ArIB [V11L,V16A] (P02755) Protein Card

General Information
Name ArIB [V11L,V16A]
Organism synthetic construct
Protein Type Synthetic
Parent ArIB
Notes Best published inhibitor for the homomeric Alpha7 receptor (Whiteaker et al. 2007, 2008). A fluorescent derivative was successfully synthesised by conjugation of the N-terminal amine with a Cy3 NHS dye (Hone et al. 2009).

Classification
Conopeptide class conotoxin
Gene superfamily
Pharmacological family alpha conotoxin

Sequence
DECCSNPACRLNNPHACRRR
Average Mass 2311.57
Monoisotopic Mass 2309.97
Isoelectric Point 12.03
Extinction Coefficient [280nm] NA

Activity

IC50: Nicotinic acetylcholine receptors

TargetOrganismIC50AgonistRef
α3β2R. norvegicus74.5nM100uM acetyylcholineWhiteaker et al. (2007)
α6/α3β2β3R. norvegicus120nM100uM acetyylcholineWhiteaker et al. (2007)
α7R. norvegicus356pM200uM acetyylcholineWhiteaker et al. (2007)

References
Whiteaker, P., Christensen,S., Yoshikami,D., Dowell,C., Watkins,M., Gulyas,J., Rivier,J., Olivera,B.M. and McIntosh,J.M. (2007) Discovery, Synthesis, and Structure Activity of a Highly Selective alpha7 Nicotinic Acetylcholine Receptor Antagonist Biochemistry 46:6628-6638
Whiteaker,P., Marks,M.J., Christensen,S., Dowell,C., Collins,A.C. and McIntosh,J.M. (2008) Synthesis and characterization of 125I-alpha-conotoxin ArIB[V11L;V16A], a selective alpha7 nicotinic acetylcholine receptor antagonist. J. Pharmacol. Exp. Ther. 325:910-919
Hone,A.J., Whiteaker,P., Christensen,S., Xiao,Y., Meyer,E.L. and McIntosh,J.M. (2009) A novel fluorescent alpha-conotoxin for the study of alpha7 nicotinic acetylcholine receptors. J. Neurochem. 111:80-89

Internal links
Nucleic acids
Structure

External links

Tools