普拉迪米辛S的特性和碳水化合物特异性
Syed Shahzad-ul-Hussan1, Rodolfo Ghirlando, Cajetan I Dogo-Isonagie
1Laboratory of Bioorganic Chemistry, National Institute of Diabetes and Digestive and Kidney Diseases, National Institutes of Health, Bethesda, Maryland 20892, United States.
Journal of the American Chemical Society
|July 14, 2012
概括
普拉迪米辛S (PRM-S) 在的存在下形成一个四聚体,使其能够结合特定的曼诺糖. 这种寡合体形式对于通过与病毒相互作用来抑制HIV-1的进入至关重要.
科学领域:
- 碳水化合物化学 碳水化合物化学
- 结构生物学 结构生物学
- 药用化学 医学化学
背景情况:
- 普拉迪米辛抗生素家族表现出抗感染性质,并作为小分子碳水化合物识别的模型.
- 普拉迪米辛的依赖糖结合是独一无二的,但由于聚合而受到阻碍,无法进行详细的表征.
研究的目的:
- 为了表征 pradimicin S (PRM-S) 的生物相关形式和碳水化合物特异性.
- 为了研究PRM-S抑制HIV-1入口的机制.
主要方法:
- 使用NMR光谱和分析超离心法来确定PRM-S的结构和寡合化.
- 进行了功能性HIV-1入口试验,以评估抑制活性.
主要成果:
- 在生物相关度下结合后,PRM-S形成可溶性四相聚物.
- PRM-S四聚合物选择性地结合并吞特定的曼诺三糖化物.
- PRM-S表现出与寡合化相关的IC50值的抗HIV-1活性,并与HIV-1 gp120结合.
结论:
- 生物活性形式的PRM-S是一种诱导的四聚胺.
- 这项研究阐明了普拉迪米辛的碳水化合物结合机制及其作为碳水化合物受体的潜力.
- 这些发现提供了关于普拉迪米辛的抗感染性质及其与HIV-1的相互作用的见解.
相关概念视频
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Membrane carbohydrates do not have any hydrophobic region and are exclusively located on the cell's outer surface. The addition of sugar molecules or glycosylation of proteins happens in...
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Membrane carbohydrates do not have any hydrophobic region and are exclusively located on the cell's outer surface. The addition of sugar molecules or glycosylation of proteins happens in...
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Carbohydrates are polymers composed of molecules containing atoms of carbon, hydrogen and oxygen. One gram of carbohydrate can provide four kilo-calories of energy, which makes it the most efficient instant energy source.
Starch accounts for approximately 60% of the carbohydrates consumed by humans. Since amylase enzymes cannot function in the stomach's acidic environment, starch can only be digested in the mouth and small intestine. Simple sugars are found naturally in milk and fruits in the...
Starch accounts for approximately 60% of the carbohydrates consumed by humans. Since amylase enzymes cannot function in the stomach's acidic environment, starch can only be digested in the mouth and small intestine. Simple sugars are found naturally in milk and fruits in the...


