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Strong Binding (strong + binding)
Selected AbstractsChemInform Abstract: A New Receptor Molecule for Lysine and Histidine in Water: Strong Binding of Basic Amino Acid Esters by a Macrocyclic Host.CHEMINFORM, Issue 37 2001Thomas Grawe Abstract ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 100 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a "Full Text" option. The original article is trackable via the "References" option. [source] Electrochemical Cholesterol Sensor Based on Tin Oxide-Chitosan Nanobiocomposite FilmELECTROANALYSIS, Issue 8 2009Anees Abstract A chitosan (CS)-tin oxide (SnO2) nanobiocomposite film has been deposited onto an indium-tin-oxide glass plate to immobilize cholesterol oxidase (ChOx) for cholesterol detection. The value of the Michaelis,Menten constant (Km) obtained as 3.8,mM for ChOx/CS-SnO2/ITO is lower (8,mM) than that of a ChOx/CS/ITO bioelectrode revealing enhancement in affinity and/or activity of ChOx towards cholesterol and also revealing strong binding of ChOx onto CS-SnO2/ITO electrode. This ChOx/CS-SnO2/ITO cholesterol sensor retains 95% of enzyme activity after 4,6 weeks at 4,°C with response time of 5,s, sensitivity of 34.7,,A/mg dL,1 cm2 and detection limit of 5,mg/dL. [source] Towards Selective Recognition of Sialic Acid Through Simultaneous Binding to Its cis -Diol and Carboxylate FunctionsEUROPEAN JOURNAL OF ORGANIC CHEMISTRY, Issue 17 2010Martín Regueiro-Figueroa Abstract A series of receptors containing phenylboronic acid and urea or thiourea units have been designed for simultaneous recognition of the cis -diol and carboxylate functions of sialic acids, which are known to be overexpressed on the surfaces of tumor cells. The interaction of the receptors with 5-acetylneuraminic acid (Neu5Ac) and 2-,- O -methyl Neu5Ac (MeNeu5Ac) in DMSO solution has been investigated bymeans of spectrophotometric titrations and 1H, 13C, and 11B NMR spectroscopy. Additionally, we have also investigated the binding of these receptors with competing monosaccharides such as D -(+)-glucose, D -fructose, methyl ,- D -galactoside, and methyl ,- D -mannoside. Our results show that 2-{[3-(4-nitrophenyl)thioureido]methyl}phenylboronic acid (3a) recognizes both Neu5Ac and MeNeu5Ac with good selectivity with regard to the remaining monosaccharides investigated. DFT calculations performed at the B3LYP/6-31G(d) level show that this selectivity is due to a cooperative two-site binding of Neu5Ac through 1) ester formation by interaction at the phenylboronic acid function of the receptor and 2) hydrogen-bond interaction between the thiourea moiety and the carboxylate group of Neu5Ac. Compound 3a can therefore be considered a promising synthon for the design of contrast agents for magnetic resonance imaging of tumors. In contrast, the analogue of 3a containing a urea moiety , compound 3b , displays strong binding to all monosaccharides investigated, due to two-site binding through interaction on the phenylboronic acid function of the receptor and a hydrogen-bond interaction between the urea moiety and the sugar hydroxy groups. [source] Dispersive Effects in Chemomechanical Reactions with Polyallylamine-Derived HydrogelsEUROPEAN JOURNAL OF ORGANIC CHEMISTRY, Issue 8 2008Kazuaki Kato Abstract Volume changes of polyallylamine-derived hydrogels crosslinked with glutaraldehyde are determined with a large variety of effector compounds. Monocarboxylic effectors lead to smaller contractions, in contrast to dicarboxylate structures, which allow more effective non-covalent crosslinking between the positively charged nitrogen centers of the polymer backbone. Electroneutral compounds lead to negligible changes, whereas effectors with either a large p -moiety like in naphthoic acid or phenyl derivatives with polarizable substituents induce large contractions. This finding is in line with significant contributions of van der Waals interactions between the effectors within the hydrogel. Chemomechanical differences between regioisomeric effectors such as p - and o -nitrobenzoic acid are in agreement with independent results of dispersive interactions in related complexes. The volume decrease corresponds almost entirely to the gravimetrically determined water content of the gels. The acidity profile shows a strong contraction above pH 10, which is consistent with the known pK value of such polyamines. NMR spectra of the gels indicate strong binding of the effectors by line broadening, which is significant only for the chemomechanically active compounds. (© Wiley-VCH Verlag GmbH & Co. KGaA, 69451 Weinheim, Germany, 2008) [source] Enzymatic and immunochemical evaluation of phospholipid hydroperoxide glutathione peroxidase (PHGPx) in testes and epididymal spermatozoa of rats of different agesINTERNATIONAL JOURNAL OF ANDROLOGY, Issue 2 2002Federica Tramer Selenium (Se) and selenoproteins such as glutathione peroxidases are necessary for the proper development and fertilizing capacity of sperm cells. Phospholipid hydroperoxide glutathione peroxidase (PHGPx, E.C. 1.11.1.12) is a monomeric seleno-enzyme present in different mammalian tissues in soluble and bound form. Its function, like the other glutathione peroxidases, was originally viewed as a protective role against hydroperoxides, but direct and indirect evidence indicates that it has additional regulatory roles. PHGPx is present in testis cells and sperm cells, and its appearance is hormone regulated. We present here biochemical data, which clearly indicate that the enzyme specific activity in rat is age-dependent during the life-span monitored (from 36 to 365 days), with a maximum at 3 months of age in the testis germ cells and at 6 months of age in the isolated epididymal sperm cells. Western blotting and immunocytochemical analysis by means of anti-PHGPx antibodies show the different distribution and the strong binding of PHGPx in the testes and sperm cell subcellular compartments (nucleus, acrosome, mitochondria and residual bodies) of rats of different age. The presence of the protein exhibits in the testis cells a pattern different from that of the catalytic activity, with a maximum at 6 months of age. The subcellular distribution of PHGPx is qualitatively, but not quantitatively, unchanged during ageing. These different behaviours are compared and discussed. [source] Substituent effects of phthalimide-based nucleoside analogs on binding a CG Watson,Crick base pairJOURNAL OF PHYSICAL ORGANIC CHEMISTRY, Issue 10 2007Z. Xiao Abstract Five differently substituted phthalimide nucleosides were studied by NMR spectroscopic techniques for their ability to recognize and bind a cytosine,guanosine (CG) Watson,Crick base pair in CD2Cl2. Whereas only rather weak binding was observed for analogs with an amino, acetamido, or benzamido substituent, strong binding was observed with the analogs carrying an ureido and n -butyl ureido residue. 2D NOE measurements at low temperatures confirm the proposed binding mode for the high-affinity ligands but indicate binding interactions for the weakly bound analogs different from the expected geometry. Copyright © 2007 John Wiley & Sons, Ltd. [source] Paraquat and sustainable agriculturePEST MANAGEMENT SCIENCE (FORMERLY: PESTICIDE SCIENCE), Issue 4 2004Richard H Bromilow Abstract Sustainable agriculture is essential for man's survival, especially given our rapidly increasing population. Expansion of agriculture into remaining areas of natural vegetation is undesirable, as this would reduce biodiversity on the planet. Maintaining or indeed improving crop yields on existing farmed land, whether on a smallholder scale or on larger farms, is thus necessary. One of the limiting factors is often weed control; biological control of weeds is generally of limited use and mechanical control is either often difficult with machinery or very laborious by hand. Thus the use of herbicides has become very important. Minimum cultivation can also be important, as it reduces the power required to work the soil, limits erosion and helps to maintain the organic matter content of the soil. This last aspect helps preserve both the structure of soil and its populations of organisms, and also sustains the Earth's soil as a massive sink for carbon, an important consideration in the light of global warming. The introduction of the bipyridinium herbicide paraquat in the early 1960s greatly facilitated weed control in many crops. Paraquat has the unusual property of being active only by direct spray onto plants and not by uptake from soil in which strong binding deactivates it. Together with its rapid action in light in killing green plant tissue, such properties allow paraquat to be used in many crops, including those grown by low-tillage methods. This paper reviews the ways in which agricultural systems have been and are being developed to make use of these properties, and provides a risk/benefit analysis of the world-wide use of paraquat over nearly 40 years. Copyright © 2004 Society of Chemical Industry [source] Structure of human transthyretin complexed with bromophenols: a new mode of bindingACTA CRYSTALLOGRAPHICA SECTION D, Issue 9 2000Minakshi Ghosh The binding of two organohalogen substances, pentabromophenol (PBP) and 2,4,6-tribromophenol (TBP), to human transthyretin (TTR), a thyroid hormone transport protein, has been studied by in vitro competitive binding assays and by X-ray crystallography. Both compounds bind to TTR with high affinity, in competition with the natural ligand thyroxine (T4). The crystal structures of the TTR,PBP and TTR,TBP complexes show some unusual binding patterns for the ligands. They bind exclusively in the `reversed' mode, with their hydroxyl group pointing towards the mouth of the binding channel and in planes approximately perpendicular to that adopted by the T4 phenolic ring in a TTR,T4 complex, a feature not observed before. The hydroxyl group in the ligands, which was previously thought to be a key ingredient for a strong binding to TTR, does not seem to play an important role in the binding of these compounds to TTR. In the TTR,PBP complex, it is primarily the halogens which interact with the TTR molecule and therefore must account for the strong affinity of binding. The interactions with the halogens are smaller in number in TTR,TBP and there is a decrease in affinity, even though the interaction with the hydroxyl group is stronger than that in the TTR,PBP complex. [source] Overexpression, purification and preliminary X-ray diffraction analysis of the controller protein C.Csp231I from Citrobacter sp.ACTA CRYSTALLOGRAPHICA SECTION F (ELECTRONIC), Issue 9 2009RFL23 Restriction,modification controller proteins play an essential role in regulating the temporal expression of restriction,modification genes. The controller protein C.Csp231I represents a new class of controller proteins. The gene was sublconed to allow overexpression in Escherichia coli. The protein was purified to homogeneity and crystallized using the hanging-drop vapour-diffusion method. The crystals diffracted to 2.0,Ĺ resolution and belonged to space group P21. An electrophoretic mobility-shift assay provided evidence of strong binding of C.Csp231I to a sequence located upstream of the csp231IC start codon. [source] Bone repair with a form of BMP-2 engineered for incorporation into fibrin cell ingrowth matrices,BIOTECHNOLOGY & BIOENGINEERING, Issue 3 2005Hugo G. Schmoekel Abstract Most growth factors naturally involved in development and regeneration demonstrate strong binding to the extracellular matrix and are retained there until being locally mobilized by cells. In spite of this feedback between cell activity and growth factor mobilization in the extracellular matrix, this approach has not been extensively explored in therapeutic situations. We present an engineered bone morphogenetic protein-2 (BMP-2) fusion protein that mimics such function in a surgically relevant matrix, fibrin, incorporated into the matrix until it is locally liberated by cell surface-associated proteases. A tripartite fusion protein, denoted TG-pl-BMP-2, was designed and produced recombinantly. An N-terminal transglutaminase substrate (TG) domain provides covalent attachment to fibrin during coagulation under the influence of the blood transglutaminase factor XIIIa. A central plasmin substrate (pl) domain provides a cleavage site for local release of the attached growth factor from the fibrin matrix under the influence of cell-activated plasmin. A C-terminal human BMP-2 domain provides osteogenic activity. TG-pl-BMP-2 in fibrin was evaluated in vivo in critical-size craniotomy defects in rats, where it induced 76% more defect healing with bone at 3 weeks with a dose of 1 ,g/defect than wildtype BMP-2 in fibrin. After a dosing study in rabbits, the engineered growth factor in fibrin was evaluated in a prospective clinical study for pancarpal fusion in dogs, where it induced statistically faster and more extensive bone bridging than equivalent treatment with cancellous bone autograft. The strong healing response shown by fibrin including a bound BMP-2 variant suggests that with the combination of bound growth factor and ingrowth matrix, it may be possible to improve upon the natural growth factor and even upon tissue autograft. © 2004 Wiley Periodicals, Inc. [source] Affinity Purification of Lipid VesiclesBIOTECHNOLOGY PROGRESS, Issue 1 2004Boris Peker We present a novel column chromatography technique for recovery and purification of lipid vesicles, which can be extended to other macromolecular assemblies. This technique is based on reversible binding of biotinylated lipids to monomeric avidin. Unlike the very strong binding of biotin and biotin-functionalized molecules to streptavidin, the interaction between biotin-functionalized molecules and monomeric avidin can be disrupted effectively by ligand competition from free biotin. In this work, biotin-functionalized lipids (biotin-PEG-PE) were incorporated into synthetic lipid vesicles (DOPC), resulting in unilamellar biotinylated lipid vesicles. The vesicles were bound to immobilized monomeric avidin, washed extensively with buffer, and eluted with a buffer supplemented with free biotin. Increasing the biotinyl lipid molar ratio beyond 0.53% of all lipids did not increase the efficiency of vesicle recovery. A simple adsorption model suggests 1.1 × 1013 active binding sites/mL of resin with an equilibrium binding constant of K = 1.0 × 108 M,1. We also show that this method is very robust and reproducible and can accommodate vesicles of varying sizes with diverse contents. This method can be scaled up to larger columns and/or high throughput analysis, such as a 96-well plate format. [source] Conformationally Constrained Mimics of the Membrane-Proximal Domain of Fc,RI,CHEMBIOCHEM, Issue 15 2007Carsten Peters Dr. Spitting image. The peptide fragment KAPREKYWL is part of the high-affinity IgE receptor and is critical in mast cell signaling. By applying ring-closing metathesis (RCM), conformationally constraint cyclic peptides were prepared that mimicked the 3D structure of KAPREKYWL. Peptide 1 (illustrated in the scheme) showed strong binding to a monoclonal anti-KAPREKYWL antibody; this was predicted by molecular modeling. [source] Aminoglycoside,Quinacridine Conjugates: Towards Recognition of the P6.1 Element of Telomerase RNACHEMBIOCHEM, Issue 2 2006Markus Kaiser Dr. Abstract A modular synthesis has been developed which allows easy and rapid attachment of one or two aminoglycoside units to a quinacridine intercalator, thereby leading to monomeric and dimeric conjugates. Melting temperature (Tm) experiments show that the tobramycin dimeric conjugate TD1 exhibits strong binding to the P6.1 element of human telomerase RNA. By contrast, tobramycin alone is much less efficient and the monomeric compound TM1 elicits a poor binding ability. Monitoring of the interaction by an electrophoretic mobility shift assay shows a 1:1 stoichiometry for the binding of the dimeric compound to the hairpin structure and confirms the lower affinity for a control duplex. Protection experiments with RNase T1 indicate interaction of the drug both in the stem and in the loop of the hairpin. Taken together, the data suggest a binding of TD1 inside the hairpin at the stem-loop junction. The same trends are observed with paromomycin and kanamycin analogues but with a lower affinity. [source] Synthesis, and DNA-Binding and DNA-Photocleavage Properties of Multiply Charged PorphyrinsCHEMISTRY & BIODIVERSITY, Issue 3 2007Kai Wang Abstract Four new cationic porphyrins, compounds 1,4, with five to seven positive charges, were synthesized, characterized, and investigated for their binding properties towards calf-thymus DNA (CT-DNA). UV/VIS and fluorescence-titration data indicated strong binding, the apparent binding constants (Kapp; (1.3,10)×10,6M) increasing with increasing number of charges, as determined by competitive fluorescence titration using ethidium bromide (EB) as molecular probe. These results were qualitatively confirmed by the observed photocleavage efficiency of the porphyrins towards plasmid pBR322 DNA. [source] | |||||||||||||||||||||||||