Ligand efficacy and affinity in an interacting 7TM receptor model

ONARAN H. O., GÜRDAL H.

TRENDS IN PHARMACOLOGICAL SCIENCES, cilt.20, sa.7, ss.274-278, 1999 (SCI-Expanded) identifier identifier identifier

  • Yayın Türü: Makale / Tam Makale
  • Cilt numarası: 20 Sayı: 7
  • Basım Tarihi: 1999
  • Doi Numarası: 10.1016/s0165-6147(99)01364-4
  • Dergi Adı: TRENDS IN PHARMACOLOGICAL SCIENCES
  • Derginin Tarandığı İndeksler: Science Citation Index Expanded (SCI-EXPANDED), Scopus
  • Sayfa Sayıları: ss.274-278
  • Ankara Üniversitesi Adresli: Evet

Özet

Quantitative understanding of the activation of G protein-coupled receptors is based mostly on some theoretical models that describe the interaction between ligand and protein partners and the activation process of the receptor. All of these models provide different definitions for observable affinity or efficacy. However, the property common to such parameters defined in the context of these models is that they are always independent of the concentration of the receptor molecule. This is based on the assumption that receptors do not interact with each other appreciably. In this article, experimental evidence for which this assumption does not seem to apply is discussed and an oligomerization model for seven-transmembrane-domain receptors that explains the relationship between receptor concentration, apparent affinity and efficacy is provided.