PeIA[V10A] (P05853) Protein Card

General Information

Name	PeIA[V10A]
Alternative name(s)	[Ala10]PeIA
Organism	synthetic construct
Protein Type	Synthetic
Parent	PeIA

Classification

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

Sequence

GCCSHPACSANHPELC(nh2)

Modified residues

position	symbol	name
17	nh2	C-term amidation

Average Mass

1623.81

Monoisotopic Mass

1622.58

Isoelectric Point

6.81

Extinction Coefficient [280nm]

Activity

IC50: Nicotinic acetylcholine receptors

Target	Organism	IC50		Agonist	Ref
α3β2	R. norvegicus	2.2nM	+/-0.3	100uM Ach	Hone,A.J. et al. (2012)
		3.37 nM	[3.05-3.72]	Ach (100 uM)	Hone,A.J. et al. (2019)
α3β4	R. norvegicus	2.7uM	+/-0.5	100uM Ach	Hone,A.J. et al. (2012)
α6/α3β2β3	R. norvegicus	2.4nM	+/-0.3	100uM Ach	Hone,A.J. et al. (2012)
α6/α3β4	H. sapiens	22.1 nM	[19-25.6]	300 uM ACh	Hone,A.J. et al. (2021)
	R. norvegicus	302nM	+/-28	100uM Ach	Hone,A.J. et al. (2012)
		137 nM	[111-168]	300 uM ACh	Hone,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., Ruiz,M., Scadden,M., Christensen,S., Gajewiak,J., Azam,L. and McIntosh,J.M. (2013) Positional scanning mutagenesis of α-conotoxin PeIA identifies critical residues that confer potency and selectivity for α6/α3β2β3 and α3β2 nicotinic acetylcholine receptors. J. Biol. Chem. 288:25428-25439

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

Please cite:
Kaas Q, Yu R, Jin AH, Dutertre S and Craik DJ. ConoServer: updated content, knowledge, and discovery tools in the conopeptide database. Nucleic Acids Research (2012) 40(Database issue):D325-30
Kaas Q, Westermann JC, Halai R, Wang CK and Craik DJ. ConoServer, a database for conopeptide sequences and structures. Bioinformatics (2008) 24(3):445-6

ConoServer is managed at the Institute of Molecular Bioscience IMB, Brisbane, Australia.

The database and computational tools found on this website may be used for academic research only, provided that it is referred to ConoServer, the database of conotoxins (http://www.conoserver.org) and the above reference is cited. For any other use please contact David Craik (d.craik@imb.uq.edu.au).

Contacts:
David Craik
Quentin Kaas

Last updated: Friday 27 May 2022