LEADER 05411nam 2200673Ia 450 001 9910144274103321 005 20170814180155.0 010 $a1-280-72349-1 010 $a9786610723492 010 $a3-527-60824-9 010 $a3-527-60826-5 035 $a(CKB)1000000000376653 035 $a(EBL)481392 035 $a(OCoLC)609855273 035 $a(SSID)ssj0000301765 035 $a(PQKBManifestationID)11215509 035 $a(PQKBTitleCode)TC0000301765 035 $a(PQKBWorkID)10264696 035 $a(PQKB)10796418 035 $a(MiAaPQ)EBC481392 035 $a(EXLCZ)991000000000376653 100 $a20060118d2006 uy 0 101 0 $aeng 135 $aur|n|---||||| 181 $ctxt 182 $cc 183 $acr 200 00$aLigand design for G protein-coupled receptors$b[electronic resource] /$fedited by Didier Rognan 210 $aWeinheim ;$a[Great Britain] $cWiley$d2006 215 $a1 online resource (286 p.) 225 1 $aMethods and principles in medicinal chemistry ;$vv. 30 300 $aDescription based upon print version of record. 311 $a3-527-31284-6 320 $aIncludes bibliographical references and index. 327 $aLigand Design for G Protein-coupled Receptors; Contents; Preface; A Personal Foreword; List of Contributors; 1 G Protein-coupled Receptors in the Human Genome; 1.1 Introduction; 1.2 The Adhesion Family; 1.3 The Secretin Family; 1.4 The Frizzled/Taste 2 Family; 1.4.1 The Frizzled Receptor Cluster; 1.4.2 The Taste 2 Receptor Cluster; 1.5 The Glutamate Family; 1.6 The Rhodopsin Family; 1.6.1 The Rhodopsin ?-Group; 1.6.1.1 The Prostaglandin Receptor Cluster; 1.6.1.2 The Amine Receptor Cluster; 1.6.1.3 The Opsin Receptor Cluster; 1.6.1.4 The Melatonin Receptor Cluster 327 $a1.6.1.5 The MECA Receptor Cluster1.6.1.6 Other Rhodopsin ?-Receptors; 1.6.2 Rhodopsin ?-Group; 1.6.3 Rhodopsin ?-Group; 1.6.3.1 The SOG Receptor Cluster; 1.6.3.2 The Melanocyte Concentrating Hormone Receptor Cluster; 1.6.3.3 The Chemokine Receptor Cluster; 1.6.3.4 Other Rhodopsin ?-Receptors; 1.6.4 The Rhodopsin ?-Group; 1.6.4.1 The MAS-related Receptor Cluster; 1.6.4.2 The Glycoprotein Receptor Cluster; 1.6.4.3 The Coagulation Factor Receptor Cluster; 1.6.4.4 The Purinergic Receptor Cluster; 1.6.4.5 The Olfactory Receptor Cluster; 1.6.4.6 Other Rhodopsin ?-Receptors; 1.7 Other GPCRs 327 $a1.8 Future PerspectiveReferences; 2 Why G Protein-coupled Receptors Databases are Needed; 2.1 Introduction; 2.2 A Non-exhaustive List of the GPCR Data Models; 2.3 Using the Central Dogma of Biology; 2.4 Using the Tree of Life; 2.5 Using a Chemogenomic Approach; 2.6 Conclusion; References; 3 A Novel Drug Screening Assay for G Protein-coupled Receptors; 3.1 Introduction; 3.1.1 History; 3.1.2 Nuclear Translocation of Endogenous GPCRs; 3.1.3 The MOCA Method; 3.2 The MOCA Strategy Demonstrated with the D1 Dopamine Receptor; 3.2.1 Development of the Assay 327 $a3.2.2 Concentration-dependent Antagonist Blockade of Nuclear Transport3.2.3 Measurement of Receptor Cell Surface Expression: Antagonist Binding of Receptors at Cell Surface; 3.3 Development of Quantitative Methodology Suitable for High Throughput Analysis; 3.3.1 Nuclear Translocation of Orphan GPCRs; 3.4 Discussion of the MOCA Method; 3.5 Conclusion; References; 4 Importance of GPCR Dimerization for Function: The Case of the Class C GPCRs; 4.1 Introduction; 4.2 Class C GPCRs are Multidomain Proteins; 4.2.1 The VFT; 4.2.2 The CRD; 4.2.3 The HD; 4.2.4 C-Tail 327 $a4.3 Class C GPCRs are Constitutive Dimers4.4 Agonists Activate Class C GPCRs by Stabilizing the Closed State of the VFT; 4.5 Dimeric Functioning of the Dimer of VFTs; 4.5.1 Agonist Stoichiometry: Symmetry or Asymmetry?; 4.6 The Heptahelical Domain, the Target of Positive and Negative Allosteric Modulators, Behaves in a Manner Similar to Rhodopsin-like Class A GPCRs; 4.7 Allosteric Coupling Between the Extracellular and Heptahelical Domains within the Dimer; 4.7.1 Molecular Determinants of the Coupling Between the VFT and the HD; 4.7.2 Cis- and Trans-activation Can Exist within Class C GPCRs 327 $a4.8 Asymmetric Functioning of the HD Dimer 330 $aG protein-coupled receptors (GPCRs) are one of the most important target classes in pharmacology and are the target of many blockbuster drugs. Yet only with the recent elucidation of the rhodopsin structure have these receptors become amenable to a rational drug design.Based on recent examples from academia and the pharmaceutical industry, this book demonstrates how to apply the whole range of bioinformatics, chemoinformatics and molecular modeling tools to the rational design of novel drugs targeting GPCRs. Essential reading for medicinal chemists and drug designers working with this 410 0$aMethods and principles in medicinal chemistry ;$vv. 30. 606 $aLigands (Biochemistry) 606 $aG proteins 606 $aDrugs$xDesign 608 $aElectronic books. 615 0$aLigands (Biochemistry) 615 0$aG proteins. 615 0$aDrugs$xDesign. 676 $a541.2242 676 $a615.19 701 $aRognan$b Didier$0505528 801 0$bMiAaPQ 801 1$bMiAaPQ 801 2$bMiAaPQ 906 $aBOOK 912 $a9910144274103321 996 $aLigand design for G protein-coupled receptors$91968231 997 $aUNINA