## Abstract It has been recently established that G‐protein‐coupled receptors (GPCRs) can be constitutively active, i.e., they can be active in the absence of an agonist. This activity can be inhibited by so‐called inverse agonists. For a number of GPCRs, such inverse agonists have been developed a
Cell-Penetrating Mimics of Agonist-Activated G-Protein Coupled Receptors
✍ Scribed by Pernilla Östlund; Kalle Kilk; Maria Lindgren; Mattias Hällbrink; Yang Jiang; Metka Budihna; Katarina Cerne; Aljosa Bavec; Claes-Göran Östenson; Matjaz Zorko; Ülo Langel
- Publisher
- Springer Netherlands
- Year
- 2005
- Tongue
- English
- Weight
- 360 KB
- Volume
- 11
- Category
- Article
- ISSN
- 1573-3149
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A modified concept of functioning of G-protein coupled receptors is presented, on the assumption that agonistic and antagonistic effects of drugs are related to their interaction with two separate receptor sites that exist simultaneously on a single receptor molecule and possess different ligand-spe