A paper from the labs of Yan Xu, PhD, and Pei Tang, PhD, in partnership with collaborators at Temple University, University of Pennsylvania, and Shanghai Jiaotong University, was published this month in the journal Proceedings of the National Academy of Sciences (full text link below):
- Xiao J, Bondarenko V, Wang Y, Suma A, Wells MM, Chen Q, Tillman T, Lui Y, Yu B, Dailey WP, Eckenhoff R, Tang P, Carnevale V, Klein ML, Xu Y. Regulation and drug modulation of a voltage-gated sodium channel: Pivotal role of the S4–S5 linker in activation and slow inactivation. PNAS, 2021 Jul 13; 118(28): e2102285118. Doi: 10.1073/pnas.2102285118. PMID: 34260401
In their paper, the authors report critical structural insights into the activation and propofol effects on slow inactivation of voltage-gated sodium channels. Elucidating this new mechanism of general anesthetic action points to a possible direction for conformation-specific drug development to target the gating machinery of voltage-gated ion channels.