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Titlebook: G Protein-Coupled Receptors in Drug Discovery; Wayne R. Leifert Book 2009 Humana Press 2009 Calcium.Cellular signalling.Chemokine.Drug dev

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New Insights into GPCR Function: Implications for HTS,ique targeted therapeutic uses, including “designer” drugs such as allosteric regulators, inverse agonists, and drugs targeting hetero-oligomeric complexes. This has been facilitated by the development of new screening technologies to identify novel drugs against both known and orphan GPCRs.
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An Overview on GPCRs and Drug Discovery: Structure-Based Drug Design and Structural Biology on GPCRf structure-based drug design has been possible. Much effort has been dedicated to structural biology on GPCRs and very recently an X-ray structure of the β2-adrenergic receptor was obtained. This breakthrough will certainly increase the efforts in structural biology on GPCRs and furthermore speed up and facilitate the drug discovery process.
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BacMam: Versatile Gene Delivery Technology for GPCR Assays,ample, coexpression of a receptor and a G protein or a reporter gene. BacMam viruses are compatible with the GPCR cell-based assay formats typically used in high-throughput screening and provide an unparalleled level of experimental flexibility that is simply not possible when using stable recombinant cell lines.
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Resonant Waveguide Grating Biosensor for Whole-Cell GPCR Assays,disease relevant environments. We have shown that these biosensor assays enable high-throughput screening of pathway-biased ligands acting on endogenous β.-adrenergic receptor in cells. These biosensor cellular assays hold the potential to reduce attrition rates in drug discovery and development process.
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