Antiviral drug strategies. (2011)

• Record Type: Book
• Further Information: Note: Edited by Erik De Clercq.
• Other Names: De Clercq, Erik
• Contents: Preface; OUTLOOK OF THE ANTIVIRAL DRUG ERA, NOW MORE THAN 50 YEARS AFTER DESCRIPTION OF THE FIRST ANTIVIRAL DRUG; Introduction: The Prehistory; Key Events in Antiviral Drug Development; Antiviral Drugs: Current State of the Art; Antiviral Drugs Active against Herpesviruses (i.e., HSV, VZV, and so on); Antiviral Drugs Active against Retroviruses (HIV); Antiviral Drugs Active against Hepatitis B Virus; Antiviral Drugs Active against DNA Viruses at Large; Antiviral Drugs for Influenza A Virus Infections; Antiviral Drugs for Hepatitis C Virus; Antiviral Drugs for Poxviruses (i.e., Variola, Vaccinia, and so on); Further Options to Treat Virus Infections; Conclusions; INHIBITION OF HIV ENTRY; Introduction; The HIV Glycoproteins; Mechanism of HIV Entry; Inhibition of HIV Entry; Concluding Remarks; TARGETING INTEGRATION BEYOND ATRAND TRANSFER: DEVELOPMENT OF SECOND-GENERATION HIV INTEGRASE INHIBITORS; HIV: The Causative Agent of AIDS; The Integration Step: A Complex Mechanism with Different Possibilities for Inhibition; DNA Binding Inhibitors; Multimerization Inhibitors; Targeting Integrase Cofactor Interactions; Conclusion; FROM SAQUINAVIR TO DARUNAVIR: THE IMPACT OF 10 YEARS OF MEDICINAL CHEMISTRY ON A LETHAL DISEASE; Introduction; The HIV Protease as a Target for AIDS; The Early Protease Inhibitors; The Medical Need for a "Next"-Generation PI; How Can We Explain the Superior Antiviral Activity of Darunavir?; Clinical Development of Darunavir; Conclusions and Future Developments; ACYCLIC AND CYCLIC NUCLEOSIDE PHOSPHONATES; Introduction; Nucleoside Phosphonate Strategy for Antivirals; Acyclic Nucleoside Phosphonates; Cyclic Nucleoside Phosphonates; Prodrugs of Nucleoside Phosphonates; Clinical Applications of Antiviral Nucleoside Phosphonates; Conclusions; HELICASE-PRIMASE INHIBITORS: A NEW APPROACH TO COMBAT HERPES SIMPLEX VIRUS AND VARICELLA ZOSTER VIRUS; Introduction; The Role of Helicase Primase in the Replication of HSV; Selective Inhibitors of Helicase Primase as Antiherpesvirus Antivirals; HPIs are Effective in Cell Culture in In Vivo; Effects of HPIs on the Establishment and Reactivation from Latency; HPIs: The Biochemical Basis for the Proposed Mechanism of Action; HSV Acquired Resistance to HPIs; Patterns of Cross-Resistance; Further Insight into Mode of HPI Interaction with the HSV HP Complex from the Study of Resistance Mutations; The Frequency and Origin of HPI-Resistance Mutations; UL5 Lys356Asn: A Mutation Conferring High Resistance to HPI; The Origin of Resistance Mutations at High Frequency; Conclusions; CYCLOPHILIN INHIBITORS; Introduction; Cyclophilin Overview; Cyclophilin Inhibitors Currently in Clinical Development; Cyclophilin and HIV; Cyclophilin and Hepatitis C; Clinical Results in HCV; Activity against Other Viruses; New Noncyclosporine Cyclophilin Inhibitors; Conclusion; ALKOXYALKYL ESTER PRODRUGS OF ANTIVIRAL NUCLEOSIDE PHOSPHATES AND PHOSPHONATES; Introduction; Enhancing the Oral Activity of Antiviral Compounds: Overview of the Development of Alkoxyalkyl Esterification Approach; Alkylglycerol and Alkoxyalkyl Prodrugs of Phosphonoformate: Enhanced Antiviral Activity and Synergism with AZT; Alkoxyalkyl Esters of Nucleoside 5'-Monophosphates; Oral Prodrugs of Acyclic Nucleoside; Intraocular Delivery of Antiviral Prodrugs for Treatment of Prevention of Cytomegalovirus Retinitis; Conclusion; MARIBAVIR: A NOVEL BENZIMIDAZOLE RIBONUCLEOSIDE FOR THE PREVENTION AND TREATMENT OF CYTOMEGALOVIRUS DISEASES; Cytomegalovirus Diseases: Unmet Challenges; Maribavir: Antiviral Activity; Maribavir: Mechanisms of Action and Resistance; Preclinical Studies; Clinical Development of Maribavir: Early Phase I; Clinical Development in a Transplant Population; Summary and Conclusions; ANTI-HCMV COMPOUNDS; Introduction; Anti-HCMV Drugs in Clinical Use; Need for New Anti-HCMV Drugs; Novel Viral Targets; Cellular Targets; Conclusions; LETHAL MUTAGENESIS AS AN UNCONVENTIONAL APPROACH TO COMBAT HIV; Introduction; Viral Fitness and Intrinsic Mutagenesis in RNA Viruses and Retroviruses; Fundamentals of Lethal Mutagenesis; Mutagenic Pharmaceuticals as Antiviral Agents; KP-1212: From Bench to Clinic; Challenges and Advantages of Lethal Mutagenesis Compared to Conventional Strategies; Concluding Remarks and Future Perspectives; RECENT PROGRESS IN THE DEVELOPMENT OF HCV PROTEASE INHIBITORS; Introduction; HCV Therapy; Mechanism of Resistance and Cross-Resistance to NS3 Protease Inhibitors; Antiviral Potency and Clinical Efficacy of HCV Protease Inhibitors; Future Directions; ANTIVIRAL RNAi: HOW TO SILENCE VIRUSES; The Discovery of RNA Interference; Therapeutic Application of the RNAi Mechanism; Mammalian Viruses and the RNAi Mechanism; Basic Design of an RNAi Therapy against Viruses; Selecting Optimal Targets; Prevention of Viral Escape; Multiplexing siRNAs; Delivery Issues; Potential Risks of an RNAi Therapy; Example of an Acute Infection: RSV; Example of a Chronic Infection: HIV-1; Future Perspective; NEURAMINIDASE INHIBITORS AS ANTI-INFLUENZA AGENTS; Introduction; Influenza Neuraminidase as a Drug Target; Neuraminidase Active Site and Inhibitor Binding; Small-Molecule Inhibitors of Influenza Neuraminidase; Mechanism of Resistance; Influenza Neuraminidase Inhibitors Based on Other Scaffolds; Clinical Use of Neuraminidase Inhibitors; Concluding Remarks; FROM TIBO TO RILPIVIRINE: THE CHRONICLE OF THE DISCOVERY OF THE IDEAL NONNUCLEOSIDE REVERSE TRANSCRIPTASE INHIBITORS; Introduction; The TIBO Derivatives; From Loviride to Rilpivirine; Rilpivirine: How Does It Act?; Clinical Proof of Concept; Pharmacokinetics and Drug-Drug Interactions; Potency and Resilience to NNRTI Resistance; Conclusion; ;
• Publisher Details: Place of publication not identified : Wiley-VCH
• Publication Date: 2011
• Extent: 1 online resource (426 pages)
• Subjects: 615.7924; Antiviral agents -- Development
• Languages: English
• ISBNs: 9783527635962
• Access Rights: Legal Deposit; Only available on premises controlled by the deposit library and to one user at any one time; The Legal Deposit Libraries (Non-Print Works) Regulations (UK).
• Access Usage: Restricted: Printing from this resource is governed by The Legal Deposit Libraries (Non-Print Works) Regulations (UK) and UK copyright law currently in force.