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Functional coupling of μ-receptor-Gαi-tethered proteins in AtT20 cells

Identifieur interne : 008D22 ( Main/Exploration ); précédent : 008D21; suivant : 008D23

Functional coupling of μ-receptor-Gαi-tethered proteins in AtT20 cells

Auteurs : Billy C. Chieng [Australie] ; David J. Lee [Australie] ; Yan P. Du [Australie] ; Peregrine B. Osborne [Australie] ; Macdonald J. Christie [Australie] ; Dominique Massotte [France]

Source :

RBID : Pascal:09-0026231

Descripteurs français

English descriptors

Abstract

Opioid efficacy on μ-receptor may be influenced by various Gi/o-G-protein subunits interacting with intracellular face of receptor. Pertussis toxin-insensitive Gαil and Gαi2 subunits tethered with μ-receptor were stably transfected into AtT20 cells to (i) determine coupling of different α-subunits on opioid efficacy, and (ii) determine coupling to downstream effectors, for example, calcium and potassium channels. After pertussis toxin, stimulation of [35S]GTP-γ-S incorporation persisted. Both constructs were able to couple to native calcium and potassium channels, with endomorphins I and 2 equally effective. However, pertussis toxin abolished opioid actions on calcium and potassium channels suggesting strong coupling to endogenous G-proteins, and that differences in coupling efficacy to Gαj1 and Gαj2 previously observed are restricted to initial step of signaling cascade.


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Le document en format XML

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<div type="abstract" xml:lang="en">Opioid efficacy on μ-receptor may be influenced by various G
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<sub>il</sub>
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<sub>i2</sub>
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<sup>35</sup>
S]GTP-γ-S incorporation persisted. Both constructs were able to couple to native calcium and potassium channels, with endomorphins I and 2 equally effective. However, pertussis toxin abolished opioid actions on calcium and potassium channels suggesting strong coupling to endogenous G-proteins, and that differences in coupling efficacy to Gα
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