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多价超分子树状大分子为基础的药物。

Multivalent supramolecular dendrimer-based drugs.

机构信息

Dipartimento Farmaco Chimico Tecnologico and European Research Centre for Drug Discovery and Development, Universitàà di Siena, Via A. Moro, 53100 Siena, Italy.

出版信息

Biomacromolecules. 2010 Jan 11;11(1):182-6. doi: 10.1021/bm901055a.

Abstract

Supramolecular complexes consisting of a hydrophobic dendrimer host [DAB-dendr-(NHCONH-Ad)(64)] as well as solubilizing and bioactive guest molecules have been synthesized using a noncovalent approach. The guest-host supramolecular assembly is first preassembled in chloroform and transferred via the neat phase to aqueous solution. The bioactive guest molecules can bind to a natural (serotonin 5-HT(3)) receptor with nanomolar affinity as well as to the synthetic dendrimer receptor in aqueous solution, going toward a dynamic multivalent supramolecular construct capable of adapting itself to a multimeric receptor motif.

摘要

使用非共价方法合成了由疏水性树状大分子主体[DAB-dendr-(NHCONH-Ad)(64)]以及增溶和生物活性客体分子组成的超分子配合物。首先在氯仿中将客体-主体超分子组装体预组装,并通过纯相转移到水溶液中。生物活性客体分子可以与天然(5-羟色胺 5-HT(3))受体以纳摩尔亲和力结合,也可以与水溶液中的合成树状大分子受体结合,形成一种能够适应多聚体受体基序的动态多价超分子结构。

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