Structural basis for Ca<sub>V</sub>α<sub>2</sub>δ:gabapentin binding-Reference-Cited by-同舟云学术

Structural basis for Ca_Vα₂δ:gabapentin binding

Published:2022-12-05 Issue: Volume: Page:
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Author:

Chen Zhou,Mondal Abhisek,Minor Daniel L.^ORCID

Abstract

AbstractGabapentinoid drugs for pain and anxiety act on the CaVα2δ-1 and CaVα2δ-2 subunits of high-voltage activated calcium channels (CaV1s and CaV2s). Here, we present the cryo-EM structure of the gabapentin-bound brain and cardiac CaV1.2/CaVβ3/CaVα2δ-1 channel. The data reveal a binding pocket in the CaVα2δ-1 dCache1 domain that completely encapsulates gabapentin and define CaVα2δ isoform sequence variations that explain gabapentin binding selectivity of CaVα2δ-1 and CaVα2δ-2.

Publisher

Cold Spring Harbor Laboratory

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