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 …

Single-molecule junction: A reliable platform for monitoring molecular physical and chemical processes

X Xie, P Li, Y Xu, L Zhou, Y Yan, L Xie, C Jia, X Guo - ACS nano, 2022 - ACS Publications
Monitoring and manipulating the physical and chemical behavior of single molecules is an
important development direction of molecular electronics that aids in understanding the …

Membrane protein isolation and structure determination in cell-derived membrane vesicles

X Tao, C Zhao, R MacKinnon - Proceedings of the National …, 2023 - National Acad Sciences
Integral membrane protein structure determination traditionally requires extraction from cell
membranes using detergents or polymers. Here, we describe the isolation and structure …

[HTML][HTML] 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 …

Structure of the human voltage-gated sodium channel Nav1.4 in complex with β1

X Pan, Z Li, Q Zhou, H Shen, K Wu, X Huang, J Chen… - Science, 2018 - science.org
INTRODUCTION The nine subtypes of mammalian voltage-gated sodium (Nav) channels,
Nav1. 1 to Nav1. 9, are responsible for the initiation and propagation of action potentials in …

Structures of human Nav1.7 channel in complex with auxiliary subunits and animal toxins

H Shen, D Liu, K Wu, J Lei, N Yan - Science, 2019 - science.org
Voltage-gated sodium channel Nav1. 7 represents a promising target for pain relief. Here we
report the cryo–electron microscopy structures of the human Nav1. 7-β1-β2 complex bound …

Molecular basis for pore blockade of human Na+ channel Nav1.2 by the μ-conotoxin KIIIA

X Pan, Z Li, X Huang, G Huang, S Gao, H Shen, L Liu… - Science, 2019 - science.org
The voltage-gated sodium channel Nav1. 2 is responsible for the initiation and propagation
of action potentials in the central nervous system. We report the cryo–electron microscopy …

[HTML][HTML] Structural basis of Nav1. 7 inhibition by a gating-modifier spider toxin

H Xu, T Li, A Rohou, CP Arthur, F Tzakoniati, E Wong… - Cell, 2019 - cell.com
Voltage-gated sodium (Nav) channels are targets of disease mutations, toxins, and
therapeutic drugs. Despite recent advances, the structural basis of voltage sensing …

Membranes under the magnetic lens: a dive into the diverse world of membrane protein structures using Cryo-EM

SJ Piper, RM Johnson, D Wootten, PM Sexton - Chemical reviews, 2022 - ACS Publications
Membrane proteins are highly diverse in both structure and function and can, therefore,
present different challenges for structure determination. They are biologically important for …

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 Jin, X Huang… - Proceedings of the …, 2022 - National Acad Sciences
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 …