Neuronal Nicotinic Acetylcholine Receptor Modulators from Cone Snails

A novel α-conopeptide Eu1.6 inhibits N-type (CaV2.2) calcium channels and exhibits potent analgesic activity

(2018) Zhuguo Liu et al.   Scientific Reports

α-Conotoxin [S9A]TxID Potently Discriminates between α3β4 and α6/α3β4 Nicotinic Acetylcholine Receptors

(2017) Yong Wu et al.   JOURNAL OF MEDICINAL CHEMISTRY

A Novel Lid-Covering Peptide Inhibitor of Nicotinic Acetylcholine Receptors Derived from αD-Conotoxin GeXXA

(2017) Longjin Yang et al.   Marine Drugs

Nicotinic acetylcholine receptor inhibitors derived from snake and snail venoms

(2017) Sébastien Dutertre et al.   NEUROPHARMACOLOGY

α-Conotoxins to explore the molecular, physiological and pathophysiological functions of neuronal nicotinic acetylcholine receptors

(2017) Julien Giribaldi et al.   NEUROSCIENCE LETTERS

The crystal structure of Ac-AChBP in complex with α-conotoxin LvIA reveals the mechanism of its selectivity towards different nAChR subtypes

(2017) Manyu Xu et al.   Protein & Cell

Structural mechanisms for α-conotoxin activity at the human α3β4 nicotinic acetylcholine receptor

(2017) Nikita Abraham et al.   Scientific Reports

Structural Studies of Nicotinic Acetylcholine Receptors: Using Acetylcholine-Binding Protein as a Structural Surrogate

(2016) Azadeh Shahsavar et al.   BASIC & CLINICAL PHARMACOLOGY & TOXICOLOGY

Molecular simulation study of the unbinding of α-conotoxin [ϒ4E]GID at the α7 and α4β2 neuronal nicotinic acetylcholine receptors

(2016) Abishek Suresh et al.   JOURNAL OF MOLECULAR GRAPHICS & MODELLING

Residues Responsible for the Selectivity of α-Conotoxins for Ac-AChBP or nAChRs

(2016) Bo Lin et al.   Marine Drugs

X-ray structure of the human α4β2 nicotinic receptor

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

Crystal structure of a human neuronal nAChR extracellular domain in pentameric assembly: Ligand-bound α2 homopentamer

(2016) Nikolaos Kouvatsos et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

From crystal structure of α-conotoxin GIC in complex with Ac-AChBP to molecular determinants of its high selectivity for α3β2 nAChR

(2016) Bo Lin et al.   Scientific Reports

αS-conotoxin GVIIIB potently and selectively blocks α9α10 nicotinic acetylcholine receptors

(2015) Sean B. Christensen et al.   BIOCHEMICAL PHARMACOLOGY

α-conotoxin MrIC is a biased agonist at α7 nicotinic acetylcholine receptors

(2015) Alexander Mueller et al.   BIOCHEMICAL PHARMACOLOGY

The use of α-conotoxin ImI to actualize the targeted delivery of paclitaxel micelles to α7 nAChR-overexpressing breast cancer

(2015) Dong Mei et al.   BIOMATERIALS

Cyclic alpha-conotoxin peptidomimetic chimeras as potent GLP-1R agonists

(2015) Joakim E. Swedberg et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Key Residues in the Nicotinic Acetylcholine Receptor β2 Subunit Contribute to α-Conotoxin LvIA Binding

(2015) Dongting Zhangsun et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

α-Conotoxin Dendrimers Have Enhanced Potency and Selectivity for Homomeric Nicotinic Acetylcholine Receptors

(2015) Jingjing Wan et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Optimized deep-targeted proteotranscriptomic profiling reveals unexploredConustoxin diversity and novel cysteine frameworks

(2015) Vincent Lavergne et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Cloning, synthesis, and characterization of αO-conotoxin GeXIVA, a potent α9α10 nicotinic acetylcholine receptor antagonist

(2015) Sulan Luo et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Marine Macrocyclic Imines, Pinnatoxins A and G: Structural Determinants and Functional Properties to Distinguish Neuronal α7 from Muscle α12βγδ nAChRs

(2015) Yves Bourne et al.   STRUCTURE

Looking below the surface of nicotinic acetylcholine receptors

(2015) Clare Stokes et al.   TRENDS IN PHARMACOLOGICAL SCIENCES

Conotoxin αD-GeXXA utilizes a novel strategy to antagonize nicotinic acetylcholine receptors

(2015) Shaoqiong Xu et al.   Scientific Reports

Natural Compounds Interacting with Nicotinic Acetylcholine Receptors: From Low-Molecular Weight Ones to Peptides and Proteins

(2015) Denis Kudryavtsev et al.   Toxins

Characterization of a T-superfamily conotoxin TxVC from Conus textile that selectively targets neuronal nAChR subtypes

(2014) Shuo Wang et al.   BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS

Merging old and new perspectives on nicotinic acetylcholine receptors

(2014) Roger L. Papke   BIOCHEMICAL PHARMACOLOGY

Discovery, Synthesis, and Structure–Activity Relationships of Conotoxins

(2014) Kalyana B. Akondi et al.   CHEMICAL REVIEWS

A novel α4/7-conotoxin LvIA from Conus lividus that selectively blocks α3β2 vs. α6/α3β2β3 nicotinic acetylcholine receptors

(2014) Sulan Luo et al.   FASEB JOURNAL

Cone snail venomics: from novel biology to novel therapeutics

(2014) Jutty Rajan Prashanth et al.   Future Medicinal Chemistry

Alanine Scan of α-Conotoxin RegIIA Reveals a Selective α3β4 Nicotinic Acetylcholine Receptor Antagonist

(2014) Shiva N. Kompella et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Discovery of a Potent and Selective α3β4 Nicotinic Acetylcholine Receptor Antagonist from an α-Conotoxin Synthetic Combinatorial Library

(2014) Yi-Pin Chang et al.   JOURNAL OF MEDICINAL CHEMISTRY

Conotoxins Targeting Nicotinic Acetylcholine Receptors: An Overview

(2014) Eline Lebbe et al.   Marine Drugs

Recent progress in neuroactive marine natural products

(2014) Ryuichi Sakai et al.   NATURAL PRODUCT REPORTS

Crystal structures of free and antagonist-bound states of human α9 nicotinic receptor extracellular domain

(2014) Marios Zouridakis et al.   NATURE STRUCTURAL & MOLECULAR BIOLOGY

Discovery of a new subclass of α-conotoxins in the venom of Conus australis

(2014) Eline K.M. Lebbe et al.   TOXICON

Intraspecific variations in Conus geographus defence-evoked venom and estimation of the human lethal dose

(2014) Sébastien Dutertre et al.   TOXICON

Evolution of separate predation- and defence-evoked venoms in carnivorous cone snails

(2014) Sébastien Dutertre et al.   Nature Communications

Isolation and characterization of α-conotoxin LsIA with potent activity at nicotinic acetylcholine receptors

(2013) Marco C. Inserra et al.   BIOCHEMICAL PHARMACOLOGY

MrIC, a Novel α-Conotoxin Agonist in the Presence of PNU at Endogenous α7 Nicotinic Acetylcholine Receptors

(2013) Ai-Hua Jin et al.   BIOCHEMISTRY

Design and synthesis of α-conotoxin GID analogues as selective α4β2 nicotinic acetylcholine receptor antagonists

(2013) Jayati Banerjee et al.   BIOPOLYMERS

?7 Nicotinic Acetylcholine Receptors: A Therapeutic Target in the Structure Era

(2013) Antoine Taly et al.   CURRENT DRUG TARGETS

Characterization of a Novel α-Conotoxin TxID from Conus textile That Potently Blocks Rat α3β4 Nicotinic Acetylcholine Receptors

(2013) Sulan Luo et al.   JOURNAL OF MEDICINAL CHEMISTRY

Transcriptomic Messiness in the Venom Duct ofConus milesContributes to Conotoxin Diversity

(2013) Ai-hua Jin et al.   MOLECULAR & CELLULAR PROTEOMICS

A Novel Inhibitor of α9α10 Nicotinic Acetylcholine Receptors from Conus vexillum Delineates a New Conotoxin Superfamily

(2013) Sulan Luo et al.   PLoS One

Nicotinic acetylcholine receptors mediate lung cancer growth

(2013) Ma. Reina Improgo et al.   Frontiers in Physiology

A novel µ-conopeptide, CnIIIC, exerts potent and preferential inhibition of NaV1.2/1.4 channels and blocks neuronal nicotinic acetylcholine receptors

(2012) Philippe Favreau et al.   BRITISH JOURNAL OF PHARMACOLOGY

The Nicotinic Acetylcholine Receptor: The Founding Father of the Pentameric Ligand-gated Ion Channel Superfamily

(2012) Jean-Pierre Changeux   JOURNAL OF BIOLOGICAL CHEMISTRY

Molecular basis for the differential sensitivity of rat and human α9α10 nAChRs to α-conotoxin RgIA

(2012) Layla Azam et al.   JOURNAL OF NEUROCHEMISTRY

Deep Venomics Reveals the Mechanism for Expanded Peptide Diversity in Cone Snail Venom

(2012) Sébastien Dutertre et al.   MOLECULAR & CELLULAR PROTEOMICS

Nicotinic acetylcholine receptors: From basic science to therapeutics

(2012) Raymond Hurst et al.   PHARMACOLOGY & THERAPEUTICS

Towards an integrated venomics approach for accelerated conopeptide discovery

(2012) Jutty Rajan Prashanth et al.   TOXICON

ConoServer: updated content, knowledge, and discovery tools in the conopeptide database

(2011) Q. Kaas et al.   NUCLEIC ACIDS RESEARCH

Discovery and development of the χ-conopeptide class of analgesic peptides

(2011) Richard J. Lewis   TOXICON

Blockade of Neuronal α7-nAChR by α-Conotoxin ImI Explained by Computational Scanning and Energy Calculations

(2011) Rilei Yu et al.   PLoS Computational Biology

Venomics: a new paradigm for natural products-based drug discovery

(2010) Irina Vetter et al.   AMINO ACIDS

Stabilization of α-Conotoxin AuIB: Influences of Disulfide Connectivity and Backbone Cyclization

(2010) Erica S. Lovelace et al.   ANTIOXIDANTS & REDOX SIGNALING

Atypical α-Conotoxin LtIA fromConus litteratusTargets a Novel Microsite of the α3β2 Nicotinic Receptor

(2010) Sulan Luo et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

α-Conotoxin AuIB Isomers Exhibit Distinct Inhibitory Mechanisms and Differential Sensitivity to Stoichiometry of α3β4 Nicotinic Acetylcholine Receptors

(2010) Anton A. Grishin et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Cyclization of conotoxins to improve their biopharmaceutical properties

(2010) Richard J. Clark et al.   TOXICON

Alpha-conotoxins as pharmacological probes of nicotinic acetylcholine receptors

(2009) Layla Azam et al.   ACTA PHARMACOLOGICA SINICA

Insight in nAChR subtype selectivity from AChBP crystal structures

(2009) Prakash Rucktooa et al.   BIOCHEMICAL PHARMACOLOGY

Polypeptide and peptide toxins, magnifying lenses for binding sites in nicotinic acetylcholine receptors

(2009) Victor Tsetlin et al.   BIOCHEMICAL PHARMACOLOGY

Novel αD-Conopeptides and Their Precursors Identified by cDNA Cloning Define the D-Conotoxin Superfamily†‡

(2009) Marion L. Loughnan et al.   BIOCHEMISTRY

Structure and Activity of (2,8)-Dicarba-(3,12)-cystino α-ImI, an α-Conotoxin Containing a Nonreducible Cystine Analogue†

(2009) Christopher A. MacRaild et al.   JOURNAL OF MEDICINAL CHEMISTRY

χ-Conopeptide Pharmacophore Development: Toward a Novel Class of Norepinephrine Transporter Inhibitor (Xen2174) for Pain⊥

(2009) Andreas Brust et al.   JOURNAL OF MEDICINAL CHEMISTRY

Conotoxins: natural product drug leads

(2009) Reena Halai et al.   NATURAL PRODUCT REPORTS

Remarkable inter- and intra-species complexity of conotoxins revealed by LC/MS

(2009) Jasmine Davis et al.   PEPTIDES

Inhibition of Neuronal Nicotinic Acetylcholine Receptor Subtypes by α-Conotoxin GID and Analogues

(2008) Emma L. Millard et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

α-RgIA, a Novel Conotoxin That Blocks the α9α10 nAChR: Structure and Identification of Key Receptor-Binding Residues

(2008) Michael Ellison et al.   JOURNAL OF MOLECULAR BIOLOGY

Diversity of vertebrate nicotinic acetylcholine receptors

(2008) Neil S. Millar et al.   NEUROPHARMACOLOGY

α4/7-conotoxin Lp1.1 is a novel antagonist of neuronal nicotinic acetylcholine receptors

(2008) Can Peng et al.   PEPTIDES

Nicotinic agonists stimulate acetylcholine release from mouse interpeduncular nucleus: a function mediated by a different nAChR than dopamine release from striatum

(2003) Sharon R. Grady et al.   JOURNAL OF NEUROCHEMISTRY