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首页> 外文期刊>Journal of Cellular Physiology >Protease-mediated arsenic prodrug strategy in cancer and infectious diseases: a hypothesis for targeted activation.
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Protease-mediated arsenic prodrug strategy in cancer and infectious diseases: a hypothesis for targeted activation.

机译：Protease-mediated砷前体药物策略癌症和传染病:一个假设有针对性的激活。

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摘要

A strategy for the selective in vivo activation of prodrugs by proteases is presented. The approach is based on the design of polythiol peptides able to neutralize the toxicity of As(III) through chelation, and contemporarily to be recognized as substrates of a disease-linked specific protease. Enzyme digestion implies conversion of such polythiol peptides into monothiol fragments with irreversible loss of the ability to chelate the metalloid, thus triggering the release in its free and pharmacologically effective form. The proteases whose activity appears dramatically up-regulated in various pathologies, ranging from cancer to infectious diseases, can be conveniently employed as prodrug activators in the disease microenvironment. The design of the representative peptide shown here has been assisted by molecular modeling in order to fulfill the dual characteristic to be an efficient As(III) chelator and simultaneously a substrate of the matrix metalloproteinase-9 (MMP-9) whose activity results dramatically increased at the surface of cells affected by several pathologies.
机译：的选择性激活体内的策略高活性的蛋白酶。基于polythiol肽的设计可以吗压制的毒性(III)螯合,眼前是公认的基质的病有关的特定的蛋白酶。酶消化意味着这样的转换polythiol肽为monothiol片段不可逆损失的螯合能力金属,从而引发的释放自由和药物有效的形式。蛋白酶的活性急剧出现上调各种病态,从癌症对传染性疾病,可以方便地用作药物前体催化剂微环境。代表肽所示分子建模,以协助是一个实现双重特征有效的(3)螯合剂和同时metalloproteinase-9衬底的矩阵(MMP-9)的活动效果显著增加表面的细胞的影响一些病态。

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