G Protein-Coupled Receptors in Drug Discovery pp 51-66

Part of the Methods in Molecular Biology book series (MIMB, volume 552)

| Cite as

An Overview on GPCRs and Drug Discovery: Structure-Based Drug Design and Structural Biology on GPCRs

  • Kenneth Lundstrom


G protein-coupled receptors (GPCRs) represent 50–60% of the current drug targets. There is no doubt that this family of membrane proteins plays a crucial role in drug discovery today. Classically, a number of drugs based on GPCRs have been developed for such different indications as cardiovascular, metabolic, neurodegenerative, psychiatric, and oncologic diseases. Owing to the restricted structural information on GPCRs, only limited exploration of 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.

Key words

GPCRs Drug discovery Overexpression Functional receptor X-ray crystallography Structure-based drug design 


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Copyright information

© Humana Press, a part of Springer Science+Business Media, LLC 2009

Authors and Affiliations

  • Kenneth Lundstrom
    • 1
  1. 1.PanTherapeuticsLutry

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