Structural basis for CaVα2δ:gabapentin binding.

Zhou Chen, Abhisek Mondal, Daniel L Minor

Nature structural & molecular biology 2023 Jun

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Gabapentinoid 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 the gabapentin binding selectivity of CaVα2δ-1 and CaVα2δ-2. © 2023. The Author(s), under exclusive licence to Springer Nature America, Inc.

Citation

Zhou Chen, Abhisek Mondal, Daniel L Minor. Structural basis for CaVα2δ:gabapentin binding. Nature structural & molecular biology. 2023 Jun;30(6):735-739