1.

Record Nr.

UNINA9910831167703321

Titolo

Ligand design for G protein-coupled receptors [[electronic resource] /] / edited by Didier Rognan

Pubbl/distr/stampa

Weinheim ; ; [Great Britain], : Wiley, 2006

ISBN

1-280-72349-1

9786610723492

3-527-60824-9

3-527-60826-5

Descrizione fisica

1 online resource (286 p.)

Collana

Methods and principles in medicinal chemistry ; ; v. 30

Altri autori (Persone)

RognanDidier

Disciplina

541.2242

615.19

Soggetti

Ligands (Biochemistry)

G proteins

Drugs - Design

Lingua di pubblicazione

Inglese

Formato

Materiale a stampa

Livello bibliografico

Monografia

Note generali

Description based upon print version of record.

Nota di bibliografia

Includes bibliographical references and index.

Nota di contenuto

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 Cluster

1.6.1.5 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 GPCRs

1.8 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

3.2.2 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

4.3 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

4.8 Asymmetric Functioning of the HD Dimer

Sommario/riassunto

G 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



2.

Record Nr.

UNINA9911007369403321

Titolo

Food colloids : interactions, microstructure and processing / / edited by Eric Dickinson

Pubbl/distr/stampa

Cambridge, : Royal Society of Chemistry, 2005

ISBN

9781628704648

1628704640

9781847552389

1847552382

Edizione

[1st ed.]

Descrizione fisica

1 online resource (498 p.)

Collana

Special publication ; ; no. 298

Altri autori (Persone)

DickinsonEric

Disciplina

664

Soggetti

Colloids

Food - Composition

Food - Analysis

Lingua di pubblicazione

Inglese

Formato

Materiale a stampa

Livello bibliografico

Monografia

Note generali

"The proceedings of Food Colloids 2004 : Interactions, Microstructure and Processing held on 18-21 April 2004 in Harrogate"--T.p. verso.

Nota di bibliografia

Includes bibliographical references and index.

Nota di contenuto

FCO-Prelim; FCO-Preface; FCO-Contents; FCO-1Chapter 1; FCO-16Chapter 2; FCO-26Chapter 3; FCO-37Chapter 4; FCO-48Chapter 5; FCO-59Chapter 6; FCO-74Chapter 7; FCO-85Chapter 8; FCO-97Chapter 9; FCO-120Chapter 10; FCO-131Chapter 11; FCO-143Chapter 12; FCO-152Chapter 13; FCO-160Chapter 14; FCO-177Chapter 15; FCO-194Chapter 16; FCO-209Chapter 17; FCO-218Chapter 18; FCO-230Chapter 19; FCO-237Chapter 20; FCO-247Chapter 21; FCO-257Chapter 22; FCO-273Chapter 23; FCO-284Chapter 24; FCO-301Chapter 25; FCO-317Chapter 26; FCO-326Chapter 27; FCO-337Chapter 28; FCO-356Chapter 29; FCO-367Chapter 30

FCO-380Chapter 31FCO-393Chapter 32; FCO-420Chapter 33; FCO-432Chapter 34; FCO-443Chapter 35; FCO-466Chapter 36; FCO-482Index

Sommario/riassunto

Food Colloids: Interactions, Microstructure and Processing describes the principles and practice underlying the formulation of food emulsions, dispersions, gels, and foams. Emphasis is on understanding



how the functional properties of biopolymers and surfactants determine the texture and shelf-life of multiphase food materials. This book provides essential new findings by experts in the field on specific topics including: the interfacial rheological properties of proteins; the use of microscopy and image analysis to probe structure and phase transitions; the control of colloidal stability duri