ChemBioChem

Cover image for Vol. 18 Issue 10

Editor: Meghan Campbell; Editorial Board Chairs: Thomas Carell, Donald Hilvert, Barbara Imperiali

Online ISSN: 1439-7633

Associated Title(s): ChemCatChem, ChemMedChem, ChemPhysChem, ChemSusChem

October 17, 2002

Just Appeared: Special Issue on G-Protein-Coupled Receptors

Just Appeared: Special Issue on G-Protein-Coupled Receptors

ChemBioChem editors are proud of its special issue (10/2002) on G-protein-coupled receptors (GPCRs). In January 2002, G. Wess, H. Schwalbe, and T. Klabunde organized a Goethe University (Frankfurt, Germany) and Aventis Chemical Biology Workshop entitled "Dissecting G-Protein-Coupled Receptors: Structure, Function, and Ligand Interaction". This issue will contain focused articles based on the workshop including the following:

  • Drug Design Strategies for Targeting GPCRs (Review by T. Klabunde and G. Hessler)
  • Dopamine D3 Receptor Ligands (Review by H. Stark and A. E. Hackling)
  • Active States of Rhodopsin (Minireview by O. P. Ernst and F. J. Bartl)
  • NMR Spectroscopy of Membrane Proteins (Minireview by B. W. Koenig)
  • Crystal Structure of Rhodopsin (Minireview by R. E. Stenkamp et al.)
  • GPCR Microarrays (Concept by J. Lahiri et al.)
  • original contributions from the groups of G. Vriend, J. A. Hendrix, N. C. R. van Straten, B. Kobilka, and P. Schmieder
  • GPCR Web Sites (by H. Schwalbe)

Make sure you don't miss it!

The cover picture shows bovine rhodopsin, the first G-protein-coupled receptor (GPCR) structure determined at atomic resolution. It is embedded into the cell membrane with the conserved seven transmembrane helices. Rhodopsin is unique among GPCRs due to its activation mechanism: The covalently bound ligand retinal (shown in red) undergoes a light-induced isomerization, thus activating the receptor. For other GPCRs intracellular responses are modulated by binding of extracellular signal molecules and drugs. Valsartan, fexofenadine, montelukast, and clapidogrel are examples of drug compounds acting on GPCRs that bind peptides, biogenic amines, lipids, and nucleotides, respectively. Further details will be found in the review article by Klabunde and Hessler.

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