核苷（酸）类抗病毒药物的发现：谨以此书献给埃里克·德·克勒克教授 80 华诞。
Drug Discovery of Nucleos(t)ide Antiviral Agents: Dedicated to Prof. Dr. Erik De Clercq on Occasion of His 80th Birthday.
机构信息
Department of Laboratory Medicine, The Second Xiangya Hospital, Central South University, Changsha 410011, China.
Hunan Provincial Key Laboratory of Clinical Epidemiology, Xiangya School of Public Health, Central South University, Changsha 410078, China.
出版信息
Molecules. 2021 Feb 9;26(4):923. doi: 10.3390/molecules26040923.
Nucleoside and nucleotide analogues are essential antivirals in the treatment of infectious diseases such as human immunodeficiency virus (HIV), hepatitis B virus (HBV), hepatitis C virus (HCV), herpes simplex virus (HSV), varicella-zoster virus (VZV), and human cytomegalovirus (HCMV). To celebrate the 80th birthday of Prof. Dr. Erik De Clercq on 28 March 2021, this review provides an overview of his contributions to eight approved nucleos(t)ide drugs: (i) three adenosine nucleotide analogues, namely tenofovir disoproxil fumarate (Viread) and tenofovir alafenamide (Vemlidy) against HIV and HBV infections and adefovir dipivoxil (Hepsera) against HBV infections; (ii) two thymidine nucleoside analogues, namely brivudine (Zostex) against HSV-1 and VZV infections and stavudine (Zerit) against HIV infections; (iii) two guanosine analogues, namely valacyclovir (Valtrex, Zelitrex) against HSV and VZV and rabacfosadine (Tanovea-CA1) for the treatment of lymphoma in dogs; and (iv) one cytidine nucleotide analogue, namely cidofovir (Vistide) for the treatment of HCMV retinitis in AIDS patients. Although adefovir dipivoxil, stavudine, and cidofovir are virtually discontinued for clinical use, tenofovir disoproxil fumarate and tenofovir alafenamide remain the most important antivirals against HIV and HBV infections worldwide. Overall, the broad-spectrum antiviral potential of nucleos(t)ide analogues supports their development to treat or prevent current and emerging infectious diseases worldwide.
核苷（酸）类似物是治疗人类免疫缺陷病毒（HIV）、乙型肝炎病毒（HBV）、丙型肝炎病毒（HCV）、单纯疱疹病毒（HSV）、水痘-带状疱疹病毒（VZV）和人巨细胞病毒（HCMV）等传染病的重要抗病毒药物。为庆祝 Erik De Clercq 教授 2021 年 3 月 28 日 80 岁生日，本文概述了他在以下 8 种已批准的核苷（酸）类药物方面的贡献：（i）三种腺苷核苷酸类似物，即替诺福韦二吡呋酯（Viread）和替诺福韦艾拉酚胺（Vemlidy），用于治疗 HIV 和 HBV 感染，阿德福韦酯（Hepsera）用于治疗 HBV 感染；（ii）两种胸苷核苷类似物，即溴夫定（Zostex），用于治疗 HSV-1 和 VZV 感染，司他夫定（Zerit）用于治疗 HIV 感染；（iii）两种鸟嘌呤类似物，即伐昔洛韦（Valtrex、Zelitrex），用于治疗 HSV 和 VZV 感染，以及拉布夫定（Tanovea-CA1），用于治疗犬的淋巴瘤；（iv）一种胞苷核苷酸类似物，即更昔洛韦（Vistide），用于治疗 AIDS 患者的 HCMV 视网膜炎。虽然阿德福韦酯、司他夫定和更昔洛韦几乎已不再用于临床，但替诺福韦二吡呋酯和替诺福韦艾拉酚胺仍是全球治疗 HIV 和 HBV 感染的最重要的抗病毒药物。总的来说，核苷（酸）类似物的广谱抗病毒潜力支持其开发，以治疗或预防全球当前和新出现的传染病。
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