Abstract
α-Conotoxins (α-CgTxs) are a family of Cys-enriched peptides found in several marine snails from the genus Conus. These small peptides behave pharmacologically as competitive antagonists of the nicotinic acetylcholine receptor (AChR). The data indicate that (1) α-CgTxs are able to discriminate between muscle- and neuronal-type AChRs and even among distinct AChR subtypes; (2) the binding sites for α-CgTxs are located, like other cholinergic ligands, at the interface of α and non-α subunits (γ, δ, and ε for the muscle-type AChR, and β for several neuronal-type AChRs); (3) some α-CgTxs differentiate the high- from the low-affinity binding site found on either α/non-α subunit interface; and that (4) specific residues in the cholinergic binding site are energetically coupled with their corresponding pairs in the toxin stabilizing the α-CgTx-AChR complex. The α-CgTxs have proven to be excellent probes for studying the structure and function of the AChR family. (C) 2000 Elsevier Science Ltd.
Original language | English |
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Pages (from-to) | 1017-1028 |
Number of pages | 12 |
Journal | International Journal of Biochemistry and Cell Biology |
Volume | 32 |
Issue number | 10 |
DOIs | |
State | Published - 4 Dec 2000 |
Externally published | Yes |
Keywords
- α-Conotoxins
- Competitive antagonists
- Nicotinic acetylcholine receptors