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alpha Conotoxins Nicotinic Acetylcholine Receptor Antagonists as Pharmacological Tools and Potential Drug Leads

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Abstract:

a-Conotoxins are small disulfide rich peptides from the venoms of marine cone snails. They target specific nicotinic acetylcholine receptor (nAChR) subtypes with high affinity and potency and are therefore valuable as neuropharmacological probes and potential drug leads. This article gives a general overview of the chemical and biological features of a-conotoxins, including their pharmacology, binding interactions and structure. A detailed analysis of recently reported three-dimensional structures from members of different subfamilies of the a-conotoxins, including those with 3/5, 4/3, 4/6 and 4/7 spacings of their two intracysteine loops is given. The structures are generally well defined and represent useful frameworks for the display of amino acid residues to target molecules.

Keywords: ACh evoked currents; Nicotinic Acetylcholine; autoimmune disease; conotoxins; intra cystein resdues; ligands gated; nuclear magnetic; potential drug leads

Document Type: Review Article

DOI: http://dx.doi.org/10.2174/0929867013373453

Publication date: March 1, 2001

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  • Current Medicinal Chemistry covers all the latest and outstanding developments in medicinal chemistry and rational drug design. Each issue contains a series of timely in-depth reviews written by leaders in the field covering a range of the current topics in medicinal chemistry. Current Medicinal Chemistry is an essential journal for every medicinal chemist who wishes to be kept informed and up-to-date with the latest and most important developments.
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