Polyvalency: A promising strategy for drug design
Polyvalency: A promising strategy for drug design
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DOI：
10.1002/bit.22056
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发表时间：
2008-10-15
影响因子：
3.8
通讯作者：
Kane, Ravi S.
中科院分区：
文献类型：
--
作者：
Vance, David;Shah, Mrinal;Kane, Ravi S.
一个实体上的多个配体与另一实体上的多个受体的同时结合可导致显著大于单个配体与单个受体的结合的亲和力。这种“多价”的概念可用于设计毒素和病原体的有效抑制剂分子。我们描述了设计有效的多价抑制剂，中和炭疽毒素在体内，以及我们试图阐明抑制剂的结构和活性之间的关系。我们还强调了多价药物设计研究的前景。
The simultaneous binding of multiple ligands on one entity to multiple receptors on another can result in an affinity that is significantly greater than that for the binding of a single ligand to a single receptor. This concept of "polyvalency" can be used to design molecules that are potent inhibitors of toxins and pathogens. We describe the design of potent polyvalent inhibitors that neutralize anthrax toxin in vivo as well as our attempts to elucidate the relationship between inhibitor structure and activity. We also highlight promising future avenues for research in polyvalent drug design.