PeIA[E14(Gla)] (P08972) Protein Card

General Information
Name PeIA[E14(Gla)] (named by ConoServer)
Alternative name(s) [Gla14]PeIA
Organism synthetic construct
Protein Type Synthetic
Parent PeIA

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

Sequence
GCCSHPACSVNHP(Gla)LC(nh2)
Modified residues
positionsymbolname
14GlaGamma carboxylic glutamic acid
17nh2C-term amidation
Sequence evidence Unknown
Average Mass 1695.87
Monoisotopic Mass 1694.60
Isoelectric Point 6.79
Extinction Coefficient [280nm] NA

Activity

IC50: Nicotinic acetylcholine receptors

TargetOrganismIC50AgonistRef
α3β2R. norvegicus16.6 nM[15.1-18.4]Ach (100 uM)Hone,A.J. et al. (2019)
α6/α3β2β3R. norvegicus28.5 nM[25.7-31.6]Ach (100 uM)Hone,A.J. et al. (2019)
α6/α3β4H. sapiens18.2 nM[14.9-24.4]300 uM AChHone,A.J. et al. (2021)
R. norvegicus430 nM[374-495]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., 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