Science 药物研发新文章--共价神经氨酸酶抑制剂

dejunchem

以机制为基础的具有广谱抗流感病毒活性的共价神经氨酸酶抑制剂
Mechanism-Based Covalent Neuraminidase Inhibitors with Broad-Spectrum Influenza Antiviral Activity

Abstract

Influenza antiviral agents play important roles in modulating disease severity and in controlling pandemics while vaccines are prepared, but the development of resistance to agents like the commonly used neuraminidase inhibitor oseltamivir may limit their future utility. We report here on a new class of specific, mechanism-based anti-influenza drugs that function through the formation of a stabilized covalent intermediate in the influenza neuraminidase enzyme, and we confirm this mode of action with structural and mechanistic studies. These compounds function in cell-based assays and in animal models, with efficacies comparable to that of the neuraminidase inhibitor zanamivir and with broad-spectrum activity against drug-resistant strains in vitro. The similarity of their structure to that of the natural substrate and their mechanism-based design make these attractive antiviral candidates

dejunchem

谢谢关注！

leos

支持～{:soso_e101:}{:soso_e101:}{:soso_e101:}{:soso_e101:}

dejunchem

leos 发表于 2013-4-10 19:21

                               
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支持～

感谢leos 兄的长期支持关注!~~

leos

主要是你推荐的文章真好～～，正好我最近没时间看文献，你的文章都是精选的了～～

dejunchem

leos 发表于 2013-4-11 22:23

                               
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主要是你推荐的文章真好～～，正好我最近没时间看文献，你的文章都是精选的了～～ ...

呵呵,我看到好文献还会持续给大家分享,谢谢~~

xufund

谢谢分享。很应景嘛