Article
A cannabinoid receptor 1 mutation proximal to the DRY motif results in constitutive activity and reveals intramolecular interactions involved in receptor activation.
Brain research - 7 Sept 2006
D'Antona Aaron M, Ahn Kwang H, Wang Lei, Mierke Dale F, Lucas-Lenard Jean, Kendall Debra A
Abstract excerpt
Activation of a G-protein-coupled receptor involves changes in specific microdomain interactions within the transmembrane region of the receptor. Here, we have focused on the role of L207, proximal to the DRY motif of the human cannabinoid receptor 1 in the interconversion of the receptor resting and active states. Ligand binding analysis of the mutant receptor L207A revealed an enhanced affinity for agonists...
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