TxID[S9A] (P08412) Protein Card

General Information
Name TxID[S9A]
Organism synthetic construct
Protein Type Synthetic
Parent TxID

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

Sequence
GCCSHPVCAAMSPIC(nh2)
Modified residues
positionsymbolname
16nh2C-term amidation
Average Mass 1473.77
Monoisotopic Mass 1472.55
Isoelectric Point 8.31
Extinction Coefficient [280nm] NA

Activity

IC50: Nicotinic acetylcholine receptors

TargetOrganismIC50nhillAgonistRef
α3β4R. norvegicus3.9 nM[2.5-5.9]0.7Ach (100 uM)Yu et al. (2018)
36 nM[32-41]1Wang,S. et al. (2021)
α6/α3β4R. norvegicus178 nM[137-232]0.9Ach (100 uM)Yu et al. (2018)

Percentage inhibition: Nicotinic acetylcholine receptors

TargetOrganism% inhibitionConcentrationRef
α3β4R. norvegicus95.35 (93.95–96.75)1 µMWang,S. et al. (2021)

Synthetic variants
TxID[S9A,insN_GAGGAAG] cyclicGAGGAAGGCCSHPVCAAMSPIC
TxID[S9A,insN_GA] cyclicGAGCCSHPVCAAMSPIC
TxID[S9A,insN_GGAAGG] cyclicGGAAGGGCCSHPVCAAMSPIC
TxID[S9A,insN_GGAAG] cyclicGGAAGGCCSHPVCAAMSPIC
TxID[S9A,insN_GGAG] cyclicGGAGGCCSHPVCAAMSPIC
TxID[S9A,insN_GGA] cyclicGGAGCCSHPVCAAMSPIC

References
Yu, J., Zhu, X., Harvey, P.J., Kaas, Q., Zhangsun, D., Craik, D.J. and Luo, S. (2018) Single Amino Acid Substitution in α-Conotoxin TxID Reveals a Specific α3β4 Nicotinic Acetylcholine Receptor Antagonist Journal of medicinal chemistry 61:9256-9265
Wang,S., Ren,J., Li,R., Li,X., Zhangsun,D., Wu,Y. and Luo,S. (2021) Synthesis and evaluation of disulfide-rich cyclic α-conotoxin [S9A]TxID analogues as novel α3β4 nAChR antagonists. Bioorg Chem 112:104875

Internal links
Nucleic acids
Structure

External links

Tools