PeIA[S9H,V10(Nle),N11(Api),L15I] (P08989) Protein Card

General Information
Name PeIA[S9H,V10(Nle),N11(Api),L15I] (named by ConoServer)
Alternative name(s) PeIA-5466
Organism synthetic construct
Protein Type Synthetic
Parent PeIA

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

Sequence
GCCSHPACH(Nle)(Api)HPEIC(nh2)
Modified residues
positionsymbolname
10NleNorleucine
11Apialpha-aminopimelic acid
17nh2C-term amidation
Sequence evidence Unknown
Average Mass 1777.03
Monoisotopic Mass 1775.70
Isoelectric Point 7.10
Extinction Coefficient [280nm] NA

Activity

IC50: Nicotinic acetylcholine receptors

TargetOrganismIC50AgonistRef
α3β2R. norvegicus1.34 nM[1.13-1.6]Ach (100 uM)Hone,A.J. et al. (2019)
α3β4R. norvegicus380 nM[344-419]Ach (300 uM)Hone,A.J. et al. (2019)
α4β2R. norvegicus2066 nM[1666-2563]Ach (100 uM)Hone,A.J. et al. (2019)
α6/α3β2β3R. norvegicus377 nM[275-508]Ach (100 uM)Hone,A.J. et al. (2019)
α6/α3β4R. norvegicus205 nM[164-257]Ach (300 uM)Hone,A.J. et al. (2019)
α7R. norvegicus15.0 nM[12.1-18.5]Ach (300 uM)Hone,A.J. et al. (2019)

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

Internal links
Nucleic acids
Structure

External links

Tools