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SHR Neuro Krebs Kardio Lipid Stoffw Microb
Waldhoer, M; Fong, J; Jones, RM; Lunzer, MM; Sharma, SK; Kostenis, E; Portoghese, PS; Whistler, JL.
A heterodimer-selective agonist shows in vivo relevance of G protein-coupled receptor dimers.
PROC NAT ACAD SCI USA. 2005; 102: 9050-9055.
Doi: 10.1073/pnas.0501112102
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- Führende Autor*innen der Med Uni Graz
- Waldhoer Maria
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- Abstract:
- There has been much speculation regarding the functional relevance of G protein-coupled receptor heterodimers, primarily because demonstrating their existence in vivo has proven to be a considerable challenge. Here we show that the opioid agonist ligand 6'-guanidinonaltrindole (6'-GNTI) has the unique property of selectively activating only opioid receptor heterodimers but not homomers. Importantly, 6'-GNTI is an analgesic, thereby demonstrating that opioid receptor heterodimers are indeed functionally relevant in vivo. However, 6'-GNTI induces analgesia only when it is administered in the spinal cord but not in the brain, suggesting that the organization of heterodimers is tissue-specific. This study demonstrates a proof of concept for tissue-selective drug targeting based on G protein-coupled receptor heterodimerization. Importantly, targeting opioid heterodimers could provide an approach toward the design of analgesic drugs with reduced side effects.
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