- 1H Fast MAS NMR studies of hydrogen-bonding interactions in self-assembled monolayers
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The structures formed by the adsorption of carboxyalkylphosphonic acids on metal oxides were investigated by 1H fast magic angle spinning (MAS), heteronuclear correlation (HETCOR), and 1H double-quantum (DQ) MAS solid-state NMR experiments. The diacids HO2C(CH2)nPO3H2 (n = 2, 3, 11, and 15) were adsorbed on TiO2 and two types of ZrO2 powders having average particle sizes of 20, 30, and 5 nm, respectively. Carboxyalkylphosphonic acids bind selectively via the phosphonate group, forming monolayers with pendant carboxylic acid groups. Whereas dipolar coupled P-OH protons are detected on TiO2, there are only isolated residual P-OH groups on ZrO2, reflecting the relative binding strengths of phosphonic acids on these two substrates. From a comparative 1H MAS NMR study with an analogous monolayer system, HO2C(CH2)7SH coated gold nanoparticles, the hydrogen-bonding network at the monolayer/air interface is found to be quite disordered, at least for SAMs deposited on nonplanar substrates. Whereas only hydrogen-bonded homodimers occur in the bulk diacids, hydrogen bonding between the carboxylic and phosphonic acid groups is present in multilayers of the diacids on the ZrO2 nanopowder.
- Pawsey, Shane,McCormick, Mark,De Paul, Susan,Graf, Robert,Lee,Reven, Linda,Spiess, Hans W.
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- Photoionization studies of chromophore-labeled amino acids and peptides
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The photoionization characteristics of a naphthol chromophore covalently tethered to a few different amino acids and small peptides are investigated. To isolate the chromophore from the biological molecules the linkage between them is constructed from saturated alkyl chains of up to 12 carbons in length. Experimental results are compared with those of previous studies that explored the photoionization of macromolecules.
- Houston, Christopher T.,Reilly, James P.
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- Amantadine hapten and preparing method and application thereof
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The invention relates to the field of preparation of haptens, in particular to an amantadine hapten and a preparing method and application thereof. When the amantadine hapten is prepared, amantadine and bromine polyhydroxyalkanoate serve as raw materials, and through a nucleophilic substitution reaction, amidogen groups in amantadine molecules are connected with the bromine polyhydroxyalkanoate; then through a hydrolysis reaction, carboxyl groups are introduced to obtain a corresponding product. The amantadine hapten can be coupled with a carrier protein to prepare an artificial antigen, the artificial antigen is prepared into a monoclonal antibody or a polyclonal antibody through an immune animal, and then the monoclonal antibody or the polyclonal antibody can be used for quickly detecting residues of the amantadine in an animal product.
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Paragraph 0074; 0078; 0082
(2019/10/01)
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- NOVEL GLYCINE TRANSPORT INHIBITORS FOR THE TREATMENT OF PAIN
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The present invention relates to novel glycine transport inhibitor compounds and their use for treating pain.
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Page/Page column 48
(2018/08/12)
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- Synthesis and Characterization of Novel Acyl-Glycine Inhibitors of GlyT2
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It has been demonstrated previously that the endogenous compound N-arachidonyl-glycine inhibits the glycine transporter GlyT2, stimulates glycinergic neurotransmission, and provides analgesia in animal models of neuropathic and inflammatory pain. However, it is a relatively weak inhibitor with an IC50 of 9 μM and is subject to oxidation via cyclooxygenase, limiting its therapeutic value. In this paper we describe the synthesis and testing of a novel series of monounsaturated C18 and C16 acyl-glycine molecules as inhibitors of the glycine transporter GlyT2. We demonstrate that they are up to 28 fold more potent that N-arachidonyl-glycine with no activity at the closely related GlyT1 transporter at concentrations up to 30 μM. This novel class of compounds show considerable promise as a first generation of GlyT2 transport inhibitors.
- Mostyn, Shannon N.,Carland, Jane E.,Shimmon, Susan,Ryan, Renae M.,Rawling, Tristan,Vandenberg, Robert J.
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p. 1949 - 1959
(2017/09/26)
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- OMEGA-3 ANALOGUES
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The present invention relates to new omega-3 fatty acid analogues and to their use in cancer therapy, including anti-metastatic therapy.
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Page/Page column 14; 34
(2015/12/11)
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- Functionalised nanoparticles, their production and use
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Stable complexes are described, formed by mono- and di-functional compounds bound to nanoparticles composed of various types of transition metal oxides and of metals useful in the production processes of different types of new materials (such as for examp
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- Antiproliferative and antimigratory actions of synthetic long chain n-3 monounsaturated fatty acids in breast cancer cells that overexpress cyclooxygenase-2
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Cyclooxygenase-2 (COX-2) is overexpressed in many human cancers and converts the n-6 polyunsaturated fatty acid (PUFA) arachidonic acid to prostaglandin E2 (PGE2), which drives tumorigenesis; in contrast, n-3 PUFA inhibit tumorigenesis. We tested the hypothesis that these antitumor actions of n-3 PUFA may involve the n-3 olefinic bond. n-3 Monounsaturated fatty acids (MUFAs) of chain length C16-C22 were synthesized and evaluated in MDA-MB-468 breast cancer cells that stably overexpressed COX-2 (MDA-COX-2 cells). Longer chain (C19-C22) n-3 MUFAs inhibited proliferation, activated apoptosis, decreased PGE2 formation, and decreased cell invasion; C16-C18 analogues were less active. Molecular modeling showed that interactions of Arg120, Tyr355, and several hydrophobic amino acid residues in the COX-2 active site with C19-C22 MUFA analogues were favored. Thus, longer-chain n-3 MUFAs may be prototypes of novel anticancer agents that decrease the formation of PGE2 in tumor cells that contain high levels of COX-2.
- Cui, Pei H.,Kirsi Bourget, Tristan Rawing,Kim, Terry,Duke, Colin C.,Doddareddy, Munikumar R.,Hibbs, David E.,Zhou, Fanfan,Tattam, Bruce N.,Petrovic, Nenad,Murray, Michael
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p. 7163 - 7172
(2012/11/07)
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- FUNCTIONALISED NANOPARTICLES, THEIR PRODUCTION AND USE
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Stable complexes are described, formed by mono- and di-functional compounds bound to nanoparticles composed of various types of transition metal oxides and of metals useful in the production processes of different types of new materials (such as for examp
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