Cryo-EM in drug discovery: achievements, limitations and prospects

JP Renaud, A Chari, C Ciferri, W Liu… - Nature reviews Drug …, 2018 - nature.com
Cryo-electron microscopy (cryo-EM) of non-crystalline single particles is a biophysical
technique that can be used to determine the structure of biological macromolecules and …

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 …

Structure of a eukaryotic voltage-gated sodium channel at near-atomic resolution

H Shen, Q Zhou, X Pan, Z Li, J Wu, N Yan - Science, 2017 - science.org
INTRODUCTION Voltage-gated sodium (Nav) channels are responsible for the generation
and propagation of action potentials in excitable cells. They undergo voltage-dependent …

Architecture and autoinhibitory mechanism of the plasma membrane Na+/H+ antiporter SOS1 in Arabidopsis

Y Wang, C Pan, Q Chen, Q Xie, Y Gao, L He… - Nature …, 2023 - nature.com
Abstract Salt-overly-sensitive 1 (SOS1) is a unique electroneutral Na+/H+ antiporter at the
plasma membrane of higher plants and plays a central role in resisting salt stress. SOS1 is …

[HTML][HTML] Cryo-EM structure of a KCNQ1/CaM complex reveals insights into congenital long QT syndrome

J Sun, R MacKinnon - Cell, 2017 - cell.com
KCNQ1 is the pore-forming subunit of cardiac slow-delayed rectifier potassium (I Ks)
channels. Mutations in the kcnq1 gene are the leading cause of congenital long QT …

Transcriptional activation and phosphorylation of OsCNGC9 confer enhanced chilling tolerance in rice

J Wang, Y Ren, X Liu, S Luo, X Zhang, X Liu, Q Lin… - Molecular Plant, 2021 - cell.com
Low temperature is a major environmental factor that limits plant growth and productivity.
Although transient elevation of cytoplasmic calcium has long been recognized as a critical …

Cryo-EM and X-ray structures of TRPV4 reveal insight into ion permeation and gating mechanisms

Z Deng, N Paknejad, G Maksaev… - Nature structural & …, 2018 - nature.com
The transient receptor potential (TRP) channel TRPV4 participates in multiple biological
processes, and numerous TRPV4 mutations underlie several distinct and devastating …

The membrane electric field regulates the PIP2-binding site to gate the KCNQ1 channel

VS Mandala, R MacKinnon - Proceedings of the National …, 2023 - National Acad Sciences
Voltage-dependent ion channels underlie the propagation of action potentials and other
forms of electrical activity in cells. In these proteins, voltage sensor domains (VSDs) regulate …

Activation mechanism of a human SK-calmodulin channel complex elucidated by cryo-EM structures

CH Lee, R MacKinnon - Science, 2018 - science.org
Small-conductance Ca2+-activated K+ (SK) channels mediate neuron excitability and are
associated with synaptic transmission and plasticity. They also regulate immune responses …

Voltage-sensor movements in the Eag Kv channel under an applied electric field

VS Mandala, R MacKinnon - Proceedings of the National …, 2022 - National Acad Sciences
Voltage-dependent ion channels regulate the opening of their pores by sensing the
membrane voltage. This process underlies the propagation of action potentials and other …