α9-Containing Nicotinic Acetylcholine Receptors Are Required for RgIA-5474 Attenuation of Chemotherapy-Induced Neuropathic Pain [PDF]
ACS Pharmacology and Translational ScienceNicotinic acetylcholine receptors containing the α9 subunit have been mechanistically implicated in alleviating chemotherapy-induced neuropathic pain. However, the cell types that underlie these effects are currently unknown. RgIA-5474 is a recently developed, synthetic α-conotoxin analog that is a potent antagonist of human α9α10 nAChRs.
Layla Azam +2 more
exaly +4 more sources
The α9α10 nicotinic acetylcholine receptors antagonist α-conotoxin RgIA reverses colitis signs in murine dextran sodium sulfate model [PDF]
European Journal of Pharmacology, 2020 Nicotinic acetylcholine receptors can regulate inflammation primarily through the vagus nerve via the cholinergic anti-inflammatory pathway. α9α10 nicotinic receptors (nAChRs) are a new promising target for chronic pain and inflammation. Recently, α9α10 selective α-conotoxin antagonists were shown to have antinociception effect in neuropathic and tonic
Shakir D Alsharari +2 more
exaly +5 more sources
RgIA4 Prevention of Acute Oxaliplatin-Induced Cold Allodynia Requires α9-Containing Nicotinic Acetylcholine Receptors and CD3+ T-Cells [PDF]
Cells, 2022 Chemotherapy-induced neuropathic pain is a debilitating and dose-limiting side effect. Oxaliplatin is a third-generation platinum and antineoplastic compound that is commonly used to treat colorectal cancer and commonly yields neuropathic side effects ...
Peter N. Huynh +2 more
doaj +2 more sources
Alkaloid ligands enable function of homomeric human α10 nicotinic acetylcholine receptors [PDF]
Frontiers in Pharmacology, 2022 In the nervous system, nicotinic acetylcholine receptors (nAChRs) rapidly transduce a chemical signal into one that is electrical via ligand-gated ion flux through the central channel of the receptor.
Arik J. Hone +4 more
doaj +2 more sources
Nicotinic acetylcholine receptors: Therapeutic targets for novel ligands to treat pain and inflammation [PDF]
Pharmacological Research, 2023 Nicotinic acetylcholine receptors (nAChRs) have been historically defined as ligand-gated ion channels and function as such in the central and peripheral nervous systems. Recently, however, non-ionic signaling mechanisms via nAChRs have been demonstrated
Arik J. Hone, J. Michael McIntosh
doaj +2 more sources
Interaction of α9α10 Nicotinic Receptors With Peptides and Proteins From Animal Venoms [PDF]
Frontiers in Cellular Neuroscience, 2021 Unlike most neuronal nicotinic acetylcholine receptor (nAChR) subunits, α7, α9, and α10 subunits are able to form functional homo- or heteromeric receptors without any β subunits.
Victor Tsetlin +11 more
doaj +2 more sources
α-RgIA: A Novel Conotoxin That Specifically and Potently Blocks the α9α10 nAChR, [PDF]
Biochemistry, 2006 The alpha9 and alpha10 nicotinic acetylcholine receptor (nAChR) subunits assemble to form the alpha9alpha10 nAChR subtype. This receptor is believed to mediate cholinergic synaptic transmission between efferent olivocochlear fibers and the hair cells of the cochlea. In addition alpha9 and/or alpha10 expression has been described in dorsal root ganglion
Ellison, Michael +6 more
+7 more sources
Computational Design of α-Conotoxins to Target Specific Nicotinic Acetylcholine Receptor Subtypes. [PDF]
ChemistryFoldX was benchmarked as the best energy prediction method, and seven accurate molecular models of α‐conotoxin/nAChRs were developed as surrogates for the experimental complexes. The combined use of FoldX and these molecular models emerged as an effective approach to predict α‐conotoxins with improved pharmaceutical properties.
Wu X +6 more
europepmc +2 more sources
Археология евразийских степей, 2021 In 1894, the Museum of Classical Archeology of the Academy of Sciences was liquidated, and all its collections were transferred to the Hermitage. Documents revealed in the Russian State Historical Archives indicate that the Cabinet of Fine Arts of the ...
Victoria V. Onoshchenko +1 more
doaj +1 more source
Critical residue properties for potency and selectivity of α-Conotoxin RgIA towards α9α10 nicotinic acetylcholine receptors. [PDF]
Biochem Pharmacol, 2020 The α9α10 nicotinic acetylcholine receptor (nAChR) has been characterized as an effective anti-pain target that functions through a non-opioid mechanism. However, as a pentameric ion channel comprised of two different subunits, the specific targeting of α9α10 nAChRs has proven challenging.
Huynh PN +4 more
europepmc +7 more sources