ArIB [V11L,V16D] (P02756) Protein Card

General Information
Name ArIB [V11L,V16D]
Organism synthetic construct
Protein Type Synthetic
Parent ArIB
Notes
  • Potent and selective inhibitor of human α7 nAChR (Innocent et al. 2008).
  • ArIB [V11L,V16D] promotes the proliferation of glioma C6 cells (Terpinskaya et al., 2021).

    • Classification
    Conopeptide class conotoxin
    Gene superfamily
    Pharmacological family alpha conotoxin

    Sequence
    DECCSNPACRLNNPHDCRRR
    Average Mass 2355.58
    Monoisotopic Mass 2353.96
    Isoelectric Point 10.94
    Extinction Coefficient [280nm] NA

    Activity

    IC50: Nicotinic acetylcholine receptors

    TargetOrganismIC50AgonistRef
    α3β2R. norvegicus>10uM100uM AchWhiteaker et al. (2007)
    α6/α3β2β3R. norvegicus828nM100uM AchWhiteaker et al. (2007)
    α7R. norvegicus1.09nM200uM AchWhiteaker 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
    Innocent,N., Livingstone,P.D., Hone,A., Kimura,A., Young,T., Whiteaker,P., McIntosh,J.M. and Wonnacott,S. (2008) Alpha-conotoxin Arenatus IB[V11L,V16D] [corrected] is a potent and selective antagonist at rat and human native alpha7 nicotinic acetylcholine receptors. J. Pharmacol. Exp. Ther. 327:529-537
    Grau, V., Richter, K., Hone, A.J. and McIntosh, J.M. (2018) Conopeptides [V11L; V16D] ArIB and RgIA4: powerful tools for the identification of novel nicotinic acetylcholine receptors in monocytes Frontiers in pharmacology 9
    Terpinskaya,T.I., Osipov,A.V., Kryukova,E.V., Kudryavtsev,D.S., Kopylova,N.V., Yanchanka,T.L., Palukoshka,A.F., Gondarenko,E.A., Zhmak,M.N., Tsetlin,V.I. and Utkin,Y.N. (2021) α-Conotoxins and α-Cobratoxin Promote, while Lipoxygenase and Cyclooxygenase Inhibitors Suppress the Proliferation of Glioma C6 Cells. Mar Drugs 19

    Internal links
    Nucleic acids
    Structure

    External links

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