RegIIA (P00032) Protein Card

General Information

Name	RegIIA
Alternative name(s)	Reg2a
Organism	Conus regius
Organism region	Eastern Pacific
Organism diet	vermivorous
Protein Type	Wild type
Protein precursor	RegIIA precursor (5529)

Classification

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

Sequence

GCCSHPACNVNNPHIC(nh2)
Modified residues	position symbol name 17 nh2 C-term amidation
Sequence evidence	protein level
Average Mass	1663.88
Monoisotopic Mass	1662.63
Isoelectric Point	8.42
Extinction Coefficient [280nm]	NA

Activity

IC50: Nicotinic acetylcholine receptors

Target	Organism		IC50		nhill	Agonist	Ref
α3β2	H. sapiens		132.4nM	[109.8-159.7]	1.5	50uM ACh	Cuny,H. et al. (2016)
	R. norvegicus		33nM	+/-4		30uM ACh	Franco,A. et al. (2012)
α3β4	H. sapiens		45.6nM	[31.5-65.9]	0.9	300uM Ach	Cuny,H. et al. (2016)
	R. norvegicus		97nM	+/-20		30uM ACh	Franco,A. et al. (2012)
α4β2	R. norvegicus		>1uM			30uM ACh	Franco,A. et al. (2012)
α7	H. sapiens		210 nM	[170-270]	1.2	200 uM Ach	Yu et al. (2018)
			103nM	+/-23		200uM ACh	Franco,A. et al. (2012)
	R. norvegicus		41 nM	[33-50]	1.1	200 uM Ach	Yu et al. (2018)
α9α10	H. sapiens	(human a9 rat a10)	>1uM			30uM ACh	Franco,A. et al. (2012)

Synthetic variants

RegIIA[H5D]

GCCSDPACNVNNPHIC(nh2)

References

Franco,A., Pisarewicz,K., Moller,C., Mora,D., Fields,G.B. and Mari,F. (2006) Hyperhydroxylation: a new strategy for neuronal targeting by venomous marine molluscs Prog. Mol. Subcell. Biol. 43:83

Cuny,H., Kompella,S.N., Tae,H.S., Yu,R. and Adams,D.J. (2016) Key Structural Determinants in the Agonist Binding Loops of Human β2 and β4 Nicotinic Acetylcholine Receptor Subunits Contribute to α3β4 Subtype Selectivity of α-Conotoxins. J. Biol. Chem. 291:23779-23792

Franco,A., Kompella,S.N., Akondi,K.B., Melaun,C., Daly,N.L., Luetje,C.W., Alewood,P.F., Craik,D.J., Adams,D.J. and Marí,F. (2012) RegIIA: an α4/7-conotoxin from the venom of Conus regius that potently blocks α3β4 nAChRs. Biochem. Pharmacol. 83:419-426

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

Protein Precursor	RegIIA precursor (5529)
Nucleic acids
Structure	RegIIA NMR solution structure

External links

UniProtKB/Swiss-Prot	P85013
Ncbi	P85013

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: Monday 6 April 2020