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BL
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| Record Number
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856441
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| Title & Author
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Advances in nucleic acid therapeutics /\ edited by Sudhir Agrawal and Michael J. Gait.
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| Publication Statement
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Cambridge, UK :: Royal Society of Chemistry,, [2019]
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| Series Statement
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Drug discovery series ;; no. 68,
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| Page. NO
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1 online resource (1 volume)
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| ISBN
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1788015711
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: 1788017323
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: 9781788015714
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: 9781788017329
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1788012097
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9781788012096
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| Bibliographies/Indexes
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Includes bibliographical references and index.
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| Contents
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Intro; Half Title; Series Editors; Title; Copyright; Foreword; Preface; Contents; Chapter 1 History and Development of Nucleotide Analogues in Nucleic Acids Drugs 1; 1.1 Introduction; 1.2 The Antisense Concept; 1.3 Developments in Oligonucleotide Synthesis; 1.4 Choices for Antisense Oligodeoxynucleotide Modifications; 1.4.1 Backbone Modifications; 1.4.2 Heterocyclic Bases; 1.4.3 Sugar Modifications; 1.5 Gapmers Using Combinations of Modified Oligodeoxy and/or Oligoribonucleotides; 1.6 Antisense Conjugates; 1.7 The Role of Innate Immune Receptors in Nucleic Acid Therapeutics
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1.8 Future DirectionsAcknowledgements; References; Chapter 2 Mechanisms of Antisense Oligonucleotides 22; 2.1 Introduction; 2.2 RNase H and ASO Action; 2.3 ASOs and Regulation of Splicing; 2.4 ASOs and Activation of Frataxin, a Case Study for an Emerging Mechanism; 2.5 Summary; Acknowledgements; References; Chapter 3 The Medicinal Chemistry of RNase H-activating Antisense Oligonucleotides 32; 3.1 Introduction to Gapmers; 3.2 Human RNase H1; 3.2.1 Biochemistry of Human RNase H1; 3.2.2 Structural Biology of Human RNase H1; 3.3 Structure-Activity Relationships of Gap Modifications
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3.5.4 ASO Gapmer Duplexes3.6 Control of Protein Binding; 3.6.1 Interaction of Gapmer ASOs with Plasma Proteins; 3.6.2 Interaction of Gapmer-ASOs with Cell-surface Proteins; 3.6.3 Targeting Cell-surface Proteins for Cell-specific Delivery of Gapmers; 3.6.4 Avoiding Interactions with TLR Receptors to Avoid Immune-stimulatory Toxicities; 3.6.5 Optimizing Intracellular Distribution; 3.7 Conclusions; References; Chapter 4 Antisense Technology: Liver Targeting and Beyond for Drug Discovery 62; 4.1 Introduction; 4.2 Liver Targeting; 4.2.1 The Beginning; 4.2.2 Broadening the Liver-targeting Pipeline
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4.3 Innovations in Liver Targeting4.4 Beyond the Liver; 4.5 Conclusions; References; Chapter 5 Oligonucleotide-based Toll-like Receptor Antagonists and Therapeutic Applications 80; 5.1 Introduction; 5.2 Oligonucleotide-based TLR Antagonists; 5.2.1 Structure-Activity Relationship Studies; 5.2.2 TLR Antagonists; 5.2.3 Inhibitory Activity of TLR Antagonists; 5.2.4 Inhibitory Activity of Clinical Candidates; 5.3 Studies of TLR Antagonists in Disease Models; 5.3.1 Psoriasis; 5.3.2 Systemic Lupus Erythematosus (SLE); 5.3.3 Rheumatoid Arthritis (RA); 5.3.4 Duchenne Muscular Dystrophy (DMD)
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| Abstract
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Advances in Nucleic Acid Therapeutics provides a broad overview of techniques of contemporary interest in drug discovery.
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| Subject
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Nucleic acids-- Therapeutic use.
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| Subject
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MEDICAL-- Pharmacology.
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| Subject
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Nucleic acids-- Therapeutic use.
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| Dewey Classification
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615.31
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| LC Classification
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QP551.A3257 2019
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| Added Entry
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Agrawal, Sudhir
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Gait, M. J., (Michael J.)
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| Added Entry
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Royal Society of Chemistry (Great Britain),issuing body.
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