Fig. 4: Activation of α2A-AR. | Experimental & Molecular Medicine

Fig. 4: Activation of α2A-AR.

From: Distinct binding conformations of epinephrine with α- and β-adrenergic receptors

Fig. 4

ac Differential images of the inactive state of α2A-AR (gray; PDB 6KUX) and the active state of α2A-AR in complex with Gi (this work). d The movements of TM6 and TM7 during α2A-AR activation are shown. e Conformational changes in the CWxP motif during α2A-AR activation are shown. f Conformational changes in the PIF motif during α2A-AR activation are shown. g Y441 within the NPxxY motif packs against L139 and I142 in the active state of α2A-AR. h The ionic lock between R146 (within the DRY motif) and E384 located at the cytoplasmic end of TM6 is disrupted in the active state of α2A-AR. The ionic bonding between R146 and E384 is indicated by a dashed black line.

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