05411nam 2200673Ia 450 991014427410332120170814180155.01-280-72349-197866107234923-527-60824-93-527-60826-5(CKB)1000000000376653(EBL)481392(OCoLC)609855273(SSID)ssj0000301765(PQKBManifestationID)11215509(PQKBTitleCode)TC0000301765(PQKBWorkID)10264696(PQKB)10796418(MiAaPQ)EBC481392(EXLCZ)99100000000037665320060118d2006 uy 0engur|n|---|||||txtccrLigand design for G protein-coupled receptors[electronic resource] /edited by Didier RognanWeinheim ;[Great Britain] Wiley20061 online resource (286 p.)Methods and principles in medicinal chemistry ;v. 30Description based upon print version of record.3-527-31284-6 Includes bibliographical references and index.Ligand 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 α-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 Cluster1.6.1.5 The MECA Receptor Cluster1.6.1.6 Other Rhodopsin α-Receptors; 1.6.2 Rhodopsin β-Group; 1.6.3 Rhodopsin γ-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 γ-Receptors; 1.6.4 The Rhodopsin δ-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 α-Receptors; 1.7 Other GPCRs1.8 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 Assay3.2.2 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-Tail4.3 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 GPCRs4.8 Asymmetric Functioning of the HD DimerG 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 Methods and principles in medicinal chemistry ;v. 30.Ligands (Biochemistry)G proteinsDrugsDesignElectronic books.Ligands (Biochemistry)G proteins.DrugsDesign.541.2242615.19Rognan Didier505528MiAaPQMiAaPQMiAaPQBOOK9910144274103321Ligand design for G protein-coupled receptors1968231UNINA