Discovery of Methylene Thioacetal-Incorporated α-RgIA Analogues as Potent and Stable Antagonists of the Human α9α10 Nicotinic Acetylcholine Receptor for the Treatment of Neuropathic Pain

Alkyne-Bridged α-Conotoxin Vc1.1 Potently Reverses Mechanical Allodynia in Neuropathic Pain Models

(2021) Alessia Belgi et al.   JOURNAL OF MEDICINAL CHEMISTRY

Selective Penicillamine Substitution Enables Development of a Potent Analgesic Peptide that Acts through a Non-Opioid-Based Mechanism

(2021) Joanna Gajewiak et al.   JOURNAL OF MEDICINAL CHEMISTRY

Synthesis of disulfide surrogate peptides incorporating large-span surrogate bridges through a native chemical ligation-assisted diaminodiacid strategy

(2020) Qian Qu et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Critical residue properties for potency and selectivity of α-Conotoxin RgIA towards α9α10 nicotinic acetylcholine receptors

(2020) Peter N. Huynh et al.   BIOCHEMICAL PHARMACOLOGY

Development of Conformationally Constrained α-RgIA Analogues as Stable Peptide Antagonists of Human α9α10 Nicotinic Acetylcholine Receptors

(2020) Nan Zheng et al.   JOURNAL OF MEDICINAL CHEMISTRY

Curses or Cures: A Review of the Numerous Benefits Versus the Biosecurity Concerns of Conotoxin Research

(2020) Walden E. Bjørn-Yoshimoto et al.   Biomedicines

Backbone Cyclization Turns a Venom Peptide into a Stable and Equipotent Ligand at Both Muscle and Neuronal Nicotinic Receptors

(2020) Julien Giribaldi et al.   JOURNAL OF MEDICINAL CHEMISTRY

Medicinal chemistry, pharmacology, and therapeutic potential of α-conotoxins antagonizing the α9α10 nicotinic acetylcholine receptor

(2020) Xiao Li et al.   PHARMACOLOGY & THERAPEUTICS

Antibodies and venom peptides: new modalities for ion channels

(2019) Heike Wulff et al.   NATURE REVIEWS DRUG DISCOVERY

Adrenomedullin disulfide bond mimetics uncover structural requirements for AM1 receptor activation

(2019) Jan-Patrick Fischer et al.   JOURNAL OF PEPTIDE SCIENCE

Challenges and Opportunities for Therapeutics Targeting the Voltage-Gated Sodium Channel Isoform NaV1.7

(2019) John V. Mulcahy et al.   JOURNAL OF MEDICINAL CHEMISTRY

Crystal Structure of the Monomeric Extracellular Domain of α9 Nicotinic Receptor Subunit in Complex With α-Conotoxin RgIA: Molecular Dynamics Insights Into RgIA Binding to α9α10 Nicotinic Receptors

(2019) Marios Zouridakis et al.   Frontiers in Pharmacology

Conotoxins: Chemistry and Biology

(2019) Ai-Hua Jin et al.   CHEMICAL REVIEWS

Synthesis and Characterization of an A6-A11 Methylene Thioacetal Human Insulin Analogue with Enhanced Stability

(2019) Nan Zheng et al.   JOURNAL OF MEDICINAL CHEMISTRY

RgIA4 Accelerates Recovery from Paclitaxel-Induced Neuropathic Pain in Rats

(2019) Peter N. Huynh et al.   Marine Drugs

Structure–Activity Studies Reveal the Molecular Basis for GABAB-Receptor Mediated Inhibition of High Voltage-Activated Calcium Channels by α-Conotoxin Vc1.1

(2018) Mahsa Sadeghi et al.   ACS Chemical Biology

The Opioid Epidemic: Crisis and Solutions

(2018) Phil Skolnick   Annual Review of Pharmacology and Toxicology

Pain therapeutics from cone snail venoms: From Ziconotide to novel non-opioid pathways

(2018) Helena Safavi-Hemami et al.   Journal of Proteomics

Designing macrocyclic disulfide-rich peptides for biotechnological applications

(2018) Conan K. Wang et al.   Nature Chemical Biology

BPTI folding revisited: switching a disulfide into methylene thioacetal reveals a previously hidden path

(2018) Reem Mousa et al.   Chemical Science

Targeting of N-Type Calcium Channels via GABAB-Receptor Activation by α-Conotoxin Vc1.1 Variants Displaying Improved Analgesic Activity

(2018) Fengtao Cai et al.   JOURNAL OF MEDICINAL CHEMISTRY

Inhibition of α9α10 nicotinic acetylcholine receptors prevents chemotherapy-induced neuropathic pain

(2017) Haylie K. Romero et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

RgIA4 Potently Blocks Mouse α9α10 nAChRs and Provides Long Lasting Protection against Oxaliplatin-Induced Cold Allodynia

(2017) Sean B. Christensen et al.   Frontiers in Cellular Neuroscience

Neuropathic pain

(2017) Luana Colloca et al.   Nature Reviews Disease Primers

Prescription Opioid Misuse, Abuse, and Treatment in the United States: An Update

(2016) Kathleen T. Brady et al.   AMERICAN JOURNAL OF PSYCHIATRY

An analysis of FDA-approved drugs: natural products and their derivatives

(2016) Eric Patridge et al.   DRUG DISCOVERY TODAY

Counting on natural products for drug design

(2016) Tiago Rodrigues et al.   Nature Chemistry

Forecasting the opioid epidemic

(2016) D. S. Burke   SCIENCE

Converting disulfide bridges in native peptides to stable methylene thioacetals

(2016) C. M. B. K. Kourra et al.   Chemical Science

Voltage-Gated Sodium Channels: Structure, Function, Pharmacology, and Clinical Indications

(2015) Manuel de Lera Ruiz et al.   JOURNAL OF MEDICINAL CHEMISTRY

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

Stabilization of the Cysteine-Rich Conotoxin MrIA by Using a 1,2,3-Triazole as a Disulfide Bond Mimetic

(2014) Alessandro Gori et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Discovery, Synthesis, and Structure–Activity Relationships of Conotoxins

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

Dicarba Analogues of α-Conotoxin RgIA. Structure, Stability, and Activity at Potential Pain Targets

(2014) Sandeep Chhabra et al.   JOURNAL OF MEDICINAL CHEMISTRY

Neuronal nicotinic receptors as analgesic targets: It's a winding road

(2013) Iboro C. Umana et al.   BIOCHEMICAL PHARMACOLOGY

Multifaceted Roles of Disulfide Bonds. Peptides as Therapeutics

(2013) Miriam Góngora-Benítez et al.   CHEMICAL REVIEWS

Intrathecal Ziconotide: A Review of Its Use in Patients with Chronic Pain Refractory to Other Systemic or Intrathecal Analgesics

(2013) Mark Sanford   CNS DRUGS

γ-Aminobutyric Acid Type B (GABAB) Receptor Expression Is Needed for Inhibition of N-type (Cav2.2) Calcium Channels by Analgesic α-Conotoxins

(2012) Hartmut Cuny et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Ion Channels as Therapeutic Targets: A Drug Discovery Perspective

(2012) Sharan K. Bagal et al.   JOURNAL OF MEDICINAL CHEMISTRY

Effects of Cyclization on Stability, Structure, and Activity of α-Conotoxin RgIA at the α9α10 Nicotinic Acetylcholine Receptor and GABABReceptor

(2011) Reena Halai et al.   JOURNAL OF MEDICINAL CHEMISTRY

α-Conotoxin ImI Incorporating Stable Cystathionine Bridges Maintains Full Potency and Identical Three-Dimensional Structure

(2011) Zoltan Dekan et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

The Engineering of an Orally Active Conotoxin for the Treatment of Neuropathic Pain

(2010) Richard J. Clark et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Improving the Stability of α-Conotoxin AuIB Through N-to-C Cyclization: The Effect of Linker Length on Stability and Activity at Nicotinic Acetylcholine Receptors

(2010) Christopher J. Armishaw et al.   ANTIOXIDANTS & REDOX SIGNALING

Drug- and non-drug-associated QT interval prolongation

(2010) Charlotte Van Noord et al.   BRITISH JOURNAL OF CLINICAL PHARMACOLOGY

Solving the α-Conotoxin Folding Problem: Efficient Selenium-Directed On-Resin Generation of More Potent and Stable Nicotinic Acetylcholine Receptor Antagonists

(2010) Markus Muttenthaler et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

The structural basis of function in Cys-loop receptors

(2010) Andrew J. Thompson et al.   QUARTERLY REVIEWS OF BIOPHYSICS

Integrated Oxidative Folding of Cysteine/Selenocysteine Containing Peptides: Improving Chemical Synthesis of Conotoxins

(2009) Aleksandra Walewska et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Alpha9 nicotinic acetylcholine receptors and the treatment of pain

(2009) J. Michael McIntosh et al.   BIOCHEMICAL PHARMACOLOGY

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

Targeting the NMDA receptor subunit NR2B for the treatment of neuropathic pain

(2009) Long-Jun Wu et al.   Neurotherapeutics

Mammalian Nicotinic Acetylcholine Receptors: From Structure to Function

(2009) Edson X. Albuquerque et al.   PHYSIOLOGICAL REVIEWS

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

Analgesic  -Conotoxins Vc1.1 and Rg1A Inhibit N-Type Calcium Channels in Rat Sensory Neurons via GABAB Receptor Activation

(2008) B. Callaghan et al.   JOURNAL OF NEUROSCIENCE

Folding of Conotoxins: Formation of the Native Disulfide Bridges During Chemical Synthesis and Biosynthesis of Conus Peptides

(2007) Grzegorz Bulaj et al.   ANTIOXIDANTS & REDOX SIGNALING