Results 11 to 20 of about 22,310 (212)

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, Aijun Yang, Irina Vetter, Jeffrey R. McArthur, Richard J. Lewis, Kellie L. Tuck, Jonathan B. Baell, Charlotte Elisabet Tranberg   +7 more
doaj   +3 more sources

Conotoxin protein classification using free scores of words and support vector machines [PDF]

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, Wolfsheimer Stefan, Zaki Nazar, Khuri Sawsan   +3 more
doaj   +2 more sources

Stapling Cysteine[2,4] Disulfide Bond of α-Conotoxin LsIA and Its Potential in Target Delivery

Marine Drugs
α-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, Jiangnan Hu, Maomao Ren, Hong Chang, Dongting Zhangsun, Baojian Zhang, Shuai Dong   +6 more
doaj   +2 more sources

Pharmacological Inhibition of Cav2.2 Channels by Recombinant Phα1β Toxin (CTK01512-2). [PDF]

Basic Clin Pharmacol Toxicol
The recombinant Phα1β toxin (CTK01512‐2) partially and reversibly inhibits Cav2.2 calcium channels in HEK‐293 cells. CTK01512‐2 displays dose‐dependent inhibition of N‐type calcium currents, with an IC50 of 3.94 nM. In vivo, CTK01512‐2 effectively reduces mechanical allodynia in a neuropathic pain model, confirming its antinociceptive activity ...
Carobin NV, Moraes TR, Ferreira LA, Kushmerick C, Gomez MV, Junior CJC.   +5 more
europepmc   +2 more sources

Conkazal-M1 from the MKAVA family of conotoxins: A dual-function protease inhibitor and neuroactive peptide. [PDF]

Protein Sci
Abstract 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, Koch TL, Ryding NL, Rogalski A, Chase K, Giglio ML, Espino SS, Acyatan ZG, Watkins M, Olivera BM, Safavi-Hemami H, Teilum K, Ellgaard L.   +12 more
europepmc   +2 more sources

Satellite Glial Cells Synthesize and Release GABA to Activate Extrasynaptic GABA_A Receptors That Modulate Dorsal Root Ganglia Neuron Excitability. [PDF]

Glia
Mechanism of synthesis, release, receptor activation, uptake, and degradation of GABA in dorsal root ganglia (DRG). Left: GABA is synthesized from putrescine in satellite glial cells (SGCs). After being released by Best1 channel, it activates GABAA receptors in sensory neurons, producing a chloride current.
Jiménez-Barrios N, González-Ramírez R, Paz-Bermúdez FJ, Raya-Tafolla G, Vila JS, Felix R, Delgado-Lezama R, Garduño BF.   +7 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

GABA_B receptor-mediated modulation of sensory neuron excitability: Roles of Ca_V2.2, G-protein-coupled inwardly rectifying potassium (GIRK) channels, and hyperpolarisation-activated cyclic nucleotide-gated (HCN) channels in human and mouse nociception. [PDF]

Exp Physiol
Abstract 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, Bony AR, Garcia-Caraballo S, Adams DJ, Brierley SM.   +4 more
europepmc   +2 more sources

Alternative Pathways of Acetylcholine Release in the Colon: Role of High-Affinity Choline Transporters. [PDF]

Neurogastroenterol Motil
Mechanisms 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, Yordanova B, Traserra S, Vergara P, Jimenez M.   +4 more
europepmc   +2 more sources

A novel proline-rich M-superfamily conotoxin that can simultaneously affect sodium, potassium and calcium currents

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, Yubin Li, Longfei Liu, Maojun Zhou   +3 more
doaj   +1 more source