Conantokin-Rl2 (P05841) Protein Card

General Information
Name Conantokin-Rl2 (named by ConoServer)
Alternative name(s) conRl-B,conantokin-Rl-B
Organism Conus rolani
Protein Type Wild type
Protein precursor Conantokin-Rl2 precursor (5849)

Classification
Conopeptide class conantokin
Gene superfamily B1 superfamily
Pharmacological family

Sequence
GE(Gla)(Gla)LA(Gla)KAO(Gla)FAR(Gla)LAN(nh2)
Modified residues
positionsymbolname
3GlaGamma carboxylic glutamic acid
4GlaGamma carboxylic glutamic acid
7GlaGamma carboxylic glutamic acid
10O4-Hydroxyproline
11GlaGamma carboxylic glutamic acid
15GlaGamma carboxylic glutamic acid
19nh2C-term amidation
Sequence evidence nucleic acid level
Average Mass 2238.21
Monoisotopic Mass 2236.92
Isoelectric Point 2.02
Extinction Coefficient [280nm] NA

Activity

IC50: Ionotropic glutamate receptors

TargetOrganismIC50AgonistRef
GluN2AR. norvegicus~10uM200uM glutamateGowd,K.H. et al. (2012)
GluN2BR. norvegicus100nM200uM glutamateGowd,K.H. et al. (2012)
GluN2CR. norvegicus>10uM 200uM glutamateGowd,K.H. et al. (2012)
GluN2DR. norvegicus>10uM200uM glutamateGowd,K.H. et al. (2012)

Synthetic variants
Conantokin-Rl2[K8N,A9Q,del10O]GE(Gla)(Gla)LA(Gla)NQ(Gla)FAR(Gla)LAN(nh2)
Conantokin-Rl2[K8Nle]GE(Gla)(Gla)LA(Gla)(Nle)AO(Gla)FAR(Gla)LAN(nh2)
Conantokin-Rl2[L5Y]GE(Gla)(Gla)YA(Gla)KAO(Gla)FAR(Gla)LAN(nh2)
conantokin-Rl2[O10A]GE(Gla)(Gla)LA(Gla)KAA(Gla)FAR(Gla)LAN(nh2)
conantokin-Rl2[O10P]GE(Gla)(Gla)LA(Gla)KAP(Gla)FAR(Gla)LAN(nh2)
conantokin-Rl2[delO10]GE(Gla)(Gla)LA(Gla)KA(Gla)FAR(Gla)LAN(nh2)

References
Gowd,K.H., Han,T.S., Twede,V., Gajewiak,J., Smith,M.D., Watkins,M., Platt,R.J., Toledo,G., White,H.S., Olivera,B.M. and Bulaj,G. (2012) Conantokins derived from the Asprella clade impart conRl-B, an N-methyl d-aspartate receptor antagonist with a unique selectivity profile for NR2B subunits. Biochemistry 51:4685-4692
Yuan,Y., Balsara,R.D., Zajicek,J., Kunda,S. and Castellino,F.J. (2016) Discerning the Role of the Hydroxyproline Residue in the Structure of Conantokin Rl-B and Its Role in GluN2B Subunit-Selective Antagonistic Activity toward N-Methyl-d-Aspartate Receptors. Biochemistry 55:7112-7122
Kunda,S., Yuan,Y., Balsara,R.D., Zajicek,J. and Castellino,F.J. (2015) Hydroxyproline-induced Helical Disruption in Conantokin Rl-B Affects Subunit-selective Antagonistic Activities toward Ion Channels of N-Methyl-d-aspartate Receptors. J. Biol. Chem. 290:18156-18172

Internal links
Protein Precursor Conantokin-Rl2 precursor (5849)
Nucleic acids
Structure The solution structure of the Magnesium-bound Conantokin RLB

External links

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