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丙型肝炎病毒NS3-4A絲氨酸蛋白酵素抑制藥物之發展

The Development of Inhibitors of the Hepatitis C Virus NS3-4A Serine Protease

摘要


在丙型肝炎病毒的感染周期中,NS3-4A絲氨酸蛋白酵素對病毒蛋白質的形成起著重要的作用。利用NS3-4A蛋白酵素可被它自身聚受質水解而產生小分子所抑制的特性,幾個模擬類藥物已先後被 開發出來,並已進入臨床試驗階段的研究。本文將對此類藥物的研發作描述。

並列摘要


In the life cycle of hepatitis C virus (HCV), NS3-4A serine protease plays an essential role in maturation of viral proteins. Thus, it represents a particularly important target for developing the anti-HCV drugs. In the efforts of inhibiting NS3-4A protease, it was found that some peptide products derived from sequences of the HCV NS3 protease substrates are competitive inhibitors. On the basis of this observation, several peptidomimetic drug candidates have been developed. The discovery processes of them are briefly summarized in this article.

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