Corrigendum: Crystal structure of the monomeric extracellular domain of α9 nicotinic receptor subunit in complex with α-conotoxin RgIA: Molecular dynamics insights into RgIA binding to α9α10 nicotinic receptors [PDF]
Frontiers in Pharmacology, 2022 Marios Zouridakis +9 more
doaj +3 more sources
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.
J Michael McIntosh +2 more
exaly +4 more sources
Discovery of Methylene Thioacetal-Incorporated α-RgIA Analogues as Potent and Stable Antagonists of the Human α9α10 Nicotinic Acetylcholine Receptor for the Treatment of Neuropathic Pain [PDF]
Journal of Medicinal Chemistry, 2021 α9-Containing nicotinic acetylcholine receptors (nAChRs) are key targets for the treatment of neuropathic pain. α-Conotoxin RgIA4 is a peptide antagonist of human α9α10 nAChRs with high selectivity. However, structural rearrangement reveals a potential liability for clinical applications.
Danny Hung-Chieh Chou +2 more
exaly +5 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
Hafiz Majid Mahmood +2 more
exaly +5 more sources
d-Amino Acid Substitution of α-Conotoxin RgIA Identifies its Critical Residues and Improves the Enzymatic Stability [PDF]
Marine Drugs, 2019 α-Conotoxin RgIA is a selective and potent competitive antagonist of rat α9α10 nicotinic acetylcholine receptors (nAChR), but it is much less potent towards human α9α10 nAChR.
Jie Ren +8 more
doaj +3 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
On the issue of studying Siberian merchant class: the circle of social contacts of gold producer Yakov Frizer [PDF]
Омский научный вестник: Серия "Общество. История. Современность", 2020 The research is dedicated to Siberian merchant Yakov Frizer, a range of his communication and social contacts. Present research targets to illustrate through Frizer example particularities of everyday life and activity of the Siberian merchants on the
I. Vladimirsky, M. V. Krotova
doaj +1 more source
The Concise Guide to PHARMACOLOGY 2023/24: Ion channels
British Journal of Pharmacology, Volume 180, Issue S2, Page S145-S222, October 2023., 2023 The Concise Guide to PHARMACOLOGY 2023/24 is the sixth in this series of biennial publications. The Concise Guide provides concise overviews, mostly in tabular format, of the key properties of approximately 1800 drug targets, and over 6000 interactions with about 3900 ligands. There is an emphasis on selective pharmacology (where available), plus links
Stephen P. H. Alexander +72 more
wiley +1 more source