PeIA[S9H] (P05852) Protein Card

General Information
Name PeIA[S9H]
Alternative name(s) [His9]PeIA
Organism synthetic construct
Protein Type Synthetic
Parent PeIA

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

Sequence
GCCSHPACHVNHPELC(nh2)
Modified residues
positionsymbolname
17nh2C-term amidation
Average Mass 1701.92
Monoisotopic Mass 1700.64
Isoelectric Point 7.10
Extinction Coefficient [280nm] NA

Activity

IC50: Nicotinic acetylcholine receptors

TargetOrganismIC50AgonistRef
α3β2R. norvegicus1.30 nM[1.19-1.41]Ach (100 uM)Hone,A.J. et al. (2019)
713pM+/-347100uM AchHone,A.J. et al. (2012)
α3β4R. norvegicus66nM+/-18100uM AchHone,A.J. et al. (2012)
α6/α3β2β3R. norvegicus991pM+/-63100uM AchHone,A.J. et al. (2012)
α6/α3β4H. sapiens2.90 nM[2.35-3.57]300 uM AChHone,A.J. et al. (2021)
R. norvegicus14.5nM+/-4.1100uM AchHone,A.J. et al. (2012)
18.3 nM[13.9-24]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., 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