[HTML][HTML] Activation of the β2-adrenergic receptor involves disruption of an ionic lock between the cytoplasmic ends of transmembrane segments 3 and 6
JA Ballesteros, AD Jensen, G Liapakis… - Journal of Biological …, 2001 - ASBMB
The movements of transmembrane segments (TMs) 3 and 6 at the cytoplasmic side of the
membrane play an important role in the activation of G-protein-coupled receptors. Here we
provide evidence for the existence of an ionic lock that constrains the relative mobility of the
cytoplasmic ends of TM3 and TM6 in the inactive state of the β 2-adrenergic receptor. We
propose that the highly conserved Arg-131 3.50 at the cytoplasmic end of TM3 interacts both
with the adjacent Asp-130 3.49 and with Glu-268 6.30 at the cytoplasmic end of TM6. Such a …
membrane play an important role in the activation of G-protein-coupled receptors. Here we
provide evidence for the existence of an ionic lock that constrains the relative mobility of the
cytoplasmic ends of TM3 and TM6 in the inactive state of the β 2-adrenergic receptor. We
propose that the highly conserved Arg-131 3.50 at the cytoplasmic end of TM3 interacts both
with the adjacent Asp-130 3.49 and with Glu-268 6.30 at the cytoplasmic end of TM6. Such a …