Conantokin-R (P02594) Protein Card

General Information

Name	Conantokin-R
Alternative name(s)	Con-R
Organism	Conus radiatus
Organism region	Indo-Pacific
Organism diet	piscivorous
Protein Type	Wild type
Protein precursor	Conantokin-R precursor (1375)

Classification

Conopeptide class	conantokin
Gene superfamily	B1 superfamily
Pharmacological family

Sequence

GE(Gla)(Gla)VAKMAA(Gla)LAR(Gla)NIAKGCKVNC
YP

Modified residues

position	symbol	name
3	Gla	Gamma carboxylic glutamic acid
4	Gla	Gamma carboxylic glutamic acid
11	Gla	Gamma carboxylic glutamic acid
15	Gla	Gamma carboxylic glutamic acid

Sequence evidence

protein level

Average Mass

3098.37

Monoisotopic Mass

3096.35

Isoelectric Point

5.47

Extinction Coefficient [280nm]

1490.00

Activity

IC50: Ionotropic glutamate receptors

Target	Organism	IC50	Agonist	Ref
GluN2A	R. norvegicus	1uM	200uM glutamate	Teichert,R.W. et al. (2007)
		530nM	200uM glutamate	Twede,V.D. et al. (2009)
GluN2B	R. norvegicus	1uM	200uM glutamate	Teichert,R.W. et al. (2007)
		350nM	200uM glutamate	Twede,V.D. et al. (2009)
GluN2C	R. norvegicus	7uM	200uM glutamate	Teichert,R.W. et al. (2007)
		~10uM	200uM glutamate	Twede,V.D. et al. (2009)
GluN2D	R. norvegicus	>10uM	200uM glutamate	Teichert,R.W. et al. (2007)
		>10uM	200uM glutamate	Twede,V.D. et al. (2009)

Synthetic variants

Conantokin-R/Br	GE(Gla)(Gla)VAKMA(Gla)ERE(Gla)EAGRLDLSKFP
conantokin-R [Br5âˆ’6]	GE(Gla)(Gla)YSKMA(Gla)ELA(Gla)ENIAKGCKVNCYP
conantokin-R [Br7âˆ’9]	GE(Gla)(Gla)VAKFI(Gla)LAR(Gla)NIAKGCKVNCYP
conantokin-R [V5Y]	GE(Gla)(Gla)YAKMA(Gla)ELARENIAKGCKVNCYP

References

Klein,R.C., Prorok,M., Galdzicki,Z. and Castellino,F.J. (2001) The amino acid residue at sequence position 5 in the conantokin peptides partially governs subunit-selective antagonism of recombinant N-methyl-D-aspartate receptors J. Biol. Chem. 276:26860-26867

Jimenez,E.C., Donevan,S., Walker,C., Zhou,L.M., Nielsen,J., Cruz,L.J., Armstrong,H., White,H.S. and Olivera,B.M. (2002) Conantokin-L, a new NMDA receptor antagonist: determinants for anticonvulsant potency Epilepsy Res. 51:73-80

White,H.S., McCabe,R.T., Armstrong,H., Donevan,S.D., Cruz,L.J., Abogadie,F.C., Torres,J., Rivier,J.E., Paarmann,I., Hollmann,M. and Olivera,B.M. (2000) In vitro and in vivo characterization of conantokin-R, a selective NMDA receptor antagonist isolated from the venom of the fish-hunting snail Conus radiatus J. Pharmacol. Exp. Ther. 292:425-432

Blandl,T., Warder,S.E., Prorok,M. and Castellino,F.J. (2000) Structure-function relationships of the NMDA receptor antagonist peptide, conantokin-R FEBS Lett. 470:139-146

Teichert,R.W., Jimenez,E.C., Twede,V., Watkins,M., Hollmann,M., Bulaj,G. and Olivera,B.M. (2007) Novel conantokins from Conus parius venom are specific antagonists of N-methyl-D-aspartate receptors. J. Biol. Chem. 282:36905-36913

Internal links

Protein Precursor	Conantokin-R precursor (1375)
Nucleic acids
Structure

External links

Ncbi

P58806

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