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INHIBITOR OF VASCULAR ENDOTHELIAL CELL GROWTH FACTOR AND INHIBITOR OF NEOVASCULARIZATION
INHIBITOR OF VASCULAR ENDOTHELIAL CELL GROWTH FACTOR AND INHIBITOR OF NEOVASCULARIZATION
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机译:血管内皮细胞生长因子的抑制剂和新生血管形成的抑制剂
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摘要
PROBLEM TO BE SOLVED: To obtain the subject inhibitor capable of exhibiting antagonistic activities or the like against the bond of a vascular endothelial cell growth factor(VEGF) to heparan sulfate or heparin present in the vascular endothelial cell by including a sulfated glucosaminopglycan containing a large amount of N-sulfate group and 6-sulfate group.;SOLUTION: This inhibitor contains a sulfated glycosaminoglycan having repeating structure of a disaccharide unit composed of glucosamine and hexuronic acid, as a base skeleton, and its salt. The sulfated glycosaminoglycan and the salt have a composition containing ≥40 mol% ΔDiHS-di(6,N)S of the formula (R1 and R2 are each SO3-; R3 is H) measured by a disaccharide composition analysis combining the degradation by a glycosaminoglycan-splitting enzyme with a high-pressure liquid chromatography, and the salt thereof. The daily dose of the sulfated glycosaminoglycan is exemplified by 100 μg/kg to 100 mg/kg as a clinical dose.;COPYRIGHT: (C)2000,JPO
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机译:解决的问题:通过包含含有大分子的硫酸化的葡糖胺聚糖,获得能够表现出对血管内皮细胞生长因子(VEGF)与存在于血管内皮细胞中的硫酸乙酰肝素或肝素的键合具有拮抗活性等的本发明的抑制剂。解决方案:该抑制剂含有硫酸葡糖胺聚糖和其盐,该硫酸葡糖氨基聚糖具有由葡糖胺和己糖醛酸组成的二糖单元的重复结构。硫酸化的糖胺聚糖和其盐的组成为:通过结合二糖的二糖组成分析测得的式(R1和R2分别为SO3-; R3为H)的式(R1和R2均为SO3-; R3为H)。高压液相色谱法通过糖胺聚糖分解酶进行的降解及其盐。硫酸化糖胺聚糖的日剂量以临床剂量为例,为100μg/ kg至100mg / kg 。;版权:(C)2000,JPO
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