conantokin-Rl2[O10A] (P05845) Protein Card

General Information
Name conantokin-Rl2[O10A]
Alternative name(s) conRl-B[O10A]
Organism synthetic construct
Protein Type Synthetic
Parent Conantokin-Rl2

Classification
Conopeptide class conantokin
Gene superfamily
Pharmacological family

Sequence
GE(Gla)(Gla)LA(Gla)KAA(Gla)FAR(Gla)LAN(nh2)
Modified residues
positionsymbolname
3GlaGamma carboxylic glutamic acid
4GlaGamma carboxylic glutamic acid
7GlaGamma carboxylic glutamic acid
11GlaGamma carboxylic glutamic acid
15GlaGamma carboxylic glutamic acid
19nh2C-term amidation
Average Mass 2196.18
Monoisotopic Mass 2194.91
Isoelectric Point 2.02
Extinction Coefficient [280nm] NA

Activity

IC50: Ionotropic glutamate receptors

TargetOrganismIC50AgonistRef
GluN2AR. norvegicus>10uM200uM glutamateGowd,K.H. et al. (2012)
GluN2BR. norvegicus940nM200uM glutamateGowd,K.H. et al. (2012)
GluN2CR. norvegicus>10uM200uM glutamateGowd,K.H. et al. (2012)
GluN2DR. norvegicus>10uM200uM glutamateGowd,K.H. et al. (2012)

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

Internal links
Nucleic acids
Structure The Solution Structure of the Magnesium-bound Conantokin-R1B [O10A]

External links

Tools