Ivermectin and its target molecules: shared and unique modulation mechanisms of ion channels and receptors by ivermectin

Ivermectin activates GIRK channels in a PIP2 -dependent, Gβγ -independent manner and an amino acid residue at the slide helix governs the activation

(2017) I-Shan Chen et al.   JOURNAL OF PHYSIOLOGY-LONDON

Altenusin, a Nonsteroidal Microbial Metabolite, Attenuates Nonalcoholic Fatty Liver Disease by Activating the Farnesoid X Receptor

(2017) Zhihui Zheng et al.   MOLECULAR PHARMACOLOGY

Crystal Structures of Human GlyRα3 Bound to Ivermectin

(2017) Xin Huang et al.   STRUCTURE

A Splendid Gift from the Earth: The Origins and Impact of the Avermectins (Nobel Lecture)

(2016) Satoshi Ōmura   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Role of purinergic P2X4 receptors in regulating striatal dopamine homeostasis and dependent behaviors

(2016) Sheraz Khoja et al.   JOURNAL OF NEUROCHEMISTRY

X-ray structure of the human α4β2 nicotinic receptor

(2016) Claudio L. Morales-Perez et al.   NATURE

Ivermectin modulation of pH-sensitive chloride channels in the silkworm larvae of Bombyx mori

(2016) Yuri Nakatani et al.   PESTICIDE BIOCHEMISTRY AND PHYSIOLOGY

Novel cell-free high-throughput screening method for pharmacological tools targeting K+channels

(2016) Zhenwei Su et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Involvement of Purinergic P2X4 Receptors in Alcohol Intake of High-Alcohol-Drinking (HAD) Rats

(2015) Kelle M. Franklin et al.   ALCOHOLISM-CLINICAL AND EXPERIMENTAL RESEARCH

Glycine receptor mechanism elucidated by electron cryo-microscopy

(2015) Juan Du et al.   NATURE

Interactions of L-3,5,3'-Triiodothyronine, Allopregnanolone, and Ivermectin with the GABAA Receptor: Evidence for Overlapping Intersubunit Binding Modes

(2015) Thomas Westergard et al.   PLoS One

Roles of the lateral fenestration residues of the P2X4 receptor that contribute to the channel function and the deactivation effect of ivermectin

(2015) Chao Gao et al.   Purinergic Signalling

Selective targeting of nuclear receptor FXR by avermectin analogues with therapeutic effects on nonalcoholic fatty liver disease

(2015) Lihua Jin et al.   Scientific Reports

Modulation of P2X4/P2X7/Pannexin-1 sensitivity to extracellular ATP via Ivermectin induces a non-apoptotic and inflammatory form of cancer cell death

(2015) Dobrin Draganov et al.   Scientific Reports

Functional characterization of ivermectin binding sites in α1β2γ2L GABA(A) receptors

(2015) Argel Estrada-Mondragon et al.   Frontiers in Molecular Neuroscience

Bile acid nuclear receptor FXR and digestive system diseases

(2015) Lili Ding et al.   Acta Pharmaceutica Sinica B

Assessment of temperature-induced hERG channel blockade variation by drugs

(2014) Rahul R. Kauthale et al.   JOURNAL OF APPLIED TOXICOLOGY

Crystal structure of a human GABAA receptor

(2014) Paul S. Miller et al.   NATURE

X-ray structures of GluCl in apo states reveal a gating mechanism of Cys-loop receptors

(2014) Thorsten Althoff et al.   NATURE

P2X4 receptors (P2X4Rs) represent a novel target for the development of drugs to prevent and/or treat alcohol use disorders

(2014) Kelle M. Franklin et al.   Frontiers in Neuroscience

X-ray structure of the mammalian GIRK2–βγ G-protein complex

(2013) Matthew R. Whorton et al.   NATURE

Multiple Roles of the Extracellular Vestibule Amino Acid Residues in the Function of the Rat P2X4 Receptor

(2013) Milos B. Rokic et al.   PLoS One

PNAS Plus: From the Cover: A gating mechanism of pentameric ligand-gated ion channels

(2013) N. Calimet et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Tryptophan 46 is a site for ethanol and ivermectin action in P2X4 receptors

(2013) Maya Popova et al.   Purinergic Signalling

The antiparasitic drug ivermectin is a novel FXR ligand that regulates metabolism

(2013) Lihua Jin et al.   Nature Communications

Positive allosteric modulation by ivermectin of human but not murine P2X7 receptors

(2012) W Nörenberg et al.   BRITISH JOURNAL OF PHARMACOLOGY

Pharmacological insights into the role of P2X4 receptors in behavioural regulation: lessons from ivermectin

(2012) Marco Bortolato et al.   INTERNATIONAL JOURNAL OF NEUROPSYCHOPHARMACOLOGY

Allosteric Modulation of Ca2+flux in Ligand-gated Cation Channel (P2X4) by Actions on Lateral Portals

(2012) Damien S. K. Samways et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Structure, Function, and Modulation of GABAAReceptors

(2012) Erwin Sigel et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Molecular mechanism of ATP binding and ion channel activation in P2X receptors

(2012) Motoyuki Hattori et al.   NATURE

Natural Variation in a Chloride Channel Subunit Confers Avermectin Resistance in C. elegans

(2012) R. Ghosh et al.   SCIENCE

Ivermectin binding sites in human and invertebrate Cys-loop receptors

(2012) Timothy Lynagh et al.   TRENDS IN PHARMACOLOGICAL SCIENCES

Crystal Structure of the Mammalian GIRK2 K+ Channel and Gating Regulation by G Proteins, PIP2, and Sodium

(2011) Matthew R. Whorton et al.   CELL

Principles of activation and permeation in an anion-selective Cys-loop receptor

(2011) Ryan E. Hibbs et al.   NATURE

A glycine residue essential for high ivermectin sensitivity in Cys-loop ion channel receptors

(2010) Timothy Lynagh et al.   INTERNATIONAL JOURNAL FOR PARASITOLOGY

An Improved Ivermectin-activated Chloride Channel Receptor for Inhibiting Electrical Activity in Defined Neuronal Populations

(2010) Timothy Lynagh et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Nicotinic Acetylcholine Receptor Transmembrane Mutations Convert Ivermectin from a Positive to a Negative Allosteric Modulator

(2010) T. Collins et al.   MOLECULAR PHARMACOLOGY

Inwardly Rectifying Potassium Channels: Their Structure, Function, and Physiological Roles

(2010) Hiroshi Hibino et al.   PHYSIOLOGICAL REVIEWS

Comparative pharmacology and computational modelling yield insights into allosteric modulation of human α7 nicotinic acetylcholine receptors

(2009) David B. Sattelle et al.   BIOCHEMICAL PHARMACOLOGY

FXR agonist activity of conformationally constrained analogs of GW 4064

(2009) Adwoa Akwabi-Ameyaw et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

An Ivermectin-Sensitive Glutamate-Gated Chloride Channel from the Parasitic Nematode Haemonchus contortus

(2009) S. McCavera et al.   MOLECULAR PHARMACOLOGY

Crystal structure of the ATP-gated P2X4 ion channel in the closed state

(2009) Toshimitsu Kawate et al.   NATURE

FXR: a metabolic regulator and cell protector

(2008) Yan-Dong Wang et al.   CELL RESEARCH

Identification of P2X4 receptor transmembrane residues contributing to channel gating and interaction with ivermectin

(2008) Irena Jelínkova et al.   PFLUGERS ARCHIV-EUROPEAN JOURNAL OF PHYSIOLOGY