RgIA [S4T,Y10(Ity),R11Q,R13Y] (P10376) Protein Card

General Information
Name RgIA [S4T,Y10(Ity),R11Q,R13Y] (named by ConoServer)
Alternative name(s) RgIA5
Organism synthetic construct
Protein Type Synthetic
Parent RgIA

Classification
Conopeptide class conotoxin
Gene superfamily
Pharmacological family alpha conotoxin

Sequence
GCCTDPRCR(Ity)QCY
Modified residues
positionsymbolname
10Ity3-iodotyrosine
Average Mass 1689.65
Monoisotopic Mass 1688.45
Isoelectric Point 10.99
Extinction Coefficient [280nm] 1490.00

Activity

IC50: Nicotinic acetylcholine receptors

TargetOrganismIC50nhillAgonistRef
α9α10H. sapiens0.2 nM+/-0.11.0510 uM AChRomero,H.K. et al. (2017)
0.4 nM[0.3-0.6]100 uM AChZheng N et al. (2021)
R. norvegicus0.4 nM+/-0.10.8610 uM AChRomero,H.K. et al. (2017)

References
Romero,H.K., Christensen,S.B., Di Cesare Mannelli,L., Gajewiak,J., Ramachandra,R., Elmslie,K.S., Vetter,D.E., Ghelardini,C., Iadonato,S.P., Mercado,J.L., Olivera,B.M. and McIntosh,J.M. (2017) Inhibition of α9α10 nicotinic acetylcholine receptors prevents chemotherapy-induced neuropathic pain. Proc Natl Acad Sci U S A 114
Zheng N, Christensen SB, Dowell C, Purushottam L, Skalicky JJ, McIntosh JM, Chou DH. (2021) Discovery of Methylene Thioacetal-Incorporated α-RgIA Analogues as Potent and Stable Antagonists of the Human α9β10 Nicotinic Acetylcholine Receptor for the Treatment of Neuropathic Pain J Med Chem 64:9513-9524

Internal links
Nucleic acids
Structure

External links

Tools