PnIA [sTy15Y] (P04377) Protein Card

General Information
Name PnIA [sTy15Y]
Alternative name(s) PnIA
Organism synthetic construct
Protein Type Synthetic
Parent PnIA

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

Sequence
GCCSLPPCAANNPDYC(nh2)
Modified residues
positionsymbolname
17nh2C-term amidation
Average Mass 1622.81
Monoisotopic Mass 1621.58
Isoelectric Point 5.47
Extinction Coefficient [280nm] 1490.00

Activity

IC50: Nicotinic acetylcholine receptors

TargetOrganismIC50nhillAgonistRef
α3β2R. norvegicus9.56nM1300uM AchLuo,S. et al. (1999)
Unknown7.74nM[6.79-8.81]0.85100uM AchDutertre,S. et al. (2005)
α4β2Unknown>10uM100uM AchDutertre,S. et al. (2005)
α6/α3β2β3H. sapiens2.8 nM[2-3.8]ACh(100 uM) Hone et al. (2018)
R. norvegicus3.3 nM[3-3.6]ACh(100 uM) Hone et al. (2018)
α6/α3β4H. sapiens149 nM[135-164]ACh(300 uM) Hone et al. (2018)
R. norvegicus8456 nM[5419-13290]300uM AchHone et al. (2018)
α7G. gallus349nM200uM AchHogg,R.C. et al. (2003)
R. norvegicus252nM1.21mM AchLuo,S. et al. (1999)

Kd: Nicotinic acetylcholine receptors

TargetOrganismKdRef
α7R. norvegicus176nMLuo,S. et al. (1999)

Ki: Nicotinic acetylcholine receptors

TargetOrganismKiCompetitorAgonistRef
AChBPL. stagnalis1000 nM+/-300I-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., 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
Hone, A.J., Talley, T.T., Bobango, J., Melo, C.H., Hararah, F., Gajewiak, J., Christensen, S., Harvey, P.J., Craik, D.J. and McIntosh, J.M. (2018) Molecular determinants of α-conotoxin potency for inhibition of human and rat α6β4 nicotinic acetylcholine receptors Journal of Biological Chemistry 293:17838-17852

Internal links
Nucleic acids
Structure

External links

Tools