeic acid analogs including recent reports of anti-inflammatory, anti-cancer, and antiviral activities ...
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