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Review

Drug Discovery of Nucleos(t)ide Antiviral Agents: Dedicated to Prof. Dr. Erik De Clercq on Occasion of His 80th Birthday

by 1,2, 2, 2, 3, 3 and 1,*
1
Department of Laboratory Medicine, The Second Xiangya Hospital, Central South University, Changsha 410011, China
2
Hunan Provincial Key Laboratory of Clinical Epidemiology, Xiangya School of Public Health, Central South University, Changsha 410078, China
3
Laboratory of Medicinal Chemistry, Rega Institute for Medicinal Research, KU Leuven, 3000 Leuven, Belgium
*
Author to whom correspondence should be addressed.
Academic Editors: Libor Grubhoffer, Masanori Baba and Diego Muñoz-Torrero
Molecules 2021, 26(4), 923; https://doi.org/10.3390/molecules26040923
Received: 22 December 2020 / Revised: 20 January 2021 / Accepted: 5 February 2021 / Published: 9 February 2021
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. View Full-Text
Keywords: antiviral therapy; nucleoside analogue; nucleotide analogue; HIV; HBV; HCV; HSV; VZV; HCMV antiviral therapy; nucleoside analogue; nucleotide analogue; HIV; HBV; HCV; HSV; VZV; HCMV
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MDPI and ACS Style

Li, G.; Yue, T.; Zhang, P.; Gu, W.; Gao, L.-J.; Tan, L. Drug Discovery of Nucleos(t)ide Antiviral Agents: Dedicated to Prof. Dr. Erik De Clercq on Occasion of His 80th Birthday. Molecules 2021, 26, 923. https://doi.org/10.3390/molecules26040923

AMA Style

Li G, Yue T, Zhang P, Gu W, Gao L-J, Tan L. Drug Discovery of Nucleos(t)ide Antiviral Agents: Dedicated to Prof. Dr. Erik De Clercq on Occasion of His 80th Birthday. Molecules. 2021; 26(4):923. https://doi.org/10.3390/molecules26040923

Chicago/Turabian Style

Li, Guangdi, Tingting Yue, Pan Zhang, Weijie Gu, Ling-Jie Gao, and Li Tan. 2021. "Drug Discovery of Nucleos(t)ide Antiviral Agents: Dedicated to Prof. Dr. Erik De Clercq on Occasion of His 80th Birthday" Molecules 26, no. 4: 923. https://doi.org/10.3390/molecules26040923

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