Trends in peptide drug discovery
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 …
reached the market for a wide range of diseases, including diabetes, cancer, osteoporosis …
Structural biology and molecular pharmacology of voltage-gated ion channels
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 …
permeate ions across the cell membrane in response to changes in membrane potential …
Structural map** of Nav1.7 antagonists
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 …
investigational drugs for the treatment of epilepsy, arrhythmia, pain, and other disorders …
Structure of human Cav2.2 channel blocked by the painkiller ziconotide
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 …
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
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 …
promising target for develo** next-generation analgesics. A prominent characteristic of …
RCSB Protein Data Bank: Enabling biomedical research and drug discovery
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 …
three‐dimensional (3D) structures of protein targets important for discovery of new drugs …
[HTML][HTML] Structure of the cardiac sodium channel
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 …
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
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 …
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
The L-type voltage-gated Ca 2+(Ca v) channels are modulated by various compounds
exemplified by 1, 4-dihydropyridines (DHP), benzothiazepines (BTZ), and …
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 …
signaling proteins that initiate action potentials, neurotransmission, excitation-contraction …