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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1064-3745 e for cell-based GPCR screening written by leading researcheThe G protein-coupled receptors (GPCRs) and associated peripheral G proteins underpin a multitude of physiological processes. The GPCRs represent one of the largest superfamilies in the human genome and are a significant target for bioactiv

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20. H?mophilie-Symposion Hamburg 1989enous assay systems can be used to monitor the signaling cascades of GPCRs. This chapter details the authors’ collective experience of using the DiscoverX Hit Hunter cAMPII kit from GE Healthcare/DiscoverX Corporation for the direct quantification of cAMP levels in Gs and Gi GPCRs.

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,Psychopharmaka — ja oder nein?,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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,Versuche über Lochleibungsdruck,f 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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Thomas Wiedenhorn,Ursula Pfeiffer-Blattnerample, 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.