Structural basis for CaVα2δ:gabapentin binding

Autor:	Zhou Chen, Abhisek Mondal, Daniel L. Minor
Rok vydání:	2022
Popis:	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 gabapentin binding selectivity of CaVα2δ-1 and CaVα2δ-2.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_________::7a93d9e27a3c79bb1a9f047afa274cb6 https://doi.org/10.1101/2022.12.05.519047 Zobrazit plný text záznamu