ω-Conotoxin GVIA Mimetics that Bind and Inhibit Neuronal Cav2.2 Ion Channels
Marine Drugs, 2012 The neuronal voltage-gated N-type calcium channel (Cav2.2) is a validated target for the treatment of neuropathic pain. A small library of anthranilamide-derived ω-Conotoxin GVIA mimetics bearing the diphenylmethylpiperazine moiety were prepared and ...
Peter J. Duggan +7 more
doaj +3 more sources
Conotoxin protein classification using free scores of words and support vector machines
BMC Bioinformatics, 2011 Background Conotoxin has been proven to be effective in drug design and could be used to treat various disorders such as schizophrenia, neuromuscular disorders and chronic pain.
Nuel Gregory +3 more
doaj +2 more sources
Stapling Cysteine[2,4] Disulfide Bond of α-Conotoxin LsIA and Its Potential in Target Delivery
Marine Drugsα-Conotoxins, as selective nAChR antagonists, can be valuable tools for targeted drug delivery and fluorescent labeling, while conotoxin-drug or conotoxin-fluorescent conjugates through the disulfide bond are rarely reported.
Xin Sun +6 more
doaj +2 more sources
Conkazal-M1 from the MKAVA family of conotoxins: A dual-function protease inhibitor and neuroactive peptide. [PDF]
Protein SciAbstract Marine cone snails produce a diverse array of bioactive peptides, known as conotoxins, in their venom. Given their high target potency and specificity, conotoxins are attractive compounds for the development of precision research tools and pharmacological agents.
Hackney CM +12 more
europepmc +2 more sources
GABA<sub>B</sub> receptor-mediated modulation of sensory neuron excitability: Roles of Ca<sub>V</sub>2.2, G-protein-coupled inwardly rectifying potassium (GIRK) channels, and hyperpolarisation-activated cyclic nucleotide-gated (HCN) channels in human and mouse nociception. [PDF]
Exp PhysiolAbstract Chronic visceral pain is a key symptom of irritable bowel syndrome. Modulation of voltage‐gated calcium and potassium channels by G protein‐coupled receptors plays a key role in dampening nociceptive transmission. Both baclofen and the analgesic peptide α‐conotoxin Vc1.1 activate GABAB receptors (GABABR), resulting in inhibition of CaV2.2 and ...
Brizuela M +4 more
europepmc +2 more sources
Alternative Pathways of Acetylcholine Release in the Colon: Role of High-Affinity Choline Transporters. [PDF]
Neurogastroenterol MotilMechanisms of Acetylcholine release, including typical and atypical release under neuronal blockade. Left panel illustrates the classical (quantal) cholinergic transmission and the right panel the mechanism described in the present study. High‐Affinity Choline Transporter (HCT), Acetylcholine (ACh), Acetylcholinesterase (ACE), and Tetrodotoxin (TTX ...
Martinez-Daunis A +4 more
europepmc +2 more sources
Ion Channels as Marine Drug Targets [PDF]
, 2020 Marine Drugs is glad to announce its first Special Issue book on “ion channels” related research: Under the great stewardship of the Guest Editor, Dr.
core +2 more sources
Journal of Venomous Animals and Toxins including Tropical Diseases, 2021 Background Conotoxins have become a research hotspot in the neuropharmacology field for their high activity and specificity in targeting ion channels and neurotransmitter receptors.
Manyi Yang +3 more
doaj +1 more source
Systematic dissection of genomic features determining the vast diversity of conotoxins
BMC Genomics, 2023 Background Conus, a highly diverse species of venomous predators, has attracted significant attention in neuroscience and new drug development due to their rich collection of neuroactive peptides called conotoxins.
Jian-Wei Zheng +9 more
doaj +1 more source
Frontiers in Marine Science, 2022 Marine cone snail venoms represent a vast library of bioactive peptides with proven potential as research tools, drug leads, and therapeutics. In this study, a transcriptome library of four different organs, namely radular sheath, venom duct, venom gland,
Yanling Liao +8 more
doaj +1 more source