1st Edition

G Protein-Coupled Receptors in Drug Discovery

Edited By Kenneth H. Lundstrom, Mark L. Chiu Copyright 2006
    376 Pages
    by CRC Press

    376 Pages
    by CRC Press

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    The broad range of G protein-coupled receptors (GPCRs) encompasses all areas of modern medicine and have an enormous impact on the process of drug development. Using disease-oriented methods to cover everything from screening to expression and crystallization, G Protein-Coupled Receptors in Drug Discovery describes the physiological roles of GPCRs and their involvement in various human diseases.

    The book presents current approaches in drug discovery that include target selection, establishment of screening and functional assays. It also covers recombinant GPCR expression for drug screening and structural biology, different methods for structural characterization of GPCRs, and the importance of bioinformatics. The book has been carefully edited to avoid overlapping information, some duplication has been intentionally permitted so that each chapter can function as an independent unit. Providing in-depth discussions on structure and dynamics of GPCRs, this book outlines the importance of the GPCRs to drug discovery in general and drug targets specifically.

    Daniel E. Levy, editor of the Drug Discovery Series, is the founder of DEL BioPharma, a consulting service for drug discovery programs. He also maintains a blog that explores organic chemistry.

    Introduction. G Protein-Coupled Receptors as Targets for Drug Discovery. G Protein-Coupled Receptors in Cardiovascular Diseases. G Protein-Coupled Receptors in Cancer. G Protein-Coupled Receptors in Metabolic Disease. G Protein- Coupled Receptors in CNS Drug Discovery. Recombinant G Protein-Coupled Receptors for Drug Discovery. High Throughput Screening Assays for G Protein-Coupled Receptors. Bioinformatics/ Molecular Modelling of G Protein-Coupled Receptors. Structure and Dynamics of G Protein-Coupled Receptors. Toward Crystallization of G Protein-Coupled Receptors. Novel Solid-State NMR Methods for Structural Studies on G Protein-Coupled Receptors. Structural Genomics Initiatives on G Protein-Coupled Receptors. Dimerization of G Protein-Coupled Receptors. Orphan G Protein-Coupled Receptors.


    Kenneth H. Lundstrom, Mark L. Chiu