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首页> 外文期刊>Artificial cells, nanomedicine, and biotechnology. >Prioritization and characterization of validated biofilm blockers targeting glucosyltransferase C of Streptococcus mutans
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Prioritization and characterization of validated biofilm blockers targeting glucosyltransferase C of Streptococcus mutans

机译：验证的生物膜阻滞剂的优先级和表征靶向链球菌葡萄糖转移酶C的葡萄糖转移酶C.

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摘要

To date, several Glucosyltransferase C (GtfC) inhibitors have been identified and experimentally validated. All these inhibitors have been validated at different experimental conditions like degree of purity, animal models, kinetic conditions, experimental environment etc.; and most of these inhibitors (ligands) proved to be quite effective in their respective validation environment. However, due to varied experimental validation conditions, and absence of molecular interaction data, there is no way to prioritize these validated ligands for their inhibition potential against GtfC. The present study is a novel attempt of comparative evaluation of the interaction of the validated ligands on a single platform and under similar conditions with a dual objective, i.e. ligand prioritization for their respective inhibitory potential and elucidation of the involved unknown molecular interactions. Carbohydrate derivatives (6-Deoxy sucrose and Trichloro-galactosucrose) were identified as the most promising GtfC inhibitors. In addition, Asp588, Trp517, and Asn481 amino acid residues of the domain A1 proved vital for the inhibitory effect. The study highlights the importance of the comparative analysis of the validated ligands in order to identify the most promising leads for drug discovery against dental caries.
机译：迄今为止，已经确定了几种葡糖糖基转移酶C（GTFC）抑制剂并通过实验验证。所有这些抑制剂已在不同的实验条件下验证，如纯度，动物模型，动力学条件，实验环境等。并且大多数这些抑制剂（配体）在各自的验证环境中证明是非常有效的。然而，由于不同的实验验证条件，并且没有分子相互作用数据，没有办法优先考虑这些验证的配体的抑制潜力对GTFC。本研究是对单个平台上的验证配体相互作用的比较评价的新的尝试，并且在具有双目标的类似条件下，即它们各自的抑制潜力和涉及未知分子相互作用的配体优先级。碳水化合物衍生物（6-脱氧蔗糖和三氯半乳糖）被鉴定为最有前途的GTFC抑制剂。另外，ASP588，TRP517和ASN481域A1的氨基酸残基对抑制作用证明了至关重要。该研究突出了验证配体对比较分析的重要性，以确定对龋齿的药物发现最有前途的引线。

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