Structural biology and molecular pharmacology of voltage-gated ion channels

J Huang, X Pan, N Yan - Nature Reviews Molecular Cell Biology, 2024 - nature.com
Voltage-gated ion channels (VGICs), including those for Na+, Ca2+ and K+, selectively
permeate ions across the cell membrane in response to changes in membrane potential …

A structural atlas of druggable sites on Nav channels

Z Li, Q Wu, N Yan - Channels, 2024 - Taylor & Francis
Voltage-gated sodium (Nav) channels govern membrane excitability by initiating and
propagating action potentials. Consistent with their physiological significance, dysfunction …

Structural map** of Nav1.7 antagonists

Q Wu, J Huang, X Fan, K Wang, X **, G Huang… - Nature …, 2023 - nature.com
Voltage-gated sodium (Nav) channels are targeted by a number of widely used and
investigational drugs for the treatment of epilepsy, arrhythmia, pain, and other disorders …

Structural basis for high-voltage activation and subtype-specific inhibition of human Nav1.8

X Huang, X **, G Huang, J Huang, T Wu, Z Li… - Proceedings of the …, 2022 - pnas.org
The dorsal root ganglia–localized voltage-gated sodium (Nav) channel Nav1. 8 represents a
promising target for develo** next-generation analgesics. A prominent characteristic of …

Structure of human Cav2.2 channel blocked by the painkiller ziconotide

S Gao, X Yao, N Yan - Nature, 2021 - nature.com
The neuronal-type (N-type) voltage-gated calcium (Cav) channels, which are designated
Cav2. 2, have an important role in the release of neurotransmitters,–. Ziconotide is a Cav2. 2 …

Cryo-EM structure of human voltage-gated sodium channel Nav1.6

X Fan, J Huang, X **, N Yan - Proceedings of the National Academy of …, 2023 - pnas.org
Voltage-gated sodium channel Nav1. 6 plays a crucial role in neuronal firing in the central
nervous system (CNS). Aberrant function of Nav1. 6 may lead to epilepsy and other …

High-resolution structures of human Nav1. 7 reveal gating modulation through α-π helical transition of S6IV

G Huang, D Liu, W Wang, Q Wu, J Chen, X Pan… - Cell Reports, 2022 - cell.com
Na v 1.7 represents a preeminent target for next-generation analgesics for its critical role in
pain sensation. Here we report a 2.2-Å resolution cryo-EM structure of wild-type (WT) Na v …

Unwinding and spiral sliding of S4 and domain rotation of VSD during the electromechanical coupling in Nav1.7

G Huang, Q Wu, Z Li, X **, X Huang, T Wu… - Proceedings of the …, 2022 - pnas.org
Voltage-gated sodium (Nav) channel Nav1. 7 has been targeted for the development of
nonaddictive pain killers. Structures of Nav1. 7 in distinct functional states will offer an …

Structure of human NaV1.6 channel reveals Na+ selectivity and pore blockade by 4,9-anhydro-tetrodotoxin

Y Li, T Yuan, B Huang, F Zhou, C Peng, X Li… - Nature …, 2023 - nature.com
The sodium channel NaV1. 6 is widely expressed in neurons of the central and peripheral
nervous systems, which plays a critical role in regulating neuronal excitability. Dysfunction of …

Dissection of the structure–function relationship of Nav channels

Z Li, Q Wu, G Huang, X **, J Li, X Pan… - Proceedings of the …, 2024 - pnas.org
Voltage-gated sodium channels (Nav) undergo conformational shifts in response to
membrane potential changes, a mechanism known as the electromechanical coupling. To …