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 |
|---|---|
| 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 |
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Keywords
- α-Conotoxins
- Competitive antagonists
- Nicotinic acetylcholine receptors
Cite this
}
α-Conotoxins. / Arias, Hugo R.; Blanton, Michael P.
In: International Journal of Biochemistry and Cell Biology, Vol. 32, No. 10, 04.12.2000, p. 1017-1028.Research output: Contribution to journal › Review article
TY - JOUR
T1 - α-Conotoxins
AU - Arias, Hugo R.
AU - Blanton, Michael P.
PY - 2000/12/4
Y1 - 2000/12/4
N2 - 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.
AB - 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.
KW - α-Conotoxins
KW - Competitive antagonists
KW - Nicotinic acetylcholine receptors
UR - http://www.scopus.com/inward/record.url?scp=0033714035&partnerID=8YFLogxK
U2 - 10.1016/S1357-2725(00)00051-0
DO - 10.1016/S1357-2725(00)00051-0
M3 - Review article
C2 - 11091135
AN - SCOPUS:0033714035
VL - 32
SP - 1017
EP - 1028
JO - International Journal of Biochemistry and Cell Biology
JF - International Journal of Biochemistry and Cell Biology
SN - 1357-2725
IS - 10
ER -