Antibodies and venom peptides: new modalities for ion channels

Exploiting Nanobodies’ Singular Traits

(2018) Jessica R. Ingram et al.   Annual Review of Immunology

Peptide therapeutics from venom: Current status and potential

(2018) Michael W. Pennington et al.   BIOORGANIC & MEDICINAL CHEMISTRY

A novel PADRE-Kv1.3 vaccine effectively induces therapeutic antibodies and ameliorates experimental autoimmune encephalomyelitis in rats

(2018) Cheng Fan et al.   CLINICAL IMMUNOLOGY

Modulating ion channel function with antibodies and nanobodies

(2018) Catelijne Stortelers et al.   CURRENT OPINION IN IMMUNOLOGY

Design of Conformationally Constrained Acyl Sulfonamide Isosteres: Identification of N-([1,2,4]Triazolo[4,3-a]pyridin-3-yl)methane-sulfonamides as Potent and Selective hNaV1.7 Inhibitors for the Treatment of Pain

(2018) Thilo Focken et al.   JOURNAL OF MEDICINAL CHEMISTRY

Co-expression of β Subunits with the Voltage-Gated Sodium Channel NaV1.7: the Importance of Subunit Association and Phosphorylation and Their Effects on Channel Pharmacology and Biophysics

(2018) Maxim V. Sokolov et al.   JOURNAL OF MOLECULAR NEUROSCIENCE

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

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

A multiplatform strategy for the discovery of conventional monoclonal antibodies that inhibit the voltage-gated potassium channel Kv1.3

(2018) Janna Bednenko et al.   mAbs

Efficacy of the Nav1.7 blocker PF-05089771 in a randomised, placebo-controlled, double-blind clinical study in subjects with painful diabetic peripheral neuropathy

(2018) Aoibhinn McDonnell et al.   PAIN

Pharmacological characterization of potent and selective NaV1.7 inhibitors engineered from Chilobrachys jingzhao tarantula venom peptide JzTx-V

(2018) Bryan D. Moyer et al.   PLoS One

Differential Inhibition of Nav1.7 and Neuropathic Pain by Hybridoma-Produced and Recombinant Monoclonal Antibodies that Target Nav1.7

(2018) Sangsu Bang et al.   Neuroscience Bulletin

Next-Generation Sequencing of Antibody Display Repertoires

(2018) Romain Rouet et al.   Frontiers in Immunology

ATP in the tumour microenvironment drives expression of nfP2X7, a key mediator of cancer cell survival

(2018) SM Gilbert et al.   ONCOGENE

Selection of an ASIC1a-blocking combinatorial antibody that protects cells from ischemic death

(2018) Min Qiang et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Selective NaV1.1 activation rescues Dravet syndrome mice from seizures and premature death

(2018) Kay L. Richards et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

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

(2018) Xiaojing Pan et al.   SCIENCE

Selective NaV1.7 Antagonists with Long Residence Time Show Improved Efficacy against Inflammatory and Neuropathic Pain

(2018) Girish Bankar et al.   Cell Reports

Electrophoretic drug delivery for seizure control

(2018) Christopher M. Proctor et al.   Science Advances

De novo design of self-assembling helical protein filaments

(2018) Hao Shen et al.   SCIENCE

Venom peptides as therapeutics: advances, challenges and the future of venom-peptide discovery

(2017) Samuel D. Robinson et al.   Expert Review of Proteomics

Cutaneous iontophoresis of μ-conotoxin CnIIIC—A potent Na V 1.4 antagonist with analgesic, anaesthetic and myorelaxant properties

(2017) Sergio del Río-Sancho et al.   INTERNATIONAL JOURNAL OF PHARMACEUTICS

Nonclinical Profile of BLZ-100, a Tumor-Targeting Fluorescent Imaging Agent

(2017) Julia Parrish-Novak et al.   INTERNATIONAL JOURNAL OF TOXICOLOGY

First-in-human phase I study of SOR-C13, a TRPV6 calcium channel inhibitor, in patients with advanced solid tumors

(2017) S. Fu et al.   INVESTIGATIONAL NEW DRUGS

Pharmacologic Characterization of AMG8379, a Potent and Selective Small Molecule Sulfonamide Antagonist of the Voltage-Gated Sodium Channel Na V 1.7

(2017) Thomas J. Kornecook et al.   JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS

Antibodies targeting G protein-coupled receptors: Recent advances and therapeutic challenges

(2017) Mohammed Akli Ayoub et al.   mAbs

Opportunities for therapeutic antibodies directed at G-protein-coupled receptors

(2017) Catherine J. Hutchings et al.   NATURE REVIEWS DRUG DISCOVERY

Next generation antibody drugs: pursuit of the 'high-hanging fruit'

(2017) Paul J. Carter et al.   NATURE REVIEWS DRUG DISCOVERY

Forty Years of Sodium Channels: Structure, Function, Pharmacology, and Epilepsy

(2017) William A. Catterall   NEUROCHEMICAL RESEARCH

Kv1.3 expression on effector memory T cells in sporadic inclusion body myositis: potential for targeted immunotherapy with dalazatide

(2017) T. Mozaffar et al.   NEUROMUSCULAR DISORDERS

Venom-derived peptide inhibitors of voltage-gated potassium channels

(2017) Raymond S. Norton et al.   NEUROPHARMACOLOGY

Development of therapeutic antibodies to G protein-coupled receptors and ion channels: Opportunities, challenges and their therapeutic potential in respiratory diseases

(2017) Julie A. Douthwaite et al.   PHARMACOLOGY & THERAPEUTICS

Potent neuroprotection after stroke afforded by a double-knot spider-venom peptide that inhibits acid-sensing ion channel 1a

(2017) Irène R. Chassagnon et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

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

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

(2017) Huaizong Shen et al.   SCIENCE

Synergistic regulation of serotonin and opioid signaling contributes to pain insensitivity in Nav1.7 knockout mice

(2017) Jörg Isensee et al.   Science Signaling

Towards a Structural View of Drug Binding to hERG K + Channels

(2017) Jamie I. Vandenberg et al.   TRENDS IN PHARMACOLOGICAL SCIENCES

Potassium channels Kv1.3 and KCa3.1 cooperatively and compensatorily regulate antigen-specific memory T cell functions

(2017) Eugene Y. Chiang et al.   Nature Communications

Pharmacological characterisation of the highly NaV1.7 selective spider venom peptide Pn3a

(2017) Jennifer R. Deuis et al.   Scientific Reports

Synergistic regulation of serotonin and opioid signaling contributes to pain insensitivity in Nav1.7 knockout mice

(2017) Jörg Isensee et al.   Science Signaling

Single-Domain Antibodies As Versatile Affinity Reagents for Analytical and Diagnostic Applications

(2017) Gualberto Gonzalez-Sapienza et al.   Frontiers in Immunology

T Cell Subset and Stimulation Strength-Dependent Modulation of T Cell Activation by Kv1.3 Blockers

(2017) Wai-Ping Fung-Leung et al.   PLoS One

Safety and pharmacodynamics of dalazatide, a Kv1.3 channel inhibitor, in the treatment of plaque psoriasis: A randomized phase 1b trial

(2017) Eric J. Tarcha et al.   PLoS One

Autocrine-Based Selection of Drugs That Target Ion Channels from Combinatorial Venom Peptide Libraries

(2016) Hongkai Zhang et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Efficient enzymatic cyclization of an inhibitory cystine knot-containing peptide

(2016) Soohyun Kwon et al.   BIOTECHNOLOGY AND BIOENGINEERING

Peptidomimetic Targeting of Cavβ2 Overcomes Dysregulation of the L-Type Calcium Channel Density and Recovers Cardiac FunctionClinical Perspective

(2016) Francesca Rusconi et al.   CIRCULATION

α-Conotoxin Vc1.1 inhibits human dorsal root ganglion neuroexcitability and mouse colonic nociception via GABA B receptors

(2016) Joel Castro et al.   GUT

Modulation of P2X3 and P2X2/3 Receptors by Monoclonal Antibodies

(2016) Anatoly Shcherbatko et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Pulmonary Delivery of the Kv1.3-Blocking Peptide HsTX1[R14A] for the Treatment of Autoimmune Diseases

(2016) Liang Jin et al.   JOURNAL OF PHARMACEUTICAL SCIENCES

Selective spider toxins reveal a role for the Nav1.1 channel in mechanical pain

(2016) Jeremiah D. Osteen et al.   NATURE

Accurate de novo design of hyperstable constrained peptides

(2016) Gaurav Bhardwaj et al.   NATURE

A mutagenesis and screening strategy to generate optimally thermostabilized membrane proteins for structural studies

(2016) Francesca Magnani et al.   Nature Protocols

A comprehensive map of molecular drug targets

(2016) Rita Santos et al.   NATURE REVIEWS DRUG DISCOVERY

Myasthenia gravis — autoantibody characteristics and their implications for therapy

(2016) Nils Erik Gilhus et al.   Nature Reviews Neurology

Generation of Recombinant Monoclonal Antibodies from Immunised Mice and Rabbits via Flow Cytometry and Sorting of Antigen-Specific IgG+ Memory B Cells

(2016) Dale. O Starkie et al.   PLoS One

Peptidomimetic Star Polymers for Targeting Biological Ion Channels

(2016) Rong Chen et al.   PLoS One

Rational design of a Kv1.3 channel-blocking antibody as a selective immunosuppressant

(2016) Rongsheng E. Wang et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Nanobodies that block gating of the P2X7 ion channel ameliorate inflammation

(2016) W. Danquah et al.   Science Translational Medicine

A monoclonal antibody against KCNK9 K+ channel extracellular domain inhibits tumour growth and metastasis

(2016) Han Sun et al.   Nature Communications

Automated structure refinement of macromolecular assemblies from cryo-EM maps using Rosetta

(2016) Ray Yu-Ruei Wang et al.   eLife

High-efficiency antibody discovery achieved with multiplexed microscopy

(2016) Shelley Mettler Izquierdo et al.   Microscopy

Phenotypic lentivirus screens to identify functional single domain antibodies

(2016) Florian I. Schmidt et al.   Nature Microbiology

Subtype-Selective Small Molecule Inhibitors Reveal a Fundamental Role for Nav1.7 in Nociceptor Electrogenesis, Axonal Conduction and Presynaptic Release

(2016) Aristos J. Alexandrou et al.   PLoS One

Ion Channels in Innate and Adaptive Immunity

(2015) Stefan Feske et al.   Annual Review of Immunology

Fusion Proteins for Half-Life Extension of Biologics as a Strategy to Make Biobetters

(2015) William R. Strohl   BIODRUGS

Peptide therapeutics: current status and future directions

(2015) Keld Fosgerau et al.   DRUG DISCOVERY TODAY

Challenges and opportunities for non-antibody scaffold drugs

(2015) Rodrigo Vazquez-Lombardi et al.   DRUG DISCOVERY TODAY

Buccal mucosal delivery of a potent peptide leads to therapeutically-relevant plasma concentrations for the treatment of autoimmune diseases

(2015) Liang Jin et al.   JOURNAL OF CONTROLLED RELEASE

The Effect of a Connexin43-Based Peptide on the Healing of Chronic Venous Leg Ulcers: A Multicenter, Randomized Trial

(2015) Gautam S. Ghatnekar et al.   JOURNAL OF INVESTIGATIVE DERMATOLOGY

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

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

Pharmaceutical Optimization of Peptide Toxins for Ion Channel Targets: Potent, Selective, and Long-Lived Antagonists of Kv1.3

(2015) Justin K. Murray et al.   JOURNAL OF MEDICINAL CHEMISTRY

Targeting voltage-gated calcium channels in neurological and psychiatric diseases

(2015) Gerald W. Zamponi   NATURE REVIEWS DRUG DISCOVERY

Structural basis of Nav1.7 inhibition by an isoform-selective small-molecule antagonist

(2015) S. Ahuja et al.   SCIENCE

Topical administration of a connexin43-based peptide augments healing of chronic neuropathic diabetic foot ulcers: A multicenter, randomized trial

(2015) Christina L. Grek et al.   WOUND REPAIR AND REGENERATION

Endogenous opioids contribute to insensitivity to pain in humans and mice lacking sodium channel Nav1.7

(2015) Michael S. Minett et al.   Nature Communications

Less is More: Design of a Highly Stable Disulfide-Deleted Mutant of Analgesic Cyclic α-Conotoxin Vc1.1

(2015) Rilei Yu et al.   Scientific Reports

A Monoclonal Antibody that Targets a NaV1.7 Channel Voltage Sensor for Pain and Itch Relief

(2014) Jun-Ho Lee et al.   CELL

Design, Synthesis and Biological Evaluation of Two Opioid Agonist and Cav2.2 Blocker Multitarget Ligands

(2014) Adriano Mollica et al.   Chemical Biology & Drug Design

Targeting the Ion Channel Kv1.3 with Scorpion Venom Peptides Engineered for Potency, Selectivity, and Half-life

(2014) Wilson Edwards et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Clinical development success rates for investigational drugs

(2014) Michael Hay et al.   NATURE BIOTECHNOLOGY

A shortened, protecting group free, synthesis of the anti-wrinkle venom analogue Syn-Ake® exploiting an optimized Hofmann-type rearrangement

(2014) A.N. Balaev et al.   TETRAHEDRON LETTERS

Proof of dual-topology architecture of Fluc F− channels with monobody blockers

(2014) Randy B. Stockbridge et al.   Nature Communications

Dicarba α-Conotoxin Vc1.1 Analogues with Differential Selectivity for Nicotinic Acetylcholine and GABAB Receptors

(2013) Bianca J. van Lierop et al.   ACS Chemical Biology

Antibody therapeutics targeting ion channels: are we there yet?

(2013) Han Sun et al.   ACTA PHARMACOLOGICA SINICA

Nanobodies: Natural Single-Domain Antibodies

(2013) Serge Muyldermans   Annual Review of Biochemistry

Neuroactive Insecticides: Targets, Selectivity, Resistance, and Secondary Effects

(2013) John E. Casida et al.   Annual Review of Entomology

Future directions for peptide therapeutics development

(2013) Allan A. Kaspar et al.   DRUG DISCOVERY TODAY

Activation and allosteric modulation of a muscarinic acetylcholine receptor

(2013) Andrew C. Kruse et al.   NATURE

In Vivo Detection of Human TRPV6-Rich Tumors with Anti-Cancer Peptides Derived from Soricidin

(2013) Chris V. Bowen et al.   PLoS One

Antibody-Mediated Targeting of the Orai1 Calcium Channel Inhibits T Cell Function

(2013) Jennifer H. Cox et al.   PLoS One

The Structural Basis of Antibody-Antigen Recognition

(2013) Inbal Sela-Culang et al.   Frontiers in Immunology

Mechanism and molecular basis for the sodium channel subtype specificity of µ-conopeptide CnIIIC

(2012) René Markgraf et al.   BRITISH JOURNAL OF PHARMACOLOGY

In Vivo Bio-imaging Using Chlorotoxin-based Conjugates

(2012) Mark R. Stroud et al.   CURRENT PHARMACEUTICAL DESIGN

Stapling Mimics Noncovalent Interactions of γ-Carboxyglutamates in Conantokins, Peptidic Antagonists ofN-Methyl-d-Aspartic Acid Receptors

(2012) Randall J. Platt et al.   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

Voltage-gated sodium channels at 60: structure, function and pathophysiology

(2012) William A. Catterall   JOURNAL OF PHYSIOLOGY-LONDON

The role of the TRPV6 channel in cancer

(2012) V’yacheslav Lehen’kyi et al.   JOURNAL OF PHYSIOLOGY-LONDON

ω-Conotoxin GVIA Mimetics that Bind and Inhibit Neuronal Cav2.2 Ion Channels

(2012) Charlotte Elisabet Tranberg et al.   Marine Drugs

Cyclisation Increases the Stability of the Sea Anemone Peptide APETx2 but Decreases Its Activity at Acid-Sensing Ion Channel 3

(2012) Jonas E. Jensen et al.   Marine Drugs

Finding the sweet spot: the role of nature and nurture in medicinal chemistry

(2012) Michael M. Hann et al.   NATURE REVIEWS DRUG DISCOVERY

Viroporins: structure and biological functions

(2012) José Luis Nieva et al.   NATURE REVIEWS MICROBIOLOGY

The Antibody Targeting the E314 Peptide of Human Kv1.3 Pore Region Serves as a Novel, Potent and Specific Channel Blocker

(2012) Xiao-Fang Yang et al.   PLoS One

Gain-of-function Nav1.8 mutations in painful neuropathy

(2012) C. G. Faber et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Structural Alert/Reactive Metabolite Concept as Applied in Medicinal Chemistry to Mitigate the Risk of Idiosyncratic Drug Toxicity: A Perspective Based on the Critical Examination of Trends in the Top 200 Drugs Marketed in the United States

(2011) Antonia F. Stepan et al.   CHEMICAL RESEARCH IN TOXICOLOGY

Venoms as a platform for human drugs: translating toxins into therapeutics

(2011) Glenn F King   EXPERT OPINION ON BIOLOGICAL THERAPY

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

Lambert–Eaton myasthenic syndrome: from clinical characteristics to therapeutic strategies

(2011) Maarten J Titulaer et al.   LANCET NEUROLOGY

Structure of a nanobody-stabilized active state of the β2 adrenoceptor

(2011) Søren G. F. Rasmussen et al.   NATURE

Fluorescent fusion protein knockout mediated by anti-GFP nanobody

(2011) Emmanuel Caussinus et al.   NATURE STRUCTURAL & MOLECULAR BIOLOGY

Accelerated Neuronal Cell Recovery from Botulinum Neurotoxin Intoxication by Targeted Ubiquitination

(2011) Chueh-Ling Kuo et al.   PLoS One

Development of a sea anemone toxin as an immunomodulator for therapy of autoimmune diseases

(2011) Victor Chi et al.   TOXICON

Ziconotide for treatment of severe chronic pain

(2010) Achim Schmidtko et al.   LANCET

The functional network of ion channels in T lymphocytes

(2009) Michael D. Cahalan et al.   IMMUNOLOGICAL REVIEWS

Sustained-release oral fampridine in multiple sclerosis: a randomised, double-blind, controlled trial

(2009) Andrew D Goodman et al.   LANCET

Chloride channels as drug targets

(2009) Alan S. Verkman et al.   NATURE REVIEWS DRUG DISCOVERY

Voltage-gated potassium channels as therapeutic targets

(2009) Heike Wulff et al.   NATURE REVIEWS DRUG DISCOVERY

Rescue of CF airway epithelial cell function in vitro by a CFTR potentiator, VX-770

(2009) F. Van Goor et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Imaging of Effector Memory T Cells during a Delayed-Type Hypersensitivity Reaction and Suppression by Kv1.3 Channel Block

(2008) Melanie P. Matheu et al.   IMMUNITY

Ion Channels as Drug Targets: The Next GPCRs

(2008) Gregory J. Kaczorowski et al.   JOURNAL OF GENERAL PHYSIOLOGY

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

High-throughput electrophysiology: an emerging paradigm for ion-channel screening and physiology

(2008) John Dunlop et al.   NATURE REVIEWS DRUG DISCOVERY

Transient receptor potential channels: targeting pain at the source

(2008) Ardem Patapoutian et al.   NATURE REVIEWS DRUG DISCOVERY

Conformational thermostabilization of the  1-adrenergic receptor in a detergent-resistant form

(2008) M. J. Serrano-Vega et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Transcriptional and functional profiles of voltage-gated Na+ channels in injured and non-injured DRG neurons in the SNI model of neuropathic pain

(2007) Temugin Berta et al.   MOLECULAR AND CELLULAR NEUROSCIENCE