LEADER 05363nam 2200649Ia 450 001 9910829904503321 005 20170816122630.0 010 $a1-280-72281-9 010 $a9786610722815 010 $a3-527-60876-1 010 $a3-527-60860-5 035 $a(CKB)1000000000376655 035 $a(EBL)481418 035 $a(SSID)ssj0000157791 035 $a(PQKBManifestationID)11149262 035 $a(PQKBTitleCode)TC0000157791 035 $a(PQKBWorkID)10139905 035 $a(PQKB)10093951 035 $a(MiAaPQ)EBC481418 035 $a(OCoLC)85821120 035 $a(EXLCZ)991000000000376655 100 $a20060111d2006 uy 0 101 0 $aeng 135 $aur|n|---||||| 181 $ctxt 182 $cc 183 $acr 200 00$aFragment-based approaches in drug discovery$b[electronic resource] /$fedited by Wolfgang Jahnke and Daniel A. Erlanson 210 $aWeinheim $cWiley-VCH ;$a[Chichester $cJohn Wiley, distributor]$dc2006 215 $a1 online resource (393 p.) 225 1 $aMethods and principles in medicinal chemistry ;$v34 300 $aDescription based upon print version of record. 311 $a3-527-31291-9 320 $aIncludes bibliographical references and index. 327 $aFragment-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 Terms 327 $a2.3 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 Multivalency 327 $a2.4.5 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 Systems 327 $a2.5.2.2 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 Ligands 327 $a2.6.3.1 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 Ligands 327 $a2.7.3 Bivalency in the Immune System 330 $aThis first systematic summary of the impact of fragment-based approaches on the drug development process provides essential information that was previously unavailable. Adopting a practice-oriented approach, this represents a book by professionals for professionals, tailor-made for drug developers in the pharma and biotech sector who need to keep up-to-date on the latest technologies and strategies in pharmaceutical ligand design. The book is clearly divided into three sections on ligand design, spectroscopic techniques, and screening and drug discovery, backed by numerous case studies. 410 0$aMethods and principles in medicinal chemistry ;$vv. 34. 606 $aDrug development 606 $aLigands (Biochemistry) 615 0$aDrug development. 615 0$aLigands (Biochemistry) 676 $a615 676 $a615.1901 701 $aJahnke$b Wolfgang$01707025 701 $aErlanson$b Daniel A$01707026 801 0$bMiAaPQ 801 1$bMiAaPQ 801 2$bMiAaPQ 906 $aBOOK 912 $a9910829904503321 996 $aFragment-based approaches in drug discovery$94094909 997 $aUNINA LEADER 01008nam a2200277 i 4500 001 991004348236707536 005 20241106113423.0 008 241106s2004 it er 001 0 mul d 040 $aBibl. Dip.le Aggr. Scienze Umane e Sociali$bita$cSocioculturale Scs 041 1 $aita$ager 082 04$a831$223 245 00$aAntologia della poesia tedesca /$ca cura di Monica Lumachi e Paolo Scotini ; introduzione di Patrizio Collini 246 14$aPoesia straniera tedesca 260 $aRoma :$bGruppo editoriale L'Espresso,$c2004 300 $a864 p. ;$c23 cm 490 1 $aLa biblioteca di Repubblica. Poesia straniera ;$v12 500 $aSupplemento a: La Repubblica 500 $aTesto originale a fronte 650 4$aPoesia tedesca$vAntologie 700 1 $aLumachi, Monica 700 1 $aScotini, Paolo 700 1 $aCollini, Patrizio 830 3$aLa biblioteca di Repubblica. Poesia straniera ;$v12 912 $a991004348236707536 996 $aAntologia della poesia tedesca$989314 997 $aUNISALENTO