PeIA[A7V,S9H,V10A,N11R,E14A] (P06804) Protein Card

General Information
Name PeIA[A7V,S9H,V10A,N11R,E14A]
Alternative name(s) PeIA-5069
Organism synthetic construct
Protein Type Synthetic
Parent PeIA

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

Sequence
GCCSHPVCHARHPALC(nh2)
Modified residues
positionsymbolname
17nh2C-term amidation
Sequence evidence Unknown
Average Mass 1685.97
Monoisotopic Mass 1684.69
Isoelectric Point 11.16
Extinction Coefficient [280nm] NA

Activity

IC50: Nicotinic acetylcholine receptors

TargetOrganismIC50AgonistRef
α3β2R. norvegicus(a3 mutant [K152E)18.2 nM+/-3.2100 uM AchHone,A.J. et al. (2013)
(E184D)30.9 uM+/-9.7100 uM AchHone,A.J. et al. (2013)
α3β4R. norvegicus(Q195T] )> 10 uM100 uM AchHone,A.J. et al. (2013)
α4β2R. norvegicus> 10 uM100 uM AchHone,A.J. et al. (2013)
α4β4R. norvegicus> 10 uM100 uM AchHone,A.J. et al. (2013)
α6β4R. norvegicus43.8 nM+/-6.9100 uM AchHone,A.J. et al. (2013)
α6/α3β2β3R. norvegicus2.16 nM+/-0.18100 uM AchHone,A.J. et al. (2013)
311 nM+/-117100 uM AchHone,A.J. et al. (2013)
5.5 uM+/-3.1100 uM AchHone,A.J. et al. (2013)
α7R. norvegicus> 10 uM200 uM AchHone,A.J. et al. (2013)

References
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., 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