Results 41 to 50 of about 1,700,583 (126)

α-Conotoxin Peptidomimetics: Probing the Minimal Binding Motif for Effective Analgesia

Toxins, 2020
Several analgesic α-conotoxins have been isolated from marine cone snails. Structural modification of native peptides has provided potent and selective analogues for two of its known biological targets—nicotinic acetylcholine and γ-aminobutyric acid ...
Adam C. Kennedy, Alessia Belgi, Benjamin W. Husselbee, David Spanswick, Raymond S. Norton, Andrea J. Robinson   +5 more
doaj   +1 more source

Monkey adrenal chromaffin cells express α6β4* nicotinic acetylcholine receptors. [PDF]

PLoS ONE, 2014
Nicotinic acetylcholine receptors (nAChRs) that contain α6 and β4 subunits have been demonstrated functionally in human adrenal chromaffin cells, rat dorsal root ganglion neurons, and on noradrenergic terminals in the hippocampus of adolescent mice.
Alicia Hernández-Vivanco, Arik J Hone, Mick L Scadden, Beatriz Carmona-Hidalgo, J Michael McIntosh, Almudena Albillos   +5 more
doaj   +1 more source

Toxinology of Marine Venomous Snails

Iranian South Medical Journal, 2021
A surprisingly large number of sea snail species are venomous. Cone snail venoms are produced in a lengthy tubular duct from a complex venom gland and form a cocktail of many toxins, particularly conotoxins which have high potency and specificity for ...
Gholam Hossein Mohebbi, Iraj Nabipour
doaj  

A Novel α4/7-Conotoxin QuIA Selectively Inhibits α3β2 and α6/α3β4 Nicotinic Acetylcholine Receptor Subtypes with High Efficacy

Marine Drugs, 2022
α6β4 nAChR is expressed in the peripheral and central nervous systems and is associated with pain, addiction, and movement disorders. Natural α-conotoxins (α-CTxs) can effectively block different nAChR subtypes with higher efficacy and selectivity ...
Liujun Wang, Xixi Wu, Xiaopeng Zhu, Dongting Zhangsun, Yong Wu, Sulan Luo   +5 more
doaj   +1 more source

Discovery, Pharmacological Characterisation and NMR Structure of the Novel µ-Conotoxin SxIIIC, a Potent and Irreversible Na_V Channel Inhibitor

Biomedicines, 2020
Voltage-gated sodium (NaV) channel subtypes, including NaV1.7, are promising targets for the treatment of neurological diseases, such as chronic pain. Cone snail-derived µ-conotoxins are small, potent NaV channel inhibitors which represent potential drug
Kirsten L. McMahon, Hue N.T. Tran, Jennifer R. Deuis, Richard J. Lewis, Irina Vetter, Christina I. Schroeder   +5 more
doaj   +1 more source

Interactions of the α3β2 Nicotinic Acetylcholine Receptor Interfaces with α-Conotoxin LsIA and its Carboxylated C-terminus Analogue: Molecular Dynamics Simulations

Marine Drugs, 2020
Notably, α-conotoxins with carboxy-terminal (C-terminal) amidation are inhibitors of the pentameric nicotinic acetylcholine receptors (nAChRs), which are therapeutic targets for neurological diseases and disorders.
Jierong Wen, David J. Adams, Andrew Hung
doaj   +1 more source

Analgesic α-conotoxins modulate GIRK1/2 channels via GABAB receptor activation and reduce neuroexcitability

bioRxiv, 2020
Activation of G protein-coupled inwardly rectifying potassium (GIRK or Kir3) channels leads to membrane hyperpolarization and dampening of neuronal excitability.
Anuja R. Bony, J. McArthur, Rocio K. Finol-Urdaneta, David John Adams   +3 more
semanticscholar   +1 more source

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

Toxins, 2015
Nicotinic acetylcholine receptors (nAChRs) fulfill a variety of functions making identification and analysis of nAChR subtypes a challenging task. Traditional instruments for nAChR research are d-tubocurarine, snake venom protein α-bungarotoxin (α-Bgt ...
Denis Kudryavtsev, Irina Shelukhina, Catherine Vulfius, Tatyana Makarieva, Valentin Stonik, Maxim Zhmak, Igor Ivanov, Igor Kasheverov, Yuri Utkin, Victor Tsetlin   +9 more
doaj   +1 more source

Molecular basis for a pore block of Tentonin 3 expressed in HEK293 cells by a conopeptide, NMB‐1

British Journal of Pharmacology, EarlyView.
Background and Purpose Tentonin 3 (TTN3/TMEM150C) is a mechanosensitive ion channel that plays critical roles in mechanotransduction processes. TTN3 forms a tetramer with a predicted rectangular shape and a central pore. A conotoxin ρ‐TIA and its synthetic analog, noxious mechanosensation blocker 1 (NMB‐1), were initially developed to inhibit slowly ...
Sujin Lim, Junhyuk Woo, Sungmin Pak, Joonho Paik, Gyu‐Sang Hong, Ji Hun Wi, Sanghee Lee, Cristina Fenollar‐Ferrer, Kyungreem Han, Young Kee Shin, Uhtaek Oh   +10 more
wiley   +1 more source

From Crystal Structures of RgIA4 in Complex with Ac-AChBP to Molecular Determinants of Its High Potency of α9α10 nAChR

Marine Drugs, 2021
α9-containing nicotinic acetylcholine receptors (nAChRs) have been shown to play critical roles in neuropathic pain. The α-conotoxin (α-CTx) RgIA and its analog RgIA4 were identified as the most selective inhibitor of α9α10 nAChR.
Si Pan, Yingxu Fan, Xiaopeng Zhu, Yi Xue, Sulan Luo, Xinquan Wang   +5 more
doaj   +1 more source