PeIA[V10I] (P08965) Protein Card

General Information
Name PeIA[V10I] (named by ConoServer)
Alternative name(s) [Ile10]PeIA
Organism synthetic construct
Protein Type Synthetic
Parent PeIA

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

Sequence
GCCSHPACSINHPELC(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. norvegicus11.8 nM[10.2-13.6]ACh(100 uM)Hone,A.J. et al. (2019)
α3β4R. norvegicus3.47 μM[2.3-5.24]ACh(300 μM)Hone,A.J. et al. (2020)
α6/α3β2β3R. norvegicus13.4 nM[10.9-16.6]ACh(100 uM)Hone,A.J. et al. (2019)
α6/α3β4H. sapiens9.24 nM[8.45-10.1]300 uM AChHone,A.J. et al. (2021)
R. norvegicus308 nM[294-322]300 uM AChHone,A.J. et al. (2021)

References
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

Tools