PeIA[N11(Api)] (P08970) Protein Card

General Information
Name PeIA[N11(Api)] (named by ConoServer)
Alternative name(s) [Api11]PeIA
Organism synthetic construct
Protein Type Synthetic
Parent PeIA

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

Sequence
GCCSHPACSV(Api)HPELC(nh2)
Modified residues
positionsymbolname
11Apialpha-aminopimelic acid
17nh2C-term amidation
Sequence evidence Unknown
Average Mass 1712.94
Monoisotopic Mass 1711.66
Isoelectric Point 6.81
Extinction Coefficient [280nm] NA

Activity

IC50: Nicotinic acetylcholine receptors

TargetOrganismIC50AgonistRef
α3β2R. norvegicus18.1 nM[14.8-22.2]ACh (100 uM)Hone,A.J. et al. (2019)
α3β4R. norvegicus0.90 μM[0.78-1.04]ACh (300 μM)Hone,A.J. et al. (2020)
α6/α3β2β3R. norvegicus5432 nM[2809-10500]ACh (100 uM)Hone,A.J. et al. (2019)
α6/α3β4H. sapiens18.9 nM[14.8-24.1]300 uM AChHone,A.J. et al. (2021)
R. norvegicus275 nM[228-332]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

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