Peptide Information

General Information of This Peptide
Peptide ID
BTDP006985
Peptide Name
Alpha-conotoxin PeIA
Species
Conus pergrandis (Grand cone)
Uniprot Name
CA1A_CONPR
Alphafold ID
Q1L777
3D Structure
Download
2D Sequence
3D Structure
Source
RSCB PDB: 5JME
Sequence
FDGRNAAANDKASDLVALTVRGCCSHPACSVNHPELCG
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Sequence Length
38
Mass (Da)
3900
Sequence Removed Signal Peptide
FDGRNAAANDKASDLVALTVRGCCSHPACSVNHPELCG
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Disulfide Bond
23-29;24-37
PDB ID
5JME
        Click to Show/Hide the Complete Species Lineage
Kingdom: Metazoa
Phylum: Mollusca
Class: Gastropoda
Order: Neogastropoda
Family: Conidae
Genus: Conus
Species: Conus pergrandis
Full List of Activity Data of This Peptide Toxin
                        Target Name Activity Data Type Activity Data Concentration Note Reference
 Target Info    nAChR alpha-6/alpha-3-beta-4 IC50
0.2 nM
 .
Mutant PeIA-5667 [A28V, S30N, N11R, L36I]
 [1- 9]
 Target Info    nAChR alpha-6/alpha-3-beta-4 IC50
0.4 nM
 .
Mutant PeIA-5667 [A28V, S30N, N11R, L36I]
 [1- 9]
 Target Info    Ca2.2 IC50
1.1 nM
 .
Via G protein-coupled GABA(B) receptor
 [1- 9]
 Target Info    nAChR alpha-3-beta-4 IC50
3.7 nM
 .
Mutant [A28V, S30H, V31A, N32R, E35A]
 [1- 9]
 Target Info    nAChR alpha-6/alpha-3-beta-2-beta-3 IC50
3.8 nM
 .
Mutant [A28V, S30H, V31A, N32R, E35A]
 [1- 9]
 Target Info    nAChR alpha-3-beta-2 IC50
6.1 nM
 .
Mutant [A28V, S30H, V31A, N32R, E35A]
 [1- 9]
 Target Info    nAChR beta-3-alpha-6-beta-2-alpha-4-beta-2 IC50
6.3 nM
 .
Mutant [A28V, S30H, V31A, N32R, E35A]
 [1- 9]
 Target Info    nAChR alpha-6/alpha-3-beta-4 IC50
6.75 nM
 .
Mutant [A28V, S30H, V31A, N32R, E35A]
 [1- 9]
 Target Info    nAChR alpha-9-alpha-10 IC50
6.9 - 54.9 nM
 .
Mutant [A28V, S30H, V31A, N32R, E35A]
 [1- 9]
 Target Info    nAChR beta-4-alpha-3-beta-4-alpha-3-alpha-5 IC50
9.2 nM
 .
Mutant [A28V, S30H, V31A, N32R, E35A]
 [1- 9]
 Target Info    nAChR alpha-3-beta-2 IC50
9.7 - 97.5 nM
 .
Mutant [A28V, S30H, V31A, N32R, E35A]
 [1- 9]
 Target Info    nAChR alpha-6/alpha-3-beta-2-beta-3 IC50
11.1 - 17.2 nM
 .
Mutant [A28V, S30H, V31A, N32R, E35A]
 [1- 9]
 Target Info    nAChR alpha-6/alpha-3-beta-2-beta-3 IC50
111 - 135 nM
 .
Mutant PeIA-5667 [A28V, S30N, N11R, L36I]
 [1- 9]
 Target Info    nAChR alpha-6/alpha-3-beta-2-beta-3 IC50
111 - 135 nM
 .
Mutant PeIA-5667 [A28V, S30N, N11R, L36I]
 [1- 9]
 Target Info    nAChR alpha-6/alpha-3-beta-4 IC50
130 - 147 nM
 .
Mutant [A28V, S30H, V31A, N32R, E35A]
 [1- 9]
 Target Info    nAChR alpha-3-beta-4 IC50
179 - 230 nM
 .
Mutant PeIA-5667 [A28V, S30N, N11R, L36I]
 [1- 9]
 Target Info    nAChR alpha-3-beta-4 IC50
179 - 230 nM
 .
Mutant PeIA-5667 [A28V, S30N, N11R, L36I]
 [1- 9]
 Target Info    nAChR alpha-3-beta-4 IC50
0.480 - 1.5 μM
 .
Mutant [A28V, S30H, V31A, N32R, E35A]
 [1- 9]
References
Ref 1 A novel alpha-conotoxin, PeIA, cloned from Conus pergrandis, discriminates between rat alpha9alpha10 and alpha7 nicotinic cholinergic receptors. J Biol Chem. 2005 Aug 26;280(34):30107-12. doi: 10.1074/jbc.M504102200. Epub 2005 Jun 27.
Ref 2 Structure and activity of alpha-conotoxin PeIA at nicotinic acetylcholine receptor subtypes and GABA(B) receptor-coupled N-type calcium channels. J Biol Chem. 2011 Mar 25;286(12):10233-7. doi: 10.1074/jbc.M110.196170. Epub 2011 Jan 20.
Ref 3 -Conotoxin PeIA[S9H,V10A,E14N] potently and selectively blocks 623 versus 64 nicotinic acetylcholine receptors. Mol Pharmacol. 2012 Nov;82(5):972-82. doi: 10.1124/mol.112.080853. Epub 2012 Aug 22.
Ref 4 Positional scanning mutagenesis of -conotoxin PeIA identifies critical residues that confer potency and selectivity for 6/323 and 32 nicotinic acetylcholine receptors. J Biol Chem. 2013 Aug 30;288(35):25428-25439. doi: 10.1074/jbc.M113.482059. Epub 2013 Jul 11.
Ref 5 -Conotoxins Identify the 34* Subtype as the Predominant Nicotinic Acetylcholine Receptor Expressed in Human Adrenal Chromaffin Cells. Mol Pharmacol. 2015 Nov;88(5):881-93. doi: 10.1124/mol.115.100982. Epub 2015 Sep 1.
Ref 6 Correction to "-Conotoxins Identify the 34* Subtype as the Predominant Nicotinic Acetylcholine Receptor Expressed in Human Adrenal Chromaffin Cells". Mol Pharmacol. 2016 Feb;89(2):322. doi: 10.1124/mol.115.100982err.
Ref 7 Inhibition of cholinergic pathways in Drosophila melanogaster by -conotoxins. FASEB J. 2015 Mar;29(3):1011-8. doi: 10.1096/fj.14-262733. Epub 2014 Dec 2.
Ref 8 Dimerization of -Conotoxins as a Strategy to Enhance the Inhibition of the Human 7 and 910 Nicotinic Acetylcholine Receptors. J Med Chem. 2020 Mar 26;63(6):2974-2985. doi: 10.1021/acs.jmedchem.9b01536. Epub 2020 Mar 17.
Ref 9 Computational and Functional Mapping of Human and Rat 64 Nicotinic Acetylcholine Receptors Reveals Species-Specific Ligand-Binding Motifs. J Med Chem. 2021 Feb 11;64(3):1685-1700. doi: 10.1021/acs.jmedchem.0c01973. Epub 2021 Feb 1.
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