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 …

Lipid nanodiscs for high-resolution NMR studies of membrane proteins

U Günsel, F Hagn - Chemical Reviews, 2021 - ACS Publications
Membrane proteins (MPs) play essential roles in numerous cellular processes. Because
around 70% of the currently marketed drugs target MPs, a detailed understanding of their …

Structural mapping of Nav1.7 antagonists

Q Wu, J Huang, X Fan, K Wang, X Jin, 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 …

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 …

Structural Basis of the Modulation of the Voltage‐Gated Calcium Ion Channel Cav1.1 by Dihydropyridine Compounds**

S Gao, N Yan - Angewandte Chemie, 2021 - Wiley Online Library
Dihydropyridines (DHP), the most commonly used antihypertensives, function by inhibiting
the L‐type voltage‐gated Ca2+ (Cav) channels. DHP compounds exhibit chirality‐specific …

[HTML][HTML] Membrane lipids and transporter function

B Stieger, J Steiger, KP Locher - … et Biophysica Acta (BBA)-Molecular Basis …, 2021 - Elsevier
Transport proteins are essential for cells in allowing the exchange of substances between
cells and their environment across the lipid bilayer forming a tight barrier. Membrane lipids …

Structural pharmacology of voltage-gated sodium channels

S Noreng, T Li, J Payandeh - Journal of Molecular Biology, 2021 - Elsevier
Voltage-gated sodium (Na V) channels initiate and propagate action potentials in excitable
tissues to mediate key physiological processes including heart contraction and nervous …

Structural basis for high-affinity trapping of the NaV1. 7 channel in its resting state by tarantula toxin

G Wisedchaisri, L Tonggu, TMG El-Din, E McCord… - Molecular cell, 2021 - cell.com
Voltage-gated sodium channels initiate electrical signals and are frequently targeted by
deadly gating-modifier neurotoxins, including tarantula toxins, which trap the voltage sensor …

The chemistry of electrical signaling in sodium channels from bacteria and beyond

WA Catterall, TMG El-Din, G Wisedchaisri - Cell Chemical Biology, 2024 - cell.com
Electrical signaling is essential for all fast processes in biology, but its molecular
mechanisms have been uncertain. This review article focuses on studies of bacterial sodium …

Amphipathic environments for determining the structure of membrane proteins by single-particle electron cryo-microscopy

C Le Bon, B Michon, JL Popot… - Quarterly Reviews of …, 2021 - cambridge.org
Over the past decade, the structural biology of membrane proteins (MPs) has taken a new
turn thanks to epoch-making technical progress in single-particle electron cryo-microscopy …