凝集素与超分子复合物之间的多价相互作用：半乳糖凝集素-1与自组装假聚轮烷
Multivalent interactions between lectins and supramolecular complexes: Galectin-1 and self-assembled pseudopolyrotaxanes.
作者信息
Belitsky Jason M, Nelson Alshakim, Hernandez Joseph D, Baum Linda G, Stoddart J Fraser
机构信息
California NanoSystems Institute, Department of Chemistry and Biochemistry, University of California, Los Angeles, Los Angeles, CA 90095, USA.
出版信息
Chem Biol. 2007 Oct;14(10):1140-51. doi: 10.1016/j.chembiol.2007.09.007.
Supramolecular chemistry has been employed to develop flexible and adaptable multivalent neoglycoconjugates for binding galectin-1 (Gal-1). Gal-1, a dimeric lectin with two galactoside-binding sites, regulates cancer progression and immune responses. Self-assembled pseudopolyrotaxanes consisting of lactoside-displaying cyclodextrin (LCD) "beads" threaded onto polyviologen "strings" display mobile ligands as a result of cyclodextrin rotation about, and limited translation along, the polymer chain. The pseudopolyrotaxanes rapidly and efficiently precipitate Gal-1 and provide valency-corrected enhancements of up to 30-fold compared to native lactose and 20-fold over free LCD in a T-cell agglutination assay. A supramolecular statistical effect was observed, wherein the efficacy of Gal-1 inhibition correlates with the number of ligands connected to each other solely through mechanical and noncovalent interactions. Such flexible and adaptable self-assembled pseudopolyrotaxanes show promise for the study of multivalent interactions and targeting of therapeutically relevant lectins.
超分子化学已被用于开发用于结合半乳糖凝集素-1（Gal-1）的灵活且适应性强的多价新糖缀合物。Gal-1是一种具有两个半乳糖苷结合位点的二聚体凝集素，可调节癌症进展和免疫反应。由展示乳糖苷的环糊精（LCD）“珠子”穿在聚紫精“线”上组成的自组装假聚轮烷，由于环糊精围绕聚合物链旋转并沿聚合物链进行有限的平移，从而展示出可移动的配体。在T细胞凝集试验中，假聚轮烷能快速有效地沉淀Gal-1，与天然乳糖相比，其价态校正增强倍数高达30倍，比游离LCD高出20倍。观察到一种超分子统计效应，其中Gal-1抑制的功效与仅通过机械和非共价相互作用相互连接的配体数量相关。这种灵活且适应性强的自组装假聚轮烷在多价相互作用研究和治疗相关凝集素的靶向方面显示出前景。
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