Rational Design of Potent α-Conotoxin PeIA Analogues with Non-Natural Amino Acids for the Inhibition of Human α9α10 Nicotinic Acetylcholine Receptors. [PDF]
Mar DrugsLi T +7 more
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The Conopeptide αD-FrXXA, an Inhibitor of Voltage-Gated Potassium Channels. [PDF]
Mar DrugsMartínez-Hernández L +3 more
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Deep learning-driven discovery and mechanism of action study of a minimalist conopeptide targeting <i>α</i>7 nicotinic acetylcholine receptor. [PDF]
Acta Pharm Sin BZhang J +9 more
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The three-dimensional structure of the analgesic α-conotoxin, RgIA [PDF]
FEBS Letters, 2008 The α‐conotoxin RgIA is a selective antagonist of the α9α10 nicotinic acetylcholine receptor and has been shown to be a potent analgesic and reduces nerve injury associated inflammation. RgIA was chemically synthesized and found to fold into two disulfide isomers, globular and ribbon.
Norelle L Daly +2 more
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Оligoarginines were recently discovered (Lebedev et al., 2019 Nov) as a novel class of nicotinic acetylcholine receptors (nAChRs) inhibitors, octaoligoarginine R8 showing a relatively high affinity (44 nM) for the α9/α10 nAChR. Since the inhibition of α9/α10 nAChR by α-conotoxin RgIA and its analogs is a possible way to drugs against neuropathic pain ...
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Molecular Interaction of α-Conotoxin RgIA with the Rat α9α10 Nicotinic Acetylcholine Receptor [PDF]
Molecular Pharmacology, 2015 The α9α10 nicotinic acetylcholine receptor (nAChR) was first identified in the auditory system, where it mediates synaptic transmission between efferent olivocochlear cholinergic fibers and cochlea hair cells. This receptor gained further attention due to its potential role in chronic pain and breast and lung cancers.
Marios Zouridakis +2 more
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Molecular basis for the differential sensitivity of rat and human α9α10 nAChRs to α-conotoxin RgIA. [PDF]
Journal of Neurochemistry, 2012 J. Neurochem. (2012) 122, 1137–1144.AbstractThe α9α10 nicotinic acetylcholine receptor (nAChR) may be a potential target in pathophysiology of the auditory system, chronic pain, and breast and lung cancers. Alpha‐conotoxins, from the predatory marine snail Conus, are potent nicotinic antagonists, some of which are selective for the α9α10 nAChR.
J Michael McIntosh, Layla Azam
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Dicarba Analogues of α-Conotoxin RgIA. Structure, Stability, and Activity at Potential Pain Targets
Journal of Medicinal Chemistry, 2014α-Conotoxin RgIA is both an antagonist of the α9α10 nicotinic acetylcholine receptor (nAChR) subtype and an inhibitor of high-voltage-activated N-type calcium channel currents. RgIA has therapeutic potential for the treatment of pain, but reduction of the disulfide bond framework under physiological conditions represents a potential liability for ...
Peter Bartels +2 more
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Oxaliplatin, a third-generation diaminocyclohexane platinum drug, is widely used alone or in combination with 5-fluorouracil and leucovorin to treat metastatic colorectal, ovarian, and pancreatic cancers. Oxaliplatin long-term treatment is associated with the development of a dose-limiting painful neuropathy that dramatically impairs the patient's ...
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