TxIA[A10L] (P08958) Protein Card

General Information
Name TxIA[A10L]
Alternative name(s) gTxIA[A10L]
Organism synthetic construct
Protein Type Synthetic
Parent TxIA

Classification
Conopeptide class conotoxin
Gene superfamily
Cysteine framework I
Pharmacological family

Sequence
GCCSRPPCILNNPDLC(nh2)
Modified residues
positionsymbolname
17nh2C-term amidation
Sequence evidence protein level
Average Mass 1699.99
Monoisotopic Mass 1698.71
Isoelectric Point 7.00
Extinction Coefficient [280nm] NA

Activity

IC50: Nicotinic acetylcholine receptors

TargetOrganismIC50nhillAgonistRef
α3β2R. norvegicus2.0 nM[1.8-2.4]AchDutertre,S. et al. (2007)
(mutant ?3(I186R)?2)76.5 nM[58.9-99.3]-1.261100 uM AChBeissner,M. et al. (2012)
α4β2R. norvegicus(mutant ô°€?4(P195Q)ô°?2)707 nM[533-939]-0.88100 uM AChBeissner,M. et al. (2012)
(mutant 􏰀?4(R185I)􏰁?2(V109G)􏰁)6.6 nM[4.8-9.1]-0.755100 uM AChBeissner,M. et al. (2012)
(mutant 􏰀?4(R185A)􏰁?2)415 nM[333-515]-0.98100 uM AChBeissner,M. et al. (2012)
(mutant 􏰀?4(R185E)􏰁?2)91.8 nM[74.8-113]-1.079100 uM AChBeissner,M. et al. (2012)
(mutant 􏰀?4?2(V109G)􏰁)213 nM[167-271]-1.031100 uM AChBeissner,M. et al. (2012)
(mutant 􏰀?4(R185I)􏰁?2)123 nM[102-113]-0.835100 uM AChBeissner,M. et al. (2012)
(mutant 􏰀?4(R185I)3.2 nM[2.6-3.8]-1.11100 uM AChBeissner,M. et al. (2012)
α7H. sapiens0.50 uM+/-0.0430 uM cholineHo,T.N.T. et al. (2021)
R. norvegicus(P195Q)􏰁?2)39 nM[31-49]nicotineDutertre,S. et al. (2007)

Ki: Nicotinic acetylcholine receptors

TargetOrganismKiCompetitorAgonistRef
AChBPL. stagnalis1.1 nM+/-0.4I-Bgt(10 uM)Dutertre,S. et al. (2007)

References
Dutertre,S., Ulens,C., Büttner,R., Fish,A., van Elk,R., Kendel,Y., Hopping,G., Alewood,P.F., Schroeder,C., Nicke,A., Smit,A.B., Sixma,T.K. and Lewis,R.J. (2007) AChBP-targeted alpha-conotoxin correlates distinct binding orientations with nAChR subtype selectivity. EMBO J. 26:3858-3867
Beissner,M., Dutertre,S., Schemm,R., Danker,T., Sporning,A., Grubmüller,H. and Nicke,A. (2012) Efficient binding of 4/7 α-conotoxins to nicotinic α4β2 receptors is prevented by Arg185 and Pro195 in the α4 subunit Mol. Pharmacol 82:711-718
Ho,T.N.T., Abraham,N., Lewis,R.J. (2021) Rigidity of loop 1 contributes to equipotency of globular and ribbon isomers of α-conotoxin AusIA Sci Rep 11:21928

Internal links
Nucleic acids
Structure ACHBP-TARGETED A-CONOTOXIN CORRELATES DISTINCT BINDING ORIENTATIONS WITH NACHR SUBTYPE SELECTIVITY.

External links

Tools