Rational Design of Potent α-Conotoxin PeIA Analogues with Non-Natural Amino Acids for the Inhibition of Human α9α10 Nicotinic Acetylcholine Receptors [PDF]
Marine Drugsα-Conotoxins (α-CTxs) are structurally related peptides that antagonize nicotinic acetylcholine receptors (nAChRs), which may serve as new alternatives to opioid-based treatment for pain-related conditions.
Tianmiao Li +7 more
doaj +2 more sources
α-Conotoxin Decontamination Protocol Evaluation: What Works and What Doesn’t [PDF]
Toxins, 2017 Nine publically available biosafety protocols for safely handling conotoxin peptides were tested to evaluate their decontamination efficacy. Circular dichroism (CD) spectroscopy and mass spectrometry (MS) were used to assess the effect of each chemical ...
Matthew W. Turner +2 more
doaj +2 more sources
Cloning, Synthesis and Functional Characterization of a Novel α-Conotoxin Lt1.3 [PDF]
Marine Drugs, 2018 α-Conotoxins (α-CTxs) are small peptides composed of 11 to 20 amino acid residues with two disulfide bridges. Most of them potently and selectively target nicotinic acetylcholine receptor (nAChR) subtypes, and a few were found to inhibit the GABAB ...
Jinqin Chen +7 more
doaj +2 more sources
Rationally Designed α-Conotoxin Analogues Maintained Analgesia Activity and Weakened Side Effects [PDF]
Molecules, 2019 A lack of specificity is restricting the further application of conotoxin from Conus bullatus (BuIA). In this study, an analogue library of BuIA was established and virtual screening was used, which identified high α7 nicotinic acetylcholine ...
Chen Liu +9 more
doaj +2 more sources
Blockade of neuronal α7-nAChR by α-conotoxin ImI explained by computational scanning and energy calculations. [PDF]
PLoS Computational Biology, 2011 α-Conotoxins potently inhibit isoforms of nicotinic acetylcholine receptors (nAChRs), which are essential for neuronal and neuromuscular transmission.
Rilei Yu, David J Craik, Quentin Kaas
doaj +1 more source
Marine Drugs, 2020 Several biochemical mechanisms, including the arachidonic acid cascade and activation of nicotinic acetylcholine receptors (nAChRs), are involved in increased tumor survival. Combined application of inhibitors acting on these two pathways may result in a
Alexey V. Osipov +6 more
doaj +1 more source
Molecular docking study on the α3β2 neuronal nicotinic acetylcholine receptor complexed with α-Conotoxin GIC [PDF]
BMB Reports, 2012 Nicotinic acetylcholine receptors (nAChRs) are a diverse familyof homo- or heteropentameric ligand-gated ion channels.Understanding the physiological role of each nAChR subtypeand the key residues responsible for normal and pathologicalstates is ...
Chewook Lee +3 more
doaj +1 more source
Residues Responsible for the Selectivity of α-Conotoxins for Ac-AChBP or nAChRs
Marine Drugs, 2016 Nicotinic acetylcholine receptors (nAChRs) are targets for developing new drugs to treat severe pain, nicotine addiction, Alzheimer disease, epilepsy, etc. α-Conotoxins are biologically and chemically diverse. With 12–19 residues and two disulfides, they
Bo Lin, Shihua Xiang, Mengsen Li
doaj +1 more source
Design of New α-Conotoxins: From Computer Modeling to Synthesis of Potent Cholinergic Compounds
Marine Drugs, 2011 A series of 14 new analogs of α-conotoxin PnIA Conus pennaceus was synthesized and tested for binding to the human α7 nicotinic acetylcholine receptor (nAChR) and acetylcholine-binding proteins (AChBP) Lymnaea stagnalis and Aplysia californica.
Alexey Y. Khruschov +3 more
doaj +1 more source
Marine Drugs, 2023 Conotoxins are a class of disulfide-rich peptides found in the venom of cone snails, which have attracted considerable attention in recent years due to their potent activity on ion channels and potential for therapeutics.
Yong Wu +6 more
doaj +1 more source