CAJ | 학술논문

丙型肝炎病毒(HCV)基因组的高度变异性使得HCV感染易呈慢性化,并极大地增加了肝硬化和肝癌的发病风险.效仿HIV蛋白酶抑制剂临床应用中取得的巨大成功,NS34A丝氨酸蛋白酶成为抗HCV感染小分子药物研发的重要靶点.此文围绕HCV NS3-4A蛋白酶抑制剂研发的最新进展、抗病毒活性、药代动力学特性、不良反应及抗药性突变进行了综述.
병형간염병독(HCV)기인조적고도변이성사득HCV감염역정만성화,병겁대지증가료간경화화간암적발병풍험.효방HIV단백매억제제림상응용중취득적거대성공,NS34A사안산단백매성위항HCV감염소분자약물연발적중요파점.차문위요HCV NS3-4A단백매억제제연발적최신진전、항병독활성、약대동역학특성、불량반응급항약성돌변진행료종술.
Hepatitis C virus (HCV) genome is of high variation,which results in persistent infection of HCV and increases the incidence of liver cirrhosis and hepatocellular carcinoma.Following the successful paradigm established for HIV protease inhibitors,HCV NS3-4A serine protease has been selected as the main target for the development of small molecule antiviral agents.In this article,we review recent progress in the discovery and development of HCV NS3-4A protease inhibitors,and discuss their antiviral activities,pharmacokinetic properties,side effects and resistance profiles.