RgIA [C3(Pen),S4T,Y10(Ity),R11Q,R13(β3hY),insC_R] (P10386) Protein Card

General Information
Name RgIA [C3(Pen),S4T,Y10(Ity),R11Q,R13(β3hY),insC_R] (named by ConoServer)
Alternative name(s) RgIA-5474
Organism synthetic construct
Protein Type Synthetic
Parent RgIA

Classification
Conopeptide class conotoxin
Gene superfamily
Pharmacological family alpha conotoxin

Sequence
GC(Pen)TDPRCR(Ity)QC(β3hY)R
Modified residues
positionsymbolname
3PenL-Penicillamine
10Ity3-iodotyrosine
13β3hYβ3-homotyrosine
Average Mass 1920.97
Monoisotopic Mass 1919.63
Isoelectric Point 12.20
Extinction Coefficient [280nm] NA

Activity

IC50: Nicotinic acetylcholine receptors

TargetOrganismIC50AgonistRef
α1β1δεH. sapiens>10000nM100 μM AChGajewiak J et al. (2021)
α2β2H. sapiens>10000nM100 μM AChGajewiak J et al. (2021)
R. norvegicus>10000nM100 μM AChGajewiak J et al. (2021)
α2β4H. sapiens>10000nM100 μM AChGajewiak J et al. (2021)
R. norvegicus>10000nM100 μM AChGajewiak J et al. (2021)
α3β2H. sapiens>10000nM100 μM AChGajewiak J et al. (2021)
R. norvegicus>10000nM100 μM AChGajewiak J et al. (2021)
α3β4H. sapiens>10000nM100 μM AChGajewiak J et al. (2021)
R. norvegicus>10000nM100 μM AChGajewiak J et al. (2021)
α4β2H. sapiens>10000nM100 μM AChGajewiak J et al. (2021)
R. norvegicus>10000nM100 μM AChGajewiak J et al. (2021)
α4β4H. sapiens>10000nM100 μM AChGajewiak J et al. (2021)
R. norvegicus>10000nM100 μM AChGajewiak J et al. (2021)
α6/α3β2β3H. sapiens>10000nM100 μM AChGajewiak J et al. (2021)
R. norvegicus>10000nM100 μM AChGajewiak J et al. (2021)
α6/α3β4H. sapiens>10000nM100 μM AChGajewiak J et al. (2021)
R. norvegicus>10000nM100 μM AChGajewiak J et al. (2021)
α7H. sapiens115 nM[102-130]100 μM AChGajewiak J et al. (2021)
R. norvegicus>333 nM100 μM AChGajewiak J et al. (2021)
α9α10H. sapiens0.050 nM[0.037-0.069]100 μM AChGajewiak J et al. (2021)
0.051 nM[0.027-0.095]100 μM AChGajewiak J et al. (2021)
R. norvegicus0.39 nM[0.33-0.48]100 μM AChGajewiak J et al. (2021)

References
Gajewiak J, Christensen SB, Dowell C, Hararah F, Fisher F, Huynh PN, Olivera BM, McIntosh JM (2021) Selective Penicillamine Substitution Enables Development of a Potent Analgesic Peptide that Acts through a Non-Opioid-Based Mechanism J Med Chem 64:9271-9278

Internal links
Nucleic acids
Structure

External links

Tools