Article
Effect of a toggle switch mutation in TM6 of the human adenosine A₃ receptor on Gi protein-dependent signalling and Gi-independent receptor internalization.
British journal of pharmacology - 1 Aug 2014
Stoddart Leigh A, Kellam Barrie, Briddon Stephen J, Hill Stephen J
Abstract excerpt
BACKGROUND AND PURPOSE: The highly conserved tryptophan (W6.48) in transmembrane domain 6 of GPCRs has been shown to play a central role in forming an active conformation in response to agonist binding. We set out to characterize the effect of this mutation on the efficacy of two agonists at multiple signalling pathways downstream of the adenosine A₃ receptor. EXPERIMENTAL APPROACH: Residue W6.48 in the human...
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