Recognition Mechanism of a Novel Gabapentinoid Drug, Mirogabalin, for Recombinant Human α 2 δ1, a Voltage-Gated Calcium Channel Subunit

• Published in: Journal of molecular biology Vol. 435; no. 10; p. 168049
• Main Authors: Kozai, Daisuke, Numoto, Nobutaka, Nishikawa, Kouki, Kamegawa, Akiko, Kawasaki, Shohei, Hiroaki, Yoko, Irie, Katsumasa, Oshima, Atsunori, Hanzawa, Hiroyuki, Shimada, Kousei, Kitano, Yutaka, Fujiyoshi, Yoshinori
• Format: Journal Article
• Language: English
• Published: Netherlands 15.05.2023
• Subjects: Calcium Channels - metabolism; Cryoelectron Microscopy; Gabapentin - chemistry; Gabapentin - pharmacology; Humans; Ligands; αδ; hydrophobic interaction; gabapentinoid; mirogabalin; cryo-EM

Mirogabalin is a novel gabapentinoid drug with a hydrophobic bicyclo substituent on the γ-aminobutyric acid moiety that targets the voltage-gated calcium channel subunit α δ1. Here, to reveal the mirogabalin recognition mechanisms of α δ1, we present structures of recombinant human α δ1 with and wit...