RgIA [del13] (P07466) Protein Card

General Information
Name RgIA [del13] (named by ConoServer)
Alternative name(s) RgIA [deltaR]
Organism synthetic construct
Protein Type Synthetic
Parent RgIA
Notes Inhibited HVA Ca2+ channel current via GABAB receptors in rat DRG neurons with an IC50 of 4.4 nM. (Halai 2011)

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

Sequence
GCCSDPRCRYRC(nh2)
Modified residues
positionsymbolname
13nh2C-term amidation
Sequence evidence protein level
Average Mass 1413.62
Monoisotopic Mass 1412.53
Isoelectric Point 12.20
Extinction Coefficient [280nm] 1490.00

Activity

IC50: Nicotinic acetylcholine receptors

TargetOrganismIC50AgonistRef
α7H. sapiens>1000 nMAch (100 uM)Liang,J. et al. (2020)
α9α10H. sapiens(α9:α10 subunit ratio of 1:3)248.7 nM+/-19.2Ach (6 uM)Liang,J. et al. (2020)
unidentified(nAChR was hybrid human α9/rat α10)34 nM[14-83]Halai,R. et al. (2011)

Percentage inhibition: Nicotinic acetylcholine receptors

TargetOrganism% inhibitionConcentrationRef
α9α10unidentified(nAChR was hybrid human α9/rat α10. )55+/-550 nMHalai,R. et al. (2011)

Synthetic variants
RgIA [del13] dimerGCCSDPRCRYRCGRRRRGGCCSDPRCRYRC

References
Halai,R., Callaghan,B., Daly,N.L., Clark,R.J., Adams,D.J. and Craik,D.J. (2011) Effects of cyclization on stability, structure, and activity of α-conotoxin RgIA at the α9α10 nicotinic acetylcholine receptor and GABA(B) receptor. J. Med. Chem. 54:6984-6992
Liang,J., Tae,H.S., Xu,X., Jiang,T., Adams,D.J. and Yu,R (2020) Dimerization of α-Conotoxins as a Strategy to Enhance the Inhibition of the Human α7 and α9α10 Nicotinic Acetylcholine Receptors J. Med. Chem 63:2974-2985

Internal links
Nucleic acids
Structure

External links

Tools