BIOspektrum

, Volume 20, Issue 1, pp 15–18 | Cite as

GPCRs als hochrelevante Targets für die Wirkstoffentwicklung

Schwerpunktthema G-Protein-Gekoppelte Rezeptoren
Wissenschaft

Abstract

G protein-coupled receptors are involved in numerous physiological processes and provide attractive drug targets for diverse diseases. However, the development of selective, efficacious drugs targeting this family of membrane proteins remains challenging due to multidimensional selectivity profiles of GPCR-agonists and antagonists. Selective GPCR ligands have the potential to induce or stabilize individual receptor conformations or to preferentially bind one particular receptor subtype.

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Literatur

  1. [1]
    Sanguinetti MC, Tristani-Firouzi M (2006) hERG potassium channels and cardiac arrhythmia. Nature 440:463–469PubMedCrossRefGoogle Scholar
  2. [2]
    Strasser A, Wittmann H-J, Buschauer A et al. (2012) Species-dependent activities of G-protein-coupled receptor ligands: lessons from histamine receptor orthologs. Trends Pharmacol Sci 34:13–31PubMedCrossRefGoogle Scholar
  3. [3]
    Löber S, Hübner H, Tschammer N et al. (2011) Recent advances in the search for D3- and D4-selective drugs: probes, models and candidates. Trends Pharmacol Sci 32:148–157PubMedCrossRefGoogle Scholar
  4. [4]
    Held C, Kling R, Gmeiner P (2013) Struktur und Funktion β-adrenerger Rezeptoren. Pharmakon 1:406–412Google Scholar
  5. [5]
    Wei H, Ahn S, Shenoy SK et al. (2003) Independent β-arrestin 2 and G protein-mediated pathways for angiotensin II activation of extracellular signal-regulated kinases 1 and 2. Proc Natl Acad Sci USA 100:10782–10787PubMedCrossRefGoogle Scholar
  6. [6]
    Hiller C, Kling RC, Heinemann FW et al. (2013) Functionally selective dopamine D2/D3 receptor agonists comprising an enyne moiety. J Med Chem 56:5130–5141PubMedCrossRefGoogle Scholar
  7. [7]
    Daniels DJ, Lenard NR, Etienne CL et al. (2005) Opioidinduced tolerance and dependence in mice is modulated by the distance between pharmacophores in a bivalent ligand series. Proc Natl Acad Sci USA 102:19208–19213PubMedCrossRefGoogle Scholar

Copyright information

© Springer-Verlag Berlin Heidelberg 2014

Authors and Affiliations

  1. 1.Lehrstuhl für Pharmazeutische ChemieUniversität Erlangen-NürnbergErlangenDeutschland
  2. 2.Lehrstuhl für Pharmazeutische ChemieFriedrich-Alexander-Universität Erlangen-NürnbergErlangenDeutschland

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