Trends in peptide drug discovery

M Muttenthaler, GF King, DJ Adams… - Nature reviews Drug …, 2021 - nature.com
Since the introduction of insulin almost a century ago, more than 80 peptide drugs have
reached the market for a wide range of diseases, including diabetes, cancer, osteoporosis …

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 …

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 …

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 …

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

X Huang, X **, G Huang, J Huang… - Proceedings of the …, 2022 - National Acad Sciences
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 …

RCSB Protein Data Bank: Enabling biomedical research and drug discovery

DS Goodsell, C Zardecki, L Di Costanzo… - Protein …, 2020 - Wiley Online Library
Analyses of publicly available structural data reveal interesting insights into the impact of the
three‐dimensional (3D) structures of protein targets important for discovery of new drugs …

[HTML][HTML] Structure of the cardiac sodium channel

D Jiang, H Shi, L Tonggu, TMG El-Din, MJ Lenaeus… - Cell, 2020 - cell.com
Voltage-gated sodium channel Na v 1.5 generates cardiac action potentials and initiates the
heartbeat. Here, we report structures of Na V 1.5 at 3.2–3.5 Å resolution. Na V 1.5 is …

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

X Fan, J Huang, X **, N Yan - Proceedings of the National …, 2023 - National Acad Sciences
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 …

Molecular basis for ligand modulation of a mammalian voltage-gated Ca2+ channel

Y Zhao, G Huang, J Wu, Q Wu, S Gao, Z Yan, J Lei… - Cell, 2019 - cell.com
The L-type voltage-gated Ca 2+(Ca v) channels are modulated by various compounds
exemplified by 1, 4-dihydropyridines (DHP), benzothiazepines (BTZ), and …

Structure and pharmacology of voltage-gated sodium and calcium channels

WA Catterall, MJ Lenaeus… - Annual review of …, 2020 - annualreviews.org
Voltage-gated sodium and calcium channels are evolutionarily related transmembrane
signaling proteins that initiate action potentials, neurotransmission, excitation-contraction …