By focusing on general molecular mechanisms of antiviral drugs rather than therapies for individual viruses, this ready reference provides the critical knowledge needed to develop entirely novel therapeutics and to target new viruses.
It begins with a general discussion of antiviral strategies, followed by a broad survey of known viral targets, such as reverse transcriptases, proteases, neuraminidases, RNA polymerases, helicases and primases, as well as their known inhibitors. The final section contains several cases studies of recent successful antiviral drug development.
Edited by Erik de Clercq, the world authority on small molecule antiviral drugs, who has developed more new antivirals than anyone else.
Table of Contents
Outlook of the Antiviral Drug Era, now more than 50 Years after Description
of the First Antiviral Drug
Inhibition of HIV Entry
Targeting Integration Beyond Strand Transfer. Development of Second Generation HIV Integrase Inhibitors
From Saquinavir to Darunavir, the Impact of 10 Years of Medicinal Chemistry on a Lethal Disease
Acyclic and Cyclic Nucleoside Phosphonates
Helicase-Primase Inhibitors -
A New Approach to Combat Herpes Simplex Virus and Varicella-Zoster Virus
Alkoxyalkyl Ester Prodrugs of Antiviral Nucleoside Phosphates and Phosphonates
Maribavir: A Novel Benzimidazole Ribonucleoside for the Prevention and Treatment of Cytomegalovirus Diseases
Lethal Mutagenesis as an Unconventional Approach to Combat HIV
Recent Progess in the Development of HCV Protease Inhibitors
Antiviral RNAi, How to Silence Viruses
Neuraminidase Inhibitors as Anti-Influenza Agents
From TIBO to Rilpivirine: The Chronicle of the Discovery of the Ideal Non-Nucleoside Reverse Transcriptase Inhibitor (NNRTI)
Erik De Clercq, M.D., PhD is currently President of the Rega Foundation, a
member of the Belgian (Flemish) Royal Academy of Medicine and of the Academia
Europaea, and a Fellow of the American Association for the Advancement of Science.
He is an active Emeritus Professor of the Katholieke Universiteit Leuven (K.U.Leuven),
Belgium. He is honorary doctor of the Universities of Ghent, Belgium, Athens,
Greece, Ferrara, Italy, Jinan (Shandong), China, Charles (Prague), Czech Republic,
and Jihoceska (Bude?jovice), Czech Republic.
For his pioneering efforts in antiviral research, Professor De Clercq received in 1996 the Aventis award from the American Society for Microbiology, and in 2000 the Maisin Prize for Biomedical Sciences from the Belgian National Science Foundation. In 2008 he was elected Inventor of the Year by the European Union. Together with Dr. Anthony Fauci, Prof. De Clercq received the Dr. Paul Janssen Award for Biomedical Research in 2010.
He is the (co)inventor of a number of antiviral drugs, used for the treatment of HSV (valaciclovir, Valtrex , Zelitrex ), VZV (brivudin, Zostex , Brivirac , Zerpex ), CMV (cidofovir, Vistide ), HBV (adefovir dipivoxil, Hepsera ), and HIV infections (AIDS) (tenofovir disoproxil fumarate, Viread ).