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
positionsymbolname
3GlaGamma carboxylic glutamic acid
4GlaGamma carboxylic glutamic acid
11GlaGamma carboxylic glutamic acid
15GlaGamma 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

TargetOrganismIC50AgonistRef
GluN2AR. norvegicus1uM200uM glutamateTeichert,R.W. et al. (2007)
530nM200uM glutamateTwede,V.D. et al. (2009)
GluN2BR. norvegicus1uM200uM glutamateTeichert,R.W. et al. (2007)
350nM200uM glutamateTwede,V.D. et al. (2009)
GluN2CR. norvegicus7uM200uM glutamateTeichert,R.W. et al. (2007)
~10uM200uM glutamateTwede,V.D. et al. (2009)
GluN2DR. norvegicus>10uM200uM glutamateTeichert,R.W. et al. (2007)
>10uM200uM glutamateTwede,V.D. et al. (2009)

Synthetic variants
Conantokin-R/BrPFKSLDLRGAE(Gla)ERE(Gla)AMKAV(Gla)(Gla)EG
conantokin-R [Br5−6]PYCNVKCGKAINE(Gla)ALE(Gla)AMKSY(Gla)(Gla)EG
conantokin-R [Br7−9]PYCNVKCGKAIN(Gla)RAL(Gla)IFKAV(Gla)(Gla)EG
conantokin-R [V5Y]PYCNVKCGKAINERALE(Gla)AMKAY(Gla)(Gla)EG

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

Tools