PnIA [A10L,sTy15Y] (P04375) Protein Card

General Information
Name PnIA [A10L,sTy15Y] (named by ConoServer)
Alternative name(s) PnIA [A10L]
Organism synthetic construct
Protein Type Synthetic
Parent PnIA

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

Sequence
GCCSLPPCALNNPDYC(nh2)
Modified residues
positionsymbolname
17nh2C-term amidation
Average Mass 1664.90
Monoisotopic Mass 1663.62
Isoelectric Point 5.47
Extinction Coefficient [280nm] 1490.00

Activity

IC50: Nicotinic acetylcholine receptors

TargetOrganismIC50nhillAgonistRef
α3β2R. norvegicus55.23 nM[50.69-60.18]1.09Ach (100 uM)Dutertre,S. et al. (2005)
99.3nM0.57300uM AchLuo,S. et al. (1999)
α4β2R. norvegicus>>1000 nMAch (100 uM)Dutertre,S. et al. (2005)
α7G. gallus168nM1.55200uM AchHogg,R.C. et al. (2003)
H. sapiens59 nM[47-72]1.1200 uM AchYu et al. (2018)
R. norvegicus12.6nM1.21mM AchLuo,S. et al. (1999)
12 nM[10-14]1200 uM AchYu et al. (2018)

Kd: Nicotinic acetylcholine receptors

TargetOrganismKdRef
α7R. norvegicus11.1nMLuo,S. et al. (1999)

Ki: Nicotinic acetylcholine receptors

TargetOrganismKiCompetitorAgonistRef
AChBPL. stagnalis80 nM+/-40I-Bgt(10 uM)Dutertre,S. et al. (2007)

References
Luo,S., Nguyen,T.A., Cartier,G.E., Olivera,B.M., Yoshikami,D. and McIntosh,J.M. (1999) Single-residue alteration in alpha-conotoxin PnIA switches its nAChR subtype selectivity Biochemistry 38:14542-14548
Dutertre,S., Ulens,C., Büttner,R., Fish,A., van Elk,R., Kendel,Y., Hopping,G., Alewood,P.F., Schroeder,C., Nicke,A., Smit,A.B., Sixma,T.K. and Lewis,R.J. (2007) AChBP-targeted alpha-conotoxin correlates distinct binding orientations with nAChR subtype selectivity. EMBO J. 26:3858-3867
Hogg,R.C., Miranda,L.P., Craik,D.J., Lewis,R.J., Alewood,P.F. and Adams,D.J. (1999) Single amino acid substitutions in alpha-conotoxin PnIA shift selectivity for subtypes of the mammalian neuronal nicotinic acetylcholine receptor. J. Biol. Chem. 274:36559-36564
Hogg,R.C., Hopping,G., Alewood,P.F., Adams,D.J. and Bertrand,D. (2003) Alpha-conotoxins PnIA and [A10L]PnIA stabilize different states of the alpha7-L247T nicotinic acetylcholine receptor. J. Biol. Chem. 278:26908-26914
Dutertre,S., Nicke,A., and Lewis,R.J. (2005) Beta2 subunit contribution to 4/7 alpha-conotoxin binding to the nicotinic acetylcholine receptor. J. Biol. Chem. 280:30460-30468
Yu, J., Zhu, X., Zhang, L., Kudryavtsev, D., Kasheverov, I., Lei, Y., Zhangsun, D., Tsetlin, V. and Luo, S. (2018) Species specificity of rat and human α7 nicotinic acetylcholine receptors towards different classes of peptide and protein antagonists Neuropharmacology 139:226-237

Internal links
Nucleic acids
Structure

External links

Tools