Structural basis for CaVα2δ:gabapentin binding.
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ABSTRACT:
SUBMITTER: Chen Z
PROVIDER: S-EPMC10896480 | biostudies-literature | 2023 Jun
REPOSITORIES: biostudies-literature
Publications
Structural basis for Ca<sub>V</sub>α<sub>2</sub>δ:gabapentin binding.
Chen Zhou Z Mondal Abhisek A Minor Daniel L DL
Nature structural & molecular biology 20230327 6
Gabapentinoid drugs for pain and anxiety act on the Ca<sub>V</sub>α<sub>2</sub>δ-1 and Ca<sub>V</sub>α<sub>2</sub>δ-2 subunits of high-voltage-activated calcium channels (Ca<sub>V</sub>1s and Ca<sub>V</sub>2s). Here we present the cryo-EM structure of the gabapentin-bound brain and cardiac Ca<sub>V</sub>1.2/Ca<sub>V</sub>β<sub>3</sub>/Ca<sub>V</sub>α<sub>2</sub>δ-1 channel. The data reveal a binding pocket in the Ca<sub>V</sub>α<sub>2</sub>δ-1 dCache1 domain that completely encapsulates gabapent ...[more]
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