Ligand Design for G Protein-coupled Receptors, Volume 30 (Methods and Principles in Medicinal Chemistry)

Content: G protein-coupled receptors in the human genome / Robert Fredriksson and Helgi B. Schiöth -- Why G protein-coupled receptors databases are needed / Jacques Haiech ... [et al.] -- A novel drug screening assay for G protein-coupled receptors / Brian F. O'Dowd ... [et al.] -- Importance of GPCR dimerization for function : the case of the class C GPCRs / Laurent Prézeau ... [et al.] -- Molecular mechanisms of GPCR activation / Robert P. Bywater and Paul Denny-Gouldson -- Allosteric properties and regulation of G protein-coupled receptors / Jean-Luc Galzi ... [et al.] -- Chemogenomics approaches to ligand design / Thomas Klabunde -- Strategies for the design of pGPCR-targeted libraries / Nikolay P. Savchuk, Sergey E. Tkachenko, and Konstantin V. Balakin -- Ligand-based rational design : virtual screening / David E. Clark and Christopher Higgs -- 3-D structure of G protein-coupled receptors / Leonardo Pardo ... [et al.] -- 7TM models in structure-based drug design / Frank E. Blaney, Anna-Maria Capelli, and Giovanna Tedesco -- Receptor-based rational design : virtual screening / Didier Rognan

g Protein-coupled Receptors (gpcrs) Are Important Switches In Biological Signal Transduction And Constitute The Most Numerous Protein Class In Higher Organisms, Reflecting Their Involvement In The Hormonal Regulation Of Virtually All Body Processes. This Regulatory Function Makes Them Prime Drug Targets, And Many Blockbuster Drugs Act Either Directly Or Indirectly On Gpcrs. Yet It Is Only With The Recent Elucidation Of The Rhodopsin Structure That These Receptors Have Become Amenable To A Rational Drug Design.

this Is The First Work To Describe In Detail The Structure-based Rational Approach To Gpcr Drug Design. Based On Recent Examples From Academia And The Pharmaceutical Industry, It Demonstrates How To Apply The Whole Range Of Bioinformatics, Chemoinformatics And Molecular Modeling Tools To The Rational Design Of Novel Drugs Targeting Gpcrs.

from The Contents:

• gpcrs In The Human Genome

• gpcr Three-dimensional Structures: From Bovine Rhodopsin To Homology Models

• orphan Gpcrs And Ligand Design

• gpcr Databases: From Genes To Proteins, From Proteins To Ligands

• druggability Of Human Gpcrs

• molecular Mechanisms Of Gpcr Activation & Oligomerisation

• allosteric Regulation Of Gpcrs

• ligand-based Rational Design

• receptor-based Rational Design

• chemogenomics Approaches To Ligand Design And Target Priorisation

• gpcr Targeted Libraries And Privileged Structures

essential Reading For Medicinal Chemists, Biochemists, Pharmaceutical Chemists, Biotechnologists And Drug Designers Working In The Pharmaceutical And Biotechnological Industries.