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	position symbol name 17 nh2 C-term amidation
Average Mass	1664.90
Monoisotopic Mass	1663.62
Isoelectric Point	5.47
Extinction Coefficient [280nm]	1490.00

Activity

IC50: Nicotinic acetylcholine receptors

Target	Organism	IC50		nhill	Agonist	Ref
α3β2	R. norvegicus	55.23 nM	[50.69-60.18]	1.09	Ach (100 uM)	Dutertre,S. et al. (2005)
		99.3nM		0.57	300uM Ach	Luo,S. et al. (1999)
α4β2	R. norvegicus	>>1000 nM			Ach (100 uM)	Dutertre,S. et al. (2005)
α7	G. gallus	168nM		1.55	200uM Ach	Hogg,R.C. et al. (2003)
	H. sapiens	59 nM	[47-72]	1.1	200 uM Ach	Yu et al. (2018)
	R. norvegicus	12.6nM		1.2	1mM Ach	Luo,S. et al. (1999)
		12 nM	[10-14]	1	200 uM Ach	Yu et al. (2018)

Kd: Nicotinic acetylcholine receptors

Target	Organism	Kd		Ref
α7	R. norvegicus	11.1nM		Luo,S. et al. (1999)

Ki: Nicotinic acetylcholine receptors

Target	Organism	Ki		Competitor	Agonist	Ref
AChBP	L. stagnalis	80 nM	+/-40	I-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

Please cite:
Kaas Q, Yu R, Jin AH, Dutertre S and Craik DJ. ConoServer: updated content, knowledge, and discovery tools in the conopeptide database. Nucleic Acids Research (2012) 40(Database issue):D325-30
Kaas Q, Westermann JC, Halai R, Wang CK and Craik DJ. ConoServer, a database for conopeptide sequences and structures. Bioinformatics (2008) 24(3):445-6

ConoServer is managed at the Institute of Molecular Bioscience IMB, Brisbane, Australia.

The database and computational tools found on this website may be used for academic research only, provided that it is referred to ConoServer, the database of conotoxins (http://www.conoserver.org) and the above reference is cited. For any other use please contact David Craik (d.craik@imb.uq.edu.au).

Contacts:
David Craik
Quentin Kaas

Last updated: Thursday 2 February 2023