Evidence 1
Activity
Activity
Neurotoxin
FUNCTION: Alpha-conotoxins act on postsynaptic membranes, they bind to the nicotinic acetylcholine receptors (nAChR) and thus inhibit them. This toxin blocks mammalian alpha-3-beta-2/CHRNA3-CHRNB2 (IC(50)=7-68 nM) and alpha-7/CHRNA7 (IC(50)=253 nM) nAChRs (PubMed:10545176, PubMed:15929983, PubMed:22024738, PubMed:25101833, PubMed:8068627). It also shows a high inhibition on alpha-6/alpha-3-beta-2-beta-3 (CHRNA6/CHRNA3-CHRNB2-CHRNB3) (IC(50)=11 nM) and a low inhibition on alpha-6-beta-4/CHRNA4-CHRNB4 (IC(50)>500 nM) (PubMed:22024738). It interacts with a hydrophobic pocket between two acetylcholine receptor subunits. In vivo, inhibits Ehrlich carcinoma growth and increase mouse survival (PubMed:32272633). These effects are greatly enhanced when the toxin is applied with the selective 12-lipoxygenase inhibitor baicalein (PubMed:32272633). {ECO:0000269|PubMed:10545176, ECO:0000269|PubMed:12734390, ECO:0000269|PubMed:15929983, ECO:0000269|PubMed:22024738, ECO:0000269|PubMed:25101833, ECO:0000269|PubMed:8068627}.
Target
nicotinic acetylcholine receptor (nAChR)
acetylcholine receptor
Source & Reference
NA
UniProtKB/Swiss-Prot Tox-Prot
Other
Conus pennaceus (Feathered cone) (Conus episcopus)
Neurotoxin
Postsynaptic neurotoxin
Acetylcholine receptor inhibiting toxin
Ion channel impairing toxin
Alpha-conotoxins act on postsynaptic membranes, they bind to the nicotinic acetylcholine receptors (nAChR) and thus inhibit them. This toxin blocks mammalian alpha-3-beta-2/CHRNA3-CHRNB2 (IC(50)=7-68 nM) and alpha-7/CHRNA7 (IC(50)=253 nM) nAChRs (PubMed:10545176, PubMed:15929983, PubMed:22024738, PubMed:25101833, PubMed:8068627).
Alpha-conotoxin PnIA (Alpha-PnIA)
cone snail
Conotoxin A superfamily
Evidence at protein level
3D-structure
Acetylcholine receptor inhibiting toxin
Amidation
Direct protein sequencing
Disulfide bond
Ion channel impairing toxin
Neurotoxin
Postsynaptic neurotoxin
Secreted
Sulfation
Toxin
TISSUE SPECIFICITY: Expressed by the venom duct. {ECO:0000305|PubMed:8068627}.