PeIA[V10A] (P05853) Protein Card

General Information
Name PeIA[V10A]
Alternative name(s) [Ala10]PeIA
Organism synthetic construct
Protein Type Synthetic
Parent PeIA

Classification
Conopeptide class conotoxin
Gene superfamily
Cysteine framework I
Pharmacological family alpha conotoxin

Sequence
GCCSHPACSANHPELC(nh2)
Modified residues
positionsymbolname
17nh2C-term amidation
Average Mass 1623.81
Monoisotopic Mass 1622.58
Isoelectric Point 6.81
Extinction Coefficient [280nm] NA

Activity

IC50: Nicotinic acetylcholine receptors

TargetOrganismIC50AgonistRef
α3β2R. norvegicus2.2nM+/-0.3100uM AchHone,A.J. et al. (2012)
3.37 nM[3.05-3.72]Ach (100 uM)Hone,A.J. et al. (2019)
α3β4R. norvegicus2.7uM+/-0.5100uM AchHone,A.J. et al. (2012)
α6/α3β2β3R. norvegicus2.4nM+/-0.3100uM AchHone,A.J. et al. (2012)
α6/α3β4H. sapiens22.1 nM[19-25.6]300 uM AChHone,A.J. et al. (2021)
R. norvegicus302nM+/-28100uM AchHone,A.J. et al. (2012)
137 nM[111-168]300 uM AChHone,A.J. et al. (2021)

References
Hone,A.J., Scadden,M., Gajewiak,J., Christensen,S., Lindstrom,J. and McIntosh,J.M. (2012) α-Conotoxin PeIA[S9H,V10A,E14N] potently and selectively blocks α6β2β3 versus α6β4 nicotinic acetylcholine receptors. Mol. Pharmacol. 82:972-982
Hone,A.J., Ruiz,M., Scadden,M., Christensen,S., Gajewiak,J., Azam,L. and McIntosh,J.M. (2013) Positional scanning mutagenesis of α-conotoxin PeIA identifies critical residues that confer potency and selectivity for α6/α3β2β3 and α3β2 nicotinic acetylcholine receptors. J. Biol. Chem. 288:25428-25439
Hone,A.J., Fisher,F., Christensen,S., Gajewiak,J., Larkin,D., Whiteaker,P. and McIntosh,J.M. (2019) PeIA-5466: A Novel Peptide Antagonist Containing Non-natural Amino Acids That Selectively Targets α3β2 Nicotinic Acetylcholine Receptors J. Med. Chem. 62:6262-6275
Hone,A.J., Kaas,Q., Kearns,I., Hararah,F., Gajewiak,J., Christensen,S., Craik,D.J. and McIntosh,J.M. (2021) Computational and Functional Mapping of Human and Rat α6β4 Nicotinic Acetylcholine Receptors Reveals Species-Specific Ligand-Binding Motifs. J Med Chem 64:1685-1700

Internal links
Nucleic acids
Structure

External links

Tools