Biomolecules & Therapeutics : eISSN 2005-4483 / pISSN 1976-9148

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Fig. 3. Effects of increasing the number of hydrophobic residues in helix 8 of D1R. (A) Database analysis of the number of hydrophobic residues. Hydrophobic residues between 8.50 and 8.58 were counted for the class A GPCRs D1R and D2R. Conserved hydrophobic residues at positions 8.50, 8.54, and 8.58 were not counted. (B) Mutant constructs in which D1R residues 8.52 and 8.56/8.59 were changed to hydrophobic residues. (C) Subcellular localization of WT and helix 8 mutant constructs of D1R were visualized by immunofluorescence using confocal microscopy. Upper panels show non-permeabilized cells, and lower panels show permeabilized cells with blue presenting nucleus (DAPI staining) and red presenting receptors. Scale bars represent 10 μm. (D) Dopamine-induced Gq and Gs signaling in WT D1R and D1R-K8.56A measured by luciferase reporter gene assay. (E) Effect of mutation on cAMP accumulation induced by 100 nM dopamine measured as described in . Error bars represent STDEV.
Biomolecules & Therapeutics 2019;27:514~521 https://doi.org/10.4062/biomolther.2019.026
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