优化糖导向的分子传递到生物受体:设计,合成和生物评价的糖二甲基-环二联合体
Juan M Benito1, Marta Gómez-García, Carmen Ortiz Mellet
1Contribution from the Instituto de Investigaciones Químicas, CSIC, Américo Vespucio 49, Isla de la Cartuja, E-41092 Seville, Spain.
Journal of the American Chemical Society
|August 19, 2004
概括
具有曼诺斯配体的新型树突性β-cyclopodextrin (betaCD) 衍生物对dcetaxel显示出高的药物溶解性. 微妙的结构变化显著影响受体亲和力和超分子组合,以增强莱克结合.
科学领域:
- 超分子化学 超分子化学
- 碳水化合物化学 碳水化合物化学
- 药物运输 药物运输 药物运输
背景情况:
- 树突性β-cyclopodextrin (betaCD) 衍生物正在被探索其有针对性的生物相互作用.
- 曼诺西尔连接体对于与特定的单蛋白和细胞表面受体结合至关重要.
研究的目的:
- 为了合成和评估betaCD-polymannoside支架的结合效率.
- 为了研究甘氨基基结构对莱克结合和分子包容性的影响.
- 评估这些结构作为药物载体的潜力,使用dcetaxel作为模型.
主要方法:
- 合成βCD衍生物使用异酸氨酸-氨基合用于thioureido链接.
- 准备具有不同联结体价值和几何形状的支架.
- 对康卡纳瓦林A (Con A) 和巨细胞受体的结合亲和度的评估.
- 评估dcetaxel的含量及其对生物识别的影响.
主要成果:
- 成功合成了一系列βCD-多曼诺酸基架.
- 证明了多塞塔克塞尔的高药物溶解能力.
- 观察到结合结构对受体亲和力的显著影响.
- 建立了宿主-客人相互作用,以创建具有增强莱克亲和力的动态葡萄糖集群.
结论:
- 树突性β-CD-多曼酸合物在药物溶解和向输送方面是有效的.
- 建筑修改提供了一种调整受体结合和超分子性能的手段.
- 这些构造显示出作为有效的治疗剂分子转运器的前景.
更多相关视频
相关概念视频
Oligosaccharide Assembly
Protein glycosylation starts in the ER lumen and continues in the Golgi apparatus. Glycosyltransferases catalyze the addition of sugar molecules or glycosylation of proteins. Usually, these enzymes add sugars to the hydroxyl groups of selected serine or threonine residues to form O-linked glycans or the amino groups of asparagine residues to form N-linked glycans. Different positions on the same polypeptide chain can contain differently linked glycans.
Multiple sugar molecules that may or may...
Multiple sugar molecules that may or may...
Sugars as Energy Storage Molecules
Sugar (a simple carbohydrate) metabolism (chemical reactions) is a classic example of the many cellular processes that use and produce energy. Living things consume sugar as a major energy source because sugar molecules have considerable energy stored within their bonds. Consumed carbohydrates have their origins in photosynthesizing organisms like plants. During photosynthesis, plants use the energy of sunlight to convert carbon dioxide gas into sugar molecules, like glucose. Because this...
Glucose Transporters
Glucose transporters facilitate the transport of glucose across the cell membrane. In addition to glucose, some glucose transporters can also aid the movement of other hexoses such as fructose, mannose, and galactose.
Facilitated diffusion-glucose transporters (GLUTs) are encoded by the solute-linked carrier (SLC) family 2, subfamily A gene family, or SLC2A. The 14 GLUT protein members are distributed into three classes:
Facilitated diffusion-glucose transporters (GLUTs) are encoded by the solute-linked carrier (SLC) family 2, subfamily A gene family, or SLC2A. The 14 GLUT protein members are distributed into three classes:
Sugars as Energy Storage Molecules
Sugar (a simple carbohydrate) metabolism (chemical reactions) is a classic example of the many cellular processes that use and produce energy. Living things consume sugar as a major energy source because sugar molecules have considerable energy stored within their bonds. Consumed carbohydrates have their origins in photosynthesizing organisms like plants. During photosynthesis, plants use the energy of sunlight to convert carbon dioxide gas into sugar molecules, like glucose. Because this...
Site-Targeted Drug Delivery Systems: Polymeric Carriers
Polymeric carriers enhance targeted drug delivery by increasing efficacy while minimizing off-target effects. These carriers comprise a biodegradable polymeric backbone integrated with functional elements that enable targeting, improve physicochemical properties, and regulate drug release.Targeting MechanismsThe targeting ability of polymeric carriers is mediated by a homing device, which is a molecular recognition component designed to selectively bind to specific tissues or cells. Monoclonal...
Biosynthesis of Polysaccharides
Polysaccharides such as glycogen and starch are synthesized from nucleoside diphosphate sugars, primarily uridine diphosphate glucose (UDPG) and adenosine diphosphate glucose (ADPG). These activated glucose donors act as key intermediates in carbohydrate metabolism and biosynthesis. UDPG primarily involves glycogen synthesis in animals and many bacteria, while ADPG plays a fundamental role in starch synthesis in plants and certain bacteria.UDPG is formed when glucose-1-phosphate reacts with...


