RgIA [C3(Smc),S4T,Y10(Ity),R11Q,ins13(bA)] (P10459) Protein Card

General Information
Name RgIA [C3(Smc),S4T,Y10(Ity),R11Q,ins13(bA)] (named by ConoServer)
Alternative name(s) RgIA-5573
Organism synthetic construct
Protein Type Synthetic
Parent RgIA
Notes A methylene thioacetal bond is formed between (Smc)3 and C12 (Zheng et al., 2021).

Classification
Conopeptide class conotoxin
Gene superfamily
Pharmacological family alpha conotoxin

Sequence
GC(Smc)TDPRCR(Ity)QC(bA)R
Modified residues
positionsymbolname
3SmcS-Methylcystine
10Ity3-iodotyrosine
13bAβ-Alanine
Average Mass 1768.77
Monoisotopic Mass 1767.55
Isoelectric Point 12.20
Extinction Coefficient [280nm] 125.00

Activity

IC50: Nicotinic acetylcholine receptors

TargetOrganismIC50AgonistRef
α9α10H. sapiens2.9 nM[1.9-4.5]100 uM AChZheng N et al. (2021)

References
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