Article
Allosteric modulators restore orthosteric agonist binding to mutated CB1 receptors.
The Journal of pharmacy and pharmacology - 1 Jan 2020
Dopart Rachel, Kendall Debra A
Abstract excerpt
OBJECTIVES: To determine if diminished orthosteric agonist binding due to mutations in extracellular loops 1 or 2 of the cannabinoid receptor 1 (CB1 ) can be overcome by an allosteric modulator and restore agonist binding. METHODS: Binding assays were performed using a range of concentrations of orthosteric compound, in the presence or absence of a set concentration of the allosteric modulator PSNCBAM-1 to...
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