Design of New α-Conotoxins: From Computer Modeling to Synthesis of Potent Cholinergic Compounds [PDF]
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
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Computational Design of α-Conotoxins to Target Specific Nicotinic Acetylcholine Receptor Subtypes. [PDF]
Chemistry, 2023 Nicotinic acetylcholine receptors (nAChRs) are drug targets for neurological diseases and disorders, but selective targeting of the large number of nAChR subtypes is challenging.
Wu X +6 more
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Posttranslational modifications of α-conotoxins: sulfotyrosine and C-terminal amidation stabilise structures and increase acetylcholine receptor binding. [PDF]
RSC Med Chem, 2021 Conotoxins are peptides found in the venoms of marine cone snails. They are typically highly structured and stable and have potent activities at nicotinic acetylcholine receptors, which make them valuable research tools and promising lead molecules for ...
Ho TNT +8 more
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Pharmacological Research, 2023 The pentameric nicotinic acetylcholine receptors (nAChRs) are typically classed as muscle- or neuronal-type, however, the latter has also been reported in non-neuronal cells.
Han-Shen Tae, David J. Adams
doaj +2 more sources
Prediction of Specificity of α-Conotoxins to Subtypes of Human Nicotinic Acetylcholine Receptors with Semi-supervised Machine Learning. [PDF]
ACS Chem NeurosciConotoxins are a family of highly toxic neurotoxins composed of cysteine-rich peptides produced by marine cone snails. The most lethal cone snail species to humans is Conus geographus, with fatality rates of up to ∼65% from a single sting, which is ...
Do HN +2 more
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On-resin strategy to label α-conotoxins: Cy5-RgIA, a potent α9α10 nicotinic acetylcholine receptor imaging probe. [PDF]
Aust J Chem, 2020 In-solution conjugation is the most commonly used strategy to label peptides and proteins with fluorophores. However, lack of site-specific control and high costs of fluorophores are recognised limitations of this approach.
Muttenthaler M +5 more
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Synthesis, Structure and Biological Activity of CIA and CIB, Two α-Conotoxins from the Predation-Evoked Venom of Conus catus. [PDF]
Toxins (Basel), 2018 Cone snails produce a fast-acting and often paralyzing venom that is usually injected into their prey or predator through a hypodermic needle-like modified radula tooth.
Giribaldi J +9 more
europepmc +2 more sources
Role of CysI-CysIII Disulfide Bond on the Structure and Activity of α-Conotoxins at Human Neuronal Nicotinic Acetylcholine Receptors. [PDF]
ACS Omega, 2017 α-Conotoxins preferentially antagonize muscle and neuronal nicotinic acetylcholine receptors (nAChRs). Native α-conotoxins have two disulfide links, CI–CIII and CII–CIV, and owing to the inherent properties of disulfide bonds, α-conotoxins have been ...
Tabassum N +6 more
europepmc +2 more sources
Key Structural Determinants in the Agonist Binding Loops of Human β2 and β4 Nicotinic Acetylcholine Receptor Subunits Contribute to α3β4 Subtype Selectivity of α-Conotoxins. [PDF]
J Biol Chem, 2016 α-Conotoxins represent a large group of pharmacologically active peptides that antagonize nicotinic acetylcholine receptors (nAChRs). The α3β4 nAChR, a predominant subtype in the peripheral nervous system, has been implicated in various ...
Cuny H +4 more
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Structural similarities reveal an expansive conotoxin family with a two-finger toxin fold. [PDF]
Protein SciAbstract Venomous animals have evolved a diverse repertoire of toxins with considerable pharmaceutical potential. The rapid evolution of peptide toxins, such as the conotoxins produced by venomous marine cone snails, often complicates efforts to infer their evolutionary relationships based solely on sequence information.
Khilji MS +11 more
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