05395nam 2200661Ia 450 991014427360332120170816122630.01-280-72281-997866107228153-527-60876-13-527-60860-5(CKB)1000000000376655(EBL)481418(OCoLC)85821120(SSID)ssj0000157791(PQKBManifestationID)11149262(PQKBTitleCode)TC0000157791(PQKBWorkID)10139905(PQKB)10093951(MiAaPQ)EBC481418(EXLCZ)99100000000037665520060111d2006 uy 0engur|n|---|||||txtccrFragment-based approaches in drug discovery[electronic resource] /edited by Wolfgang Jahnke and Daniel A. ErlansonWeinheim Wiley-VCH ;[Chichester John Wiley, distributor]c20061 online resource (393 p.)Methods and principles in medicinal chemistry ;34Description based upon print version of record.3-527-31291-9 Includes bibliographical references and index.Fragment-based Approaches in Drug Discovery; Contents; Preface; A Personal Foreword; List of Contributors; Part I: Concept and Theory; 1 The Concept of Fragment-based Drug Discovery; 1.1 Introduction; 1.2 Starting Small: Key Features of Fragment-based Ligand Design; 1.2.1 FBS Samples Higher Chemical Diversity; 1.2.2 FBS Leads to Higher Hit Rates; 1.2.3 FBS Leads to Higher Ligand Efficiency; 1.3 Historical Development; 1.4 Scope and Overview of this Book; References; 2 Multivalency in Ligand Design; 2.1 Introduction and Overview; 2.2 Definitions of Terms2.3 Selection of Key Experimental Studies2.3.1 Trivalency in a Structurally Simple System; 2.3.2 Cooperativity (and the Role of Enthalpy) in the "Chelate Effect"; 2.3.3 Oligovalency in the Design of Inhibitors to Toxins; 2.3.4 Bivalency at Well Defined Surfaces (Self-assembled Monolayers, SAMs); 2.3.5 Polyvalency at Surfaces of Viruses, Bacteria, and SAMs; 2.4 Theoretical Considerations in Multivalency; 2.4.1 Survey of Thermodynamics; 2.4.2 Additivity and Multivalency; 2.4.3 Avidity and Effective Concentration (C(eff)); 2.4.4 Cooperativity is Distinct from Multivalency2.4.5 Conformational Entropy of the Linker between Ligands2.4.6 Enthalpy/Entropy Compensation Reduces the Benefit of Multivalency; 2.5 Representative Experimental Studies; 2.5.1 Experimental Techniques Used to Examine Multivalent Systems; 2.5.1.1 Isothermal Titration Calorimetry; 2.5.1.2 Surface Plasmon Resonance Spectroscopy; 2.5.1.3 Surface Assays Using Purified Components (Cell-free Assays); 2.5.1.4 Cell-based Surface Assays; 2.5.2 Examination of Experimental Studies in the Context of Theory; 2.5.2.1 Trivalency in Structurally Simple Systems2.5.2.2 Cooperativity (and the Role of Enthalpy) in the "Chelate Effect"2.5.2.3 Oligovalency in the Design of Inhibitors of Toxins; 2.5.2.4 Bivalency in Solution and at Well Defined Surfaces (SAMs); 2.5.2.5 Polyvalency at Surfaces (Viruses, Bacteria, and SAMs); 2.6 Design Rules for Multivalent Ligands; 2.6.1 When Will Multivalency Be a Successful Strategy to Design Tight-binding Ligands?; 2.6.2 Choice of Scaffold for Multivalent Ligands; 2.6.2.1 Scaffolds for Oligovalent Ligands; 2.6.2.2 Scaffolds for Polyvalent Ligands; 2.6.3 Choice of Linker for Multivalent Ligands2.6.3.1 Rigid Linkers Represent a Simple Approach to Optimize Affinity2.6.3.2 Flexible Linkers Represent an Alternative Approach to Rigid Linkers to Optimize Affinity; 2.6.4 Strategy for the Synthesis of Multivalent Ligands; 2.6.4.1 Polyvalent Ligands: Polymerization of Ligand Monomers; 2.6.4.2 Polyvalent Ligands: Functionalization with Ligands after Polymerization; 2.7 Extensions of Multivalency to Lead Discovery; 2.7.1 Hetero-oligovalency Is a Broadly Applicable Concept in Ligand Design; 2.7.2 Dendrimers Present Opportunities for Multivalent Presentation of Ligands2.7.3 Bivalency in the Immune SystemThis first systematic summary of the impact of fragment-based approaches on the drug development process provides essential information that was previously unavailable. Adopting a practice-oriented approach, this represents a book by professionals for professionals, tailor-made for drug developers in the pharma and biotech sector who need to keep up-to-date on the latest technologies and strategies in pharmaceutical ligand design. The book is clearly divided into three sections on ligand design, spectroscopic techniques, and screening and drug discovery, backed by numerous case studies.Methods and principles in medicinal chemistry ;v. 34.Drug developmentLigands (Biochemistry)Electronic books.Drug development.Ligands (Biochemistry)615615.1901Jahnke Wolfgang997913Erlanson Daniel A997914MiAaPQMiAaPQMiAaPQBOOK9910144273603321Fragment-based approaches in drug discovery2288667UNINA02562nam 2200685Ia 450 991078488980332120231005182119.00-19-772344-61-280-52655-60-19-535992-51-4294-0776-X(CKB)1000000000399740(EBL)271202(OCoLC)191932219(SSID)ssj0000124535(PQKBManifestationID)11136542(PQKBTitleCode)TC0000124535(PQKBWorkID)10024171(PQKB)10224836(Au-PeEL)EBL271202(CaPaEBR)ebr10142220(CaONFJC)MIL52655(OCoLC)936850440(MiAaPQ)EBC271202(EXLCZ)99100000000039974019920715d1993 uy 0engur|n|---|||||txtrdacontentcrdamediacrrdacarrierCold War criticism and the politics of skepticism /Tobin SiebersNew York :Oxford University Press,1993.1 online resource (xi, 163 pages)Odéon0-19-507964-7 0-19-507965-5 Includes bibliographical references and index.Contents; 1. Introduction: The Politics of Skepticism; 2. Cold War Criticism; 3. Ethics or Politics? Comparative Literature, Multiculturalism, and Cultural Literacy; 4. Mourning Becomes Paul de Man; 5. The Politics of the Politics of Interpretation; 6. The Politics of Storytelling: Hannah Arendt's Eichmann in Jerusalem; 7. Conclusion: Toward a Post-Cold War Criticism; IndexClaiming that a Cold War mentality has impaired the ability of literary theorists to talk about the politics of criticism effectively, the author of this treatise argues that modern criticism is a child of the Cold War.Odéon.CriticismPolitical aspectsCold War in literaturePolitics and literatureCritical theorySkepticismCriticismPolitical aspects.Cold War in literature.Politics and literature.Critical theory.Skepticism.801/.95/09045Siebers Tobin845392MiAaPQMiAaPQMiAaPQBOOK9910784889803321Cold War criticism and the politics of skepticism3688791UNINA