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参考文献:一种糖基联合细胞穿透肽修饰的脑靶向纳米脂质体的制备方法与应用
标题:一种糖基联合细胞穿透肽修饰的脑靶向纳米脂质体的制备方法与应用
摘要:本发明涉及一种糖基联合细胞穿透肽修饰的脑靶向纳米脂质体及其制备方法与应用,属于靶向给药技术领域.为解决糖基修饰的脂质体穿透细胞膜能力弱而使药物聚积在细胞外,难以发挥药效的问题,本发明提供了一种糖基联合细胞穿透肽修饰的脑靶向纳米脂质体,该脂质体包含一定摩尔比的epc,Cho,糖基修饰聚乙二醇化磷脂和细胞穿透肽修饰聚乙二醇化磷脂.通过在纳米脂质体表面同时修饰糖基和细胞穿透肽,使其兼具主动靶向于脑部和穿透细胞膜的能力.将其用于药物载体,可使所携带的药物高效的特异性靶向脑组织并进入脑细胞发挥作用.经体外细胞试验和体内分布实验均证明本发明提供的脑靶向纳米脂质体可以顺利到达脑部并蓄积在脑细胞中发挥药效.

专利信息

专利号:WO-9518232-A1
优先权日:1993-12-24
标题 :Enzymatic method for synthesis of o-glycosylated amino acid or peptide or derivatives thereof
发明人：NILSSON KURT
权利人:NILSSON KURT
摘要:Present invention describes a method for synthesis of O-glycosylated amino acid or peptide or derivatives thereof, characterized by the use of a glycosyl donor which is a monosaccharide in pyranose or furanose form or which is an oligosaccharide, and by the use of an acceptor which is a hydroxyl group containing amino acid or peptide derivative which has been modified in its N-terminal α-amino group and in which the C-terminal carboxyl group is non-modified, employing an exo- or an endoglycosidase (EC 3.2) as catalyst in an equilibrium reaction and that the product is isolated from the reaction mixture or is used directly or after partial or complete isolation in a continued synthesis with chemical methods or with enzymatic methods.

专利号:US-5262312-A
优先权日:1990-04-25
标 题:Process for the glycosidase-catalyzed synthesis of glyco conjugates
发明人：HOLLA WOLFGANG; SCHUDOK MANFRED
权利人:HOECHST AG
摘要:It has been possible to show for a first time with the process according to the invention that the synthesis of glyco conjugates is possible by direct linkage of sugars with serine, serine derivatives and serine peptides with the aid of glucosidases.

专利号:EP-0725144-A1
优先权日:1995-02-06
标题 :Process for the preparation of glycosides using glycosidases from ciliates
发明人：KIY THOMAS DR; HOERSCH BRIGITTE DR; MARQUARDT RUEDIGER DR
权利人:HOECHST AG
摘要:The invention relates to a process for the production of glycosides by enzymatic glycosylation by means of α- and β-glycosidases from holotrich ciliates and in particular from Hymenostomatida.n n n Glycosidases from holotrich ciliates are very well suited for the enzymatic synthesis of alkyl glycosides, glycopeptides, di- or oligosaccharides. Preferred glycosyldoren are nitrophenylglycosides, glycosyl fluorides or disaccharides, preferred acceptors are short-chain alcohols, polyhydroxy compounds, in particular monosaccharides, or protected hydroxyamino acids or corresponding peptides.

专利号:US-4918009-A
优先权日:1985-12-11
标 题:Method of controlling the regioselectivity of glycosidic bonds
发明人：NILSSON KURT G I
权利人:SVENSKA SOCKERFABRIKS AB
摘要:A method of controlling the regioselectivity of the glycosidic bond between glycosyl donor and glycosyl acceptor in the enzymatic production of an oligosaccharide compound which either consists of or is a fragment or an analog of the cabohydrate part in a glycoconjugate, by reverse hydrolysis or transglycosidation reactions, is described. The synthesis is carried out in that a donor substance which is a mono- or oligosaccharide or a glycoside thereof, is caused to react, in the presence of a glycosidase, with an acceptor substance which is an O-, N-, C- or S-glycoside consisting of a monosaccharide, oligosaccharide or a saccharide analog and at least one aglycon which is O-, N-, C- or S-glycosidically bonded in 1-position, the alpha or beta -configuration being selected on the glycoside bond between the glycosyl group and the aglycon in the acceptor substance, and the oligosaccharide compound being separated from the reaction mixture.

专利号:EP-0736101-A1
优先权日:1993-12-24
标 题:Enzymatic method for synthesis of o-glycosylated amino acid or peptide or derivatives thereof