GVIIJ[(Btr)2W,(Scc)24C] (P06833) Protein Card

General Information
Name GVIIJ[(Btr)2W,(Scc)24C] (named by ConoServer)
Alternative name(s) GVIIJ[SH],GVIIJ[SSC]
Organism synthetic construct
Protein Type Synthetic
Parent GVIIJ
Notes Block of rNav1.2[C912A] or [C918A] mutants is slowly reversible. +DTT it is rapidly reversible [Zhang,M.M., Gajewiak (2015)].

Classification
Conopeptide class conotoxin
Gene superfamily
Cysteine framework VI/VII
Pharmacological family mu conotoxin

Sequence
GWCGDOGATCGKLRLYCCSGFCDCYTKTCKDKSSA
Modified residues
positionsymbolname
6O4-Hydroxyproline
Sequence evidence protein level
Average Mass 3739.22
Monoisotopic Mass 3736.50
Isoelectric Point 10.10
Extinction Coefficient [280nm] 8605.00

Activity

IC50: Voltage-Gated Sodium Channels

TargetOrganismIC50Ref
Nav1.1H. sapiens(Expressed in CHO cells)23 nM+/-10Gajewiak,J. et al. (2014)
Nav1.2H. sapiens(Expressed in HEK 293 cells)55 nM+/-23Gajewiak,J. et al. (2014)
Nav1.3H. sapiens(Expressed in CHO cells)139 nM+/-38Gajewiak,J. et al. (2014)
Nav1.4H. sapiens(Expressed in HEK 293 cells)14 nM+/-4Gajewiak,J. et al. (2014)
Nav1.6H. sapiens(Expressed in CHO cells)14 nM+/-11Gajewiak,J. et al. (2014)
Nav1.7H. sapiens(Expressed in HEK 293 cells)78 nM+/-21Gajewiak,J. et al. (2014)

Percentage inhibition: Voltage-Gated Sodium Channels

TargetOrganism% inhibitionConcentrationRef
Nav1.2R. norvegicus(Expressed in X. laevis oocytes. )88+/-410 μM Zhang,M.M. et al. (2015)
(Mutant: Nav1.2[C918A]. Expressed in X. laevis oocytes.)88+/-210 μM Zhang,M.M. et al. (2015)
(Mutant: Nav1.2[C912A]. Expressed in X. laevis oocytes.)92+/-410 μM Zhang,M.M. et al. (2015)
Nav1.5H. sapiens(Expressed in HEK 293 cells)0+/-610 μMGajewiak,J. et al. (2014)

References
Gajewiak,J., Azam,L., Imperial,J., Walewska,A., Green,B.R., Bandyopadhyay,P.K., Raghuraman,S., Ueberheide,B., Bern,M., Zhou,H.M., Minassian,N.A., Hagan,R.H., Flinspach,M., Liu,Y., Bulaj,G., Wickenden,A.D., Olivera,B.M., Yoshikami,D. and Zhang,M.M. (2014) A disulfide tether stabilizes the block of sodium channels by the conotoxin μO§-GVIIJ. Proc. Natl. Acad. Sci. U.S.A. 111:2758-2763
Zhang,M.M., Gajewiak,J., Azam,L., Bulaj,G., Olivera,B.M. and Yoshikami,D. (2015) Probing the Redox States of Sodium Channel Cysteines at the Binding Site of μO§-Conotoxin GVIIJ. Biochemistry 54:3911-3920
Green,B.R., Gajewiak,J., Chhabra,S., Skalicky,J.J., Zhang,M.M., Rivier,J.E., Bulaj,G., Olivera,B.M., Yoshikami,D. and Norton,R.S. (2016) Structural Basis for the Inhibition of Voltage-gated Sodium Channels by Conotoxin μO§-GVIIJ. J. Biol. Chem. 291:7205-7220

Internal links
Nucleic acids
Structure

External links

Tools