Synthesis and Affinity Evaluation of a Small Library of Bidentate Cholera Toxin Ligands: Towards Nonhydrolyzable Ganglioside Mimics

Cheshev P; Morelli L; Marchesi M; Podlipnik C; Bergstrom M; Bernardi A

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Synthesis and Affinity Evaluation of a Small Library of Bidentate Cholera Toxin Ligands: Towards Nonhydrolyzable Ganglioside Mimics

机译：小型和双歧霍乱毒素配体库的合成和亲和力评估：面向不可水解的神经节苷脂模拟物。

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A small library of nonhydrolyzable mimics of GM1 ganglioside, featuring galactose and sialic acid its pharmacophoric carbohydrate residues,, was synthesized and tested. All compounds were synthesized from readily available precursors using high-performance reactions, including click chemistry protocols, and avoiding O-glycosidic bonds. Sonic of the most active molecules also feature a point of further derivatization that can be used for conjugation will, polyvalent aglycons. Their affinity towards cholera toxin was assessed by weak affinity chromatography, which allowed a systematic evaluation and selection of the best candidates. Affinity could be enhanced up to one or two orders of magnitude over the affinity of the individual pharmacophoric sugar residues.

机译：合成并测试了一个小型的GM1神经节苷脂不可水解模拟物文库，该文库以半乳糖和唾液酸为其药效学碳水化合物残基。所有化合物均使用高效反应（包括点击化学方案）和避免O-糖苷键的合成方法从易于获得的前体中合成。最具活性的分子的音速特征还在于可以用于缀合多价糖苷配基的进一步衍生化点。通过弱亲和色谱法评估了它们对霍乱毒素的亲和力，从而可以系统地评估和选择最佳候选物。与单个药效团糖残基的亲和力相比，亲和力可以提高一个或两个数量级。

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《Chemistry: A European journal》 |2010年第6期|共17页
作者
Cheshev P; Morelli L; Marchesi M; Podlipnik C; Bergstrom M; Bernardi A;
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正文语种 eng
中图分类应用化学;
关键词
carbohydrates; cholera toxin; combinatorial chemistry; glycosides; weak affinity chromatography;

机译：碳水化合物;霍乱毒素;组合化学;糖苷;弱亲和色谱;

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1. Synthesis and Affinity Evaluation of a Small Library of Bidentate Cholera Toxin Ligands: Towards Nonhydrolyzable Ganglioside Mimics [J] . Cheshev P, Morelli L, Marchesi M, Chemistry: A European journal . 2010,第6期

机译：小型和双歧霍乱毒素配体库的合成和亲和力评估：面向不可水解的神经节苷脂模拟物。
2. Ganglioside GM1 mimics: lipophilic substituents improve affinity for cholera toxin. [J] . Arosio D, Baretti S, Cattaldo S, Bioorganic and Medicinal Chemistry Letters . 2003,第21期

机译：神经节苷脂GM1模仿：亲脂性取代基提高了对霍乱毒素的亲和力。
3. Mimics of ganglioside GM1 as cholera toxin ligands: replacement of the GalNAc residue [J] . Anna Bernard, Daniela Arosio, Leonardo Manzoni, Organic & biomolecular chemistry . 2003,第5期

机译：神经节苷脂GM1作为霍乱毒素配体的模拟物：替换GalNAc残基
4. Dynamic Modeling of Binding Kinetics Between GD1b Ganglioside and Cholera Toxin Subunit B [C] . Dongheon Lee, Akshi Singla, Hung-Jen Wu, 2018 Annual American Control Conference . 2018

机译：GD1b神经节苷脂和霍乱毒素亚基B结合动力学的动力学模型
5. Development of ganglioside-based assays for the identification of botulinum and cholera toxins utilizing an evanescent wave biosensor. [D] . Bedenbaugh, Crystal M. 2006

机译：开发基于神经节苷脂的测定方法，用于利用van逝波生物传感器鉴定肉毒杆菌和霍乱毒素。
6. Cholera Toxin Inhibitors Studied with High-Performance Liquid Affinity Chromatography: A Robust Method to Evaluate Receptor–Ligand Interactions [O] . Maria Bergström, Shuang Liu, Kristi L. Kiick, -1

机译：高效液相亲和色谱法研究霍乱毒素抑制剂：一种评估受体-配体相互作用的稳健方法
7. Cholera Toxin Inhibitors Studied with High-Performance Liquid Affinity Chromatography: A Robust Method to Evaluate Receptor-Ligand Interactions [O] . Maria Bergström, Shuang Liu, Kristi L. Kiick, 2009

机译：霍乱毒素抑制剂用高效液相色谱层析研究：一种评价受体 - 配体相互作用的鲁棒方法
8. Evaluation of Purified Cholera Toxins and Toxoids as Immunizing Agents Against Cholera and Development of a New Technique for Measuring Cholera Toxin, Toxoid and Antitoxin [R] . Pierce, N. F., Carpenter, C. C. J., Greenough, W. B. 1970

机译：评估纯化的霍乱毒素和类毒素作为霍乱免疫剂及开发一种测定霍乱毒素，类毒素和抗毒素的新技术

Synthesis and Affinity Evaluation of a Small Library of Bidentate Cholera Toxin Ligands: Towards Nonhydrolyzable Ganglioside Mimics

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