Results 111 to 120 of about 396 (138)
The Conopeptide αD-FrXXA, an Inhibitor of Voltage-Gated Potassium Channels. [PDF]
Mar DrugsMartínez-Hernández L +3 more
europepmc +1 more source
Sea Anemone-Derived Toxin Avd3i Inhibited Sodium Channel Nav1.4. [PDF]
Toxins (Basel)Gao J +6 more
europepmc +1 more source
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.
Richard J Clark +2 more
exaly +6 more sources
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Biochimie, 2022
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 ...
V A Kazakov, Yuri N Utkin, V I Tsetlin
exaly +3 more sources
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 ...
V A Kazakov, Yuri N Utkin, V I Tsetlin
exaly +3 more sources
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.
Layla Azam, J Michael Mcintosh
exaly +3 more sources
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 ...
Sandeep Chhabra +2 more
exaly +6 more sources
Experimental Neurology, 2016
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 ...
Alessandra Pacini +2 more
exaly +3 more sources
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 ...
Alessandra Pacini +2 more
exaly +3 more sources
α-Conotoxin RgIA protects against the development of nerve injury-induced chronic pain and prevents both neuronal and glial derangement [PDF]
Pain, 2014 Neuropathic pain affects millions of people worldwide, causing substantial disability and greatly impairing quality of life. Commonly used analgesics or antihyperalgesic compounds are generally characterized by limited therapeutic outcomes. Thus, there is a compelling need for novel therapeutic strategies able to prevent nervous tissue alterations ...
Lorenzo Di Cesare Mannelli +2 more
exaly +4 more sources
Journal of Molecular Graphics and Modelling, 2019
The α9α10 nicotinic acetylcholine receptor (nAChR) is an effective therapeutic target for neuropathic pain. α-Conotoxin RgIA and Vc1.1 are two well-known peptides blocking α9α10 nAChR potently and selectively, which have been extensively investigated as drug candidates. Several key residues were established in previous experimental research.
Sulan Luo
exaly +3 more sources
The α9α10 nicotinic acetylcholine receptor (nAChR) is an effective therapeutic target for neuropathic pain. α-Conotoxin RgIA and Vc1.1 are two well-known peptides blocking α9α10 nAChR potently and selectively, which have been extensively investigated as drug candidates. Several key residues were established in previous experimental research.
Sulan Luo
exaly +3 more sources