- Design, synthesis, and characterization of fatty acid derivatives of a dimeric peptide-based postsynaptic density-95 (PSD-95) inhibitor
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Dimeric peptide-based inhibitors of postsynaptic density-95 (PSD-95) can reduce ischemic brain damage and inflammatory pain in rodents. To modify the pharmacokinetic profile, we designed a series of fatty acid linked dimeric ligands, which potently inhibits PSD-95 and shows improved in vitro blood plasma stability. Subcutaneous administration in rats showed extended stability and sustained release of these ligands. This can facilitate new pharmacological uses of PSD-95 inhibitors and further exploration of PSD-95 as a drug target.
- Nissen, Klaus B.,Andersen, Julie J.,Haugaard-Kedstr?m, Linda M.,Bach, Anders,Str?mgaard, Kristian
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Read Online
- COMPOUND COMPRISING A NUCLEIC ACID AND A HALF-LIFE EXTENSION MOTIF
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Disclosed herein are compounds including a nucleic acid (A), their preparation, and their use.
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Paragraph 0852
(2021/06/04)
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- Preparation method of surfactant
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The invention provides a preparation method of a surfactant, specifically comprising the following four steps: 1, preparing an intermediate 1 by using methyl oleate as a raw material; 2, letting the intermediate 1 firstly react with borane in a solvent, then oxidizing with hydrogen peroxide, and finally performing alkaline hydrolysis to obtain an intermediate 2; 3, jointly oxidizing the intermediate 2 into an intermediate 3 in a solvent by sodium hypochlorite, sodium perchlorate and TEMPO (2, 2, 6, 6-tetramethylpiperidine-1-oxy CAS number: 2564-83-2); and 4, hydrolyzing the intermediate 3 in asolvent under an alkaline condition, and acidifying to obtain the surfactant octadecanedioic acid. The preparation method is a synthetic method including four steps of chemical reactions, and can efficiently convert methyl oleate into octadecanedioic acid. The method is simple to operate; and the reagent is cheap and easily available, green and safe, efficient and environmentally-friendly, and suitable for industrial production.
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Paragraph 0026; 0029
(2020/05/14)
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- Direct interaction, instrumental for signaling processes, between LacCer and Lyn in the lipid rafts of neutrophil-like cells
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Lactosylceramide [LacCer; β-Gal-(1-4)-β-Glc-(1-1)-Cer] has been shown to contain very long fatty acids that specifically modulate neutrophil properties. The interactions between LacCer and proteins and their role in cell signaling processes were assessed
- Chiricozzi, Elena,Ciampa, Maria Grazia,Brasile, Giuseppina,Compostella, Federica,Prinetti, Alessandro,Nakayama, Hitoshi,Ekyalongo, Roudy C.,Iwabuchi, Kazuhisa,Sonnino, Sandro,Mauri, Laura
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p. 129 - 141
(2015/03/05)
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