- Directing Neuronal Signaling through Cell-Surface Glycan Engineering
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The ability to tailor plasma membranes with specific glycans may enable the control of signaling events that are critical for proper development and function. We report a method to modify cell surfaces with specific sulfated chondroitin sulfate (CS) glycosaminoglycans using chemically modified liposomes. Neurons engineered to display CS-E-enriched polysaccharides exhibited increased activation of neurotrophin-mediated signaling pathways and enhanced axonal growth. This approach provides a facile, general route to tailor cell membranes with biologically active glycans and demonstrates the potential to direct important cellular events through cell-surface glycan engineering.
- Pulsipher, Abigail,Griffin, Matthew E.,Stone, Shannon E.,Brown, Joshua M.,Hsieh-Wilson, Linda C.
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Read Online
- Synthesis and Preclinical Evaluation of [18F]SiFA-PSMA Inhibitors in a Prostate Cancer Model
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Positron emission tomography (PET) imaging of prostate-specific membrane antigen (PSMA) with gallium-68 (68Ga) and fluorine-18 (18F) radiotracers has aroused tremendous interest over the past few years. The use of organosilicon-[18F]fluoride acceptors (Si
- Bailey, Justin J.,Bhardwaj, Atul,Schirrmacher, Ralf,Valliant, John F.,W?ngler, Bjoern,W?ngler, Carmen,Wagner, Michael,Wuest, Frank,Wuest, Melinda
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p. 15671 - 15689
(2021/11/13)
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- OXAMAZIN ANTIBIOTICS
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Disclosed herein are oxamazin monobactam compounds and their use as antibiotics resistant to degradation by β-lactamases. Also disclosed are pharmaceutical compositions containing the compounds and methods of synthesis.
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Paragraph 0191; 0192
(2014/09/29)
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- OXAMAZIN ANTIBIOTICS
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Disclosed herein are oxamazin monobactam compounds and their use as antibiotics resistant to degradation by β-lactamases. Also disclosed are pharmaceutical compositions containing the compounds and methods of synthesis.
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Paragraph 00162; 00163
(2014/10/18)
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- CROSSLINKING REAGENTS, METHODS, AND COMPOSITIONS FOR STUDYING PROTEIN-PROTEIN INTERACTIONS
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The invention provides reagents, methods, and compositions for studying protein-protein interactions. The inventive system and methods allow the analysis of protein-protein interactions in vivo and in vitro. Advantages offered by various embodiments of th
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Page/Page column 15
(2013/02/27)
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- A novel heterotrifunctional peptide-based cross-linking reagent for facile access to bioconjugates. Applications to peptide fluorescent labelling and immobilisation
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A convenient, versatile and straightforward synthesis of a novel heterotrifunctional peptide-based linker molecule is described. This generic bio-labelling reagent contains an amine-reactive N-hydroxysuccinimidyl carbamate moiety, an aldehyde/ketone-reactive aminooxy group and a thiol group with a propensity to form urea, oxime and thioether linkages respectively. The full chemical orthogonality between the free aminooxy and thiol functionalities was demonstrated through the preparation of a fluorescent reagent suitable for the selective staining of a carboxaldehyde-modified surface by means of oxime ligation. The absence of reactivity of these two functions toward the nucleophile-sensitive active carbamate was obtained by using temporary aminooxy- and thiol-protecting groups removable under mild conditions. The utility of the linker molecule to cross-link three different molecular partners has been illustrated by the preparation of fluorescent tripod-functionalised surfaces which may be useful in developing new peptide microarrays and related immunosensors.
- Clavé, Guillaume,Boutal, Hervé,Hoang, Antoine,Perraut, Fran?ois,Volland, Hervé,Renard, Pierre-Yves,Romieu, Anthony
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supporting information; experimental part
p. 3065 - 3078
(2009/02/03)
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- A novel series of parenteral cephalosporins exhibiting potent activities against Pseudomonas aeruginosa and other Gram-negative pathogens: Synthesis and structure-activity relationships
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A series of 7β-[2-(2-aminothiazol-4-yl)-2-(Z)-(carboxymethoxyimino)acetamido]cephalosporins bearing a 1-(substituted)-1H-pyrrolo[3,2-b]pyridinium group at C-3′ position was synthesized and their in vitro antibacterial activities against Pseudomonas aeruginosa and other Gram-negative pathogens were evaluated. Among the cephalosporins prepared, 7β-[2-(2-amino-5-chlorothiazol-4yl)-2(Z)-((S)-1-carboxyethoxyimino)acetamido]cephalosporins (42d) showed potent antibacterial activities against P. aeruginosa and other Gram-negative pathogens including the strains which produce class C β-lactamase and extended spectrum β-lactamase (ESBL). These results imply that both the Cl atom on the C-7 aminothiazole moiety and the α-substituent at the iminoether moiety are essential for the stability against β-lactamase and the potent activity against Gram-negative bacteria including P. aeruginosa.
- Yamawaki, Kenji,Nomura, Takashi,Yasukata, Tatsuro,Uotani, Koichi,Miwa, Hideaki,Takeda, Kei,Nishitani, Yasuhiro
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p. 6716 - 6732
(2008/03/28)
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- COMPOSITIONS CAPABLE OF INHIBITING REACTIVE OXYGEN AND CARBONYL SPECIES
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Therapeutic compositions are provided. The compositions include a single molecule that can display both antioxidant and carbonyl trapping properties. This can effectively reduce inflammation, oxidative stress and carbonyl stress, such as to prevent and/or treat cardiovascular disease and inflammatory diseases in kidney disease patients.
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Page/Page column 11; 16; 6/19
(2010/10/20)
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- Nitrosated nonsteroidal antiinflammatory compounds, compositions and methods of use related applications
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The invention describes novel nitrosated nonsteroidal antiinflammatory drugs (NSAIDs) and pharmaceutically acceptable salts thereof, and novel compositions comprising at least one nitrosated NSAID, and, optionally, at least one compound that donates, transfers or releases nitric oxide, stimulates endogenous synthesis of nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor or is a substrate for nitric oxide synthase, and/or at least one therapeutic agent. The invention also provides novel compositions comprising at least one nitrosated NSAID, and at least one compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or at least one therapeutic agent. The invention also provides novel kits comprising at least one nitrosated NSAID, and, optionally, at least one nitric oxide donor and/or at least one therapeutic agent. The invention also provides methods for treating inflammation, pain and fever; for treating gastrointestinal disorders; for facilitating wound healing; for treating and/or preventing gastrointestinal, renal and/or respiratory toxicities resulting from the use of nonsteroidal antiinflammatory compounds; for treating inflammatory disease states and/or disorders; and for treating and/or preventing ophthalmic diseases and/or disorders.
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Page/Page column 41
(2010/11/30)
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- BROAD-SPECTRUM CEPHEM COMPOUNDS
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A compound of the formula: (wherein, T is S, SO or O : X is halogen, CN, carbamoyl optionally substituted with lower alkyl, lower alkyl, lower alkoxy, or lower alkylthio ; A is substituted lower alkylene (wherein the substituent is optionally substituted mono lower alkyl, optionally substituted lower alkylidene, or optionally substituted lower alkylene) ; Z+ is an optionally substituted, a cation and an N atom-containing heterocyclic group), ester, amino-protected compound wherein the amino bonds to a thiazole ring at the 7-position, or pharmaceutically acceptable salt or solvate thereof.
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- Beta-amino acid derivatives useful for the treatment of bacterial infections
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The invention provides compounds that are useful for the treatment of bacterial infections in mammals. More specifically, it is directed to beta-amino acid derivatives or pharmaceutically acceptable salts, prodrugs, or isomers of those compounds that are
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- N- and C-terminal modifications of negamycin
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Negamycin 1 is a bactericidal antibiotic with activity against Gram-negative bacteria, and served as a template in an antibiotic discovery program. An orthogonally protected β-amino acid derivative 3a was synthesized and used in parallel synthesis of negamycin derivatives on solid support. This advanced intermediate was also used for N- and C-terminal modifications using solution-phase methodologies. The N-terminal modifications have resulted in the identification of active analogues, whereas the C-terminal modifications resulted in complete loss of antibacterial activity. The N-methyl negamycin analogue, 19a, inhibits protein synthesis (IC50=2.3 μM), has antibacterial activity (Escherichia coli, MIC=16 μg/mL), and is efficacious in an E. coli murine septicemia model (ED50=16.3 mg/kg).
- Raju,Mortell, Kathleen,Anandan, Sampathkumar,O'Dowd, Hardwin,Gao, Hongwu,Gomez, Marcela,Hackbarth, Corinne,Wu, Charlotte,Wang, Wen,Yuan, Zhengyu,White, Richard,Trias, Joaquim,Patel, Dinesh V.
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p. 2413 - 2418
(2007/10/03)
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- 1-carboxymethoxy acetidinones and their production
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A 2-azetidinone derivative having a group of the formula STR1 wherein R1 and R2 are the same or different and each represents a hydrogen atom, alkyl, aryl or arylalkyl which may have a substituent at the 1-position and an amino group, at the 3-position, which may be acylated or protected, its salt or ester, and methods of producing the same, (1) a method comprising subjecting a 2-azetidinone derivative having a group of the formula STR2 wherein the symbols are as defined above at the 1-position and an amino group at the 3-position, its salt or ester to an acylation or protective-group introduction reaction, and (2) a method comprising reacting a 2-azetidinone derivative having a hydroxy group at the 1-position and an amino group, at the 3-position, which may be acylated or protected, or its salt with a compound of the formula STR3 wherein W is a halogen atom; other symbols are as defined above, its salt or ester. The above objective compounds are utilizable as excellent antimicrobial agents or as valuable intermediates for the synthesis of the same.
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- Oxyimino-substituted cyclopropanecarboxylate pesticides
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New cyclopropane compounds have the formula STR1 wherein X is chlorine, bromine or OR in which R is hydrogen, a salt-forming cation, an alkyl group or residues of certain other alcohols; and W is thienyl, furfuryl, --CO2 R1, --CONRs
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