PeIA[V10L] (P06796) Protein Card

General Information
Name PeIA[V10L]
Alternative name(s) [Leu10]PeIA
Organism synthetic construct
Protein Type Synthetic
Parent PeIA

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

Sequence
GCCSHPACSLNHPELC(nh2)
Modified residues
positionsymbolname
17nh2C-term amidation
Sequence evidence Unknown
Average Mass 1665.89
Monoisotopic Mass 1664.63
Isoelectric Point 6.81
Extinction Coefficient [280nm] NA

Activity

IC50: Nicotinic acetylcholine receptors

TargetOrganismIC50AgonistRef
α3β2R. norvegicus3.81 nM+/-0.95Ach (100 μM)Hone,A.J. et al. (2013)
10.6 nM[9.2-12.2]Ach (100 μM)Hone,A.J. et al. (2019)
α3β4R. norvegicus0.87 μM[0.71-1.05]Ach (300 μM)Hone,A.J. et al. (2020)
α6β3β4H. sapiens9.64 nM[8.56-10.9]300 uM AChHone,A.J. et al. (2021)
R. norvegicus63.8 nM[56.5-72.1]300 uM AChHone,A.J. et al. (2021)
α6/α3β2β3R. norvegicus18.8 nM+/-3Ach (100 μM)Hone,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., 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., Rueda-Ruzafa,L., Gordon,T.J., Gajewiak,J., Christensen,S., Dyhring,T., Albillos,A. and McIntosh,J.M. (2020) Expression of α3β2β4 nicotinic acetylcholine receptors by rat adrenal chromaffin cells determined using novel conopeptide antagonists J Neurochem
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

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