4.8 Article

Structure of human Cav2.2 channel blocked by the painkiller ziconotide

Related references

Note: Only part of the references are listed.
Article Chemistry, Multidisciplinary

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

Shuai Gao et al.

Summary: This study reports the structures of Ca(v)1.1 bound with different drugs, revealing the molecular basis for their effects. The structures show that amlodipine and nifedipine have different impacts on Ca(v)1.1, while the two enantiomers of Bay K8644 as agonists are insufficient to maintain the activated state of the channel.

ANGEWANDTE CHEMIE-INTERNATIONAL EDITION (2021)

Article Multidisciplinary Sciences

Structural basis for voltage-sensor trapping of the cardiac sodium channel by a deathstalker scorpion toxin

Li Zhou et al.

Summary: The alpha-toxin LqhIII from the deathstalker scorpion inhibits fast inactivation of cardiac Na(V)1.5 channels. The cryo-EM structure of LqhIII bound to Na(V)1.5 shows that it traps the gating charges of the S4 segment in a unique intermediate-activated state, explaining why LqhIII slows inactivation of Na-V channels but does not open them.

NATURE COMMUNICATIONS (2021)

Article Chemistry, Multidisciplinary

Structural Basis for Pore Blockade of the Human Cardiac Sodium Channel Nav1.5 by the Antiarrhythmic Drug Quinidine**

Zhangqiang Li et al.

Summary: The study presents the cryo-EM structure of human Na(v)1.5 channel bound to the antiarrhythmic drug quinidine, showing how quinidine blocks the pore and induces rotation of a Tyr residue for its mechanism of action. Comparison with a truncated rat Na(v)1.5 in the presence of another antiarrhythmic drug, flecainide, reveals distinct binding poses within the pore domain for the two drugs. This work, along with previous studies, sheds light on the molecular basis of action for class I antiarrhythmic drugs.

ANGEWANDTE CHEMIE-INTERNATIONAL EDITION (2021)

Article Multidisciplinary Sciences

Structure of human Nav1.5 reveals the fast inactivation-related segments as a mutational hotspot for the long QT syndrome

Zhangqiang Li et al.

Summary: Na(v)1.5 is the primary voltage-gated Na+ channel in the heart, mutations of which are associated with various cardiac disorders. The study reveals the structural distribution of mutations associated with LQT3 and BrS, with a focus on a mutational hotspot involving the fast inactivation segments and proposing a door wedge model for fast inactivation. This structural analysis establishes a structure-function relationship for understanding the mechanistic of Na(v)1.5 channelopathies.

PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA (2021)

Article Multidisciplinary Sciences

Comparative structural analysis of human Nav1.1 and Nav1.5 reveals mutational hotspots for sodium channelopathies

Xiaojing Pan et al.

Summary: The high-resolution structures of human Na(v)1.1 and Na(v)1.5 channels associated with epilepsy and cardiac disorders were reported. Comparative structural analysis revealed common clusters of disease mutations in both channels. These mutations may affect the structural integrity and electromechanical coupling of the channels.

PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA (2021)

Article Biochemistry & Molecular Biology

Structure of the Cardiac Sodium Channel

Daohua Jiang et al.

Article Biochemistry & Molecular Biology

Structural Basis of Human KCNQ1 Modulation and Gating

Ji Sun et al.

Article Multidisciplinary Sciences

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

Huaizong Shen et al.

SCIENCE (2019)

Article Multidisciplinary Sciences

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

Xiaojing Pan et al.

SCIENCE (2019)

Article Multidisciplinary Sciences

Structural basis of α-scorpion toxin action on Nav channels

Thomas Clairfeuille et al.

SCIENCE (2019)

Article Biochemistry & Molecular Biology

Molecular Basis for Ligand Modulation of a Mammalian Voltage-Gated Ca2+ Channel

Yanyu Zhao et al.

Article Multidisciplinary Sciences

Cryo-EM structures of apo and antagonist-bound human Cav3.1

Yanyu Zhao et al.

NATURE (2019)

Article Biochemistry & Molecular Biology

SWISS-MODEL: homology modelling of protein structures and complexes

Andrew Waterhouse et al.

NUCLEIC ACIDS RESEARCH (2018)

Article Multidisciplinary Sciences

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

Xiaojing Pan et al.

SCIENCE (2018)

Letter Biochemical Research Methods

MotionCor2: anisotropic correction of beam-induced motion for improved cryo-electron microscopy

Shawn Q. Zheng et al.

NATURE METHODS (2017)

Article Multidisciplinary Sciences

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

Huaizong Shen et al.

SCIENCE (2017)

Article Biochemistry & Molecular Biology

Structure of the Nav1.4-β1 Complex from Electric Eel

Zhen Yan et al.

Article Biochemistry & Molecular Biology

Gctf: Real-time CTF determination and correction

Kai Zhang

JOURNAL OF STRUCTURAL BIOLOGY (2016)

Article Multidisciplinary Sciences

Structure of the voltage-gated calcium channel Cav1.1 at 3.6 Å resolution

Jianping Wu et al.

NATURE (2016)

Article Multidisciplinary Sciences

Structure of the voltage-gated calcium channel Cav1.1 complex

Jianping Wu et al.

SCIENCE (2015)

Review Pharmacology & Pharmacy

Dual regulation of voltage-sensitive ion channels by PIP2

Aldo A. Rodriguez-Menchaca et al.

FRONTIERS IN PHARMACOLOGY (2012)

Article Biochemical Research Methods

Features and development of Coot

P. Emsley et al.

ACTA CRYSTALLOGRAPHICA SECTION D-BIOLOGICAL CRYSTALLOGRAPHY (2010)

Article Biochemical Research Methods

PHENIX: a comprehensive Python-based system for macromolecular structure solution

Paul D. Adams et al.

ACTA CRYSTALLOGRAPHICA SECTION D-STRUCTURAL BIOLOGY (2010)

Article Medicine, General & Internal

Ziconotide for treatment of severe chronic pain

Achim Schmidtko et al.

LANCET (2010)

Review Pharmacology & Pharmacy

Targeting N-type and T-type calcium channels for the treatment of pain

JG McGivern

DRUG DISCOVERY TODAY (2006)

Article Biochemistry & Molecular Biology

Automated electron microscope tomography using robust prediction of specimen movements

DN Mastronarde

JOURNAL OF STRUCTURAL BIOLOGY (2005)

Article Biochemistry & Molecular Biology

The α2δ auxiliary subunit reduces affinity of ω-conotoxins for recombinant N-type (Cav2.2) calcium channels

J Mould et al.

JOURNAL OF BIOLOGICAL CHEMISTRY (2004)

Review Biochemistry & Molecular Biology

Ziconotide: Neuronal calcium channel blocker for treating severe chronic pain

GP Miljanich

CURRENT MEDICINAL CHEMISTRY (2004)

Article Chemistry, Multidisciplinary

UCSF chimera - A visualization system for exploratory research and analysis

EF Pettersen et al.

JOURNAL OF COMPUTATIONAL CHEMISTRY (2004)

Article Biochemistry & Molecular Biology

Optimal determination of particle orientation, absolute hand, and contrast loss in single-particle electron cryomicroscopy

PB Rosenthal et al.

JOURNAL OF MOLECULAR BIOLOGY (2003)

Article Multidisciplinary Sciences

Dual regulation of voltage-gated calcium channels by PtdIns(4,5)P2

L Wu et al.

NATURE (2002)

Article Biochemistry & Molecular Biology

Suppression of inflammatory and neuropathic pain symptoms in mice lacking the N-type Ca2+ channel

H Saegusa et al.

EMBO JOURNAL (2001)