The alpha2delta ligand gabapentin inhibits the Rab11-dependent recycling of the calcium channel subunit alpha2delta-2.

ABSTRACT: The α2δ subunits of voltage-gated calcium channels are important modulatory subunits that enhance calcium currents and may also have other roles in synaptogenesis. The antiepileptic and antiallodynic drug gabapentin (GBP) binds to the α2δ-1 and α2δ-2 isoforms of this protein, and its binding may disrupt the binding of an endogenous ligand, required for their correct function. We have shown previously that GBP produces a chronic inhibitory effect on calcium currents by causing a reduction in the total number of α2δ and α1 subunits at the cell surface. This action of GBP is likely to be attributable to a disruption of the trafficking of α2δ subunits, either to or from the plasma membrane. We studied the effect of GBP on the internalization of, and insertion into the plasma membrane of α2δ-2

SUBMITTER: Tran-Van-Minh A 

PROVIDER: S-EPMC6633565 | biostudies-literature | 2010 Sep

REPOSITORIES: biostudies-literature