EpI [sTy15Y] (P00112) Protein Card

General Information
Name EpI [sTy15Y]
Alternative name(s) EpI[Y(SO3)15Y]-NH2
Organism synthetic construct
Protein Type Synthetic
Parent EpI
Notes Did not inhibit α3β4 and α3β2 nAChRs (Nicke, 2003).

Classification
Conopeptide class conotoxin
Gene superfamily
Cysteine framework I
Pharmacological family alpha conotoxin

Sequence
GCCSDPRCNMNNPDYC(nh2)
Modified residues
positionsymbolname
17nh2C-term amidation
Average Mass 1786.95
Monoisotopic Mass 1785.58
Isoelectric Point 5.63
Extinction Coefficient [280nm] 1490.00

Activity

IC50: Nicotinic acetylcholine receptors

TargetOrganismIC50nhillAgonistRef
α3β4H. sapiens346.74 nM[269.15-436.52]30 uM nicotineHo,T.N.T. et al. (2021)
α7R. norvegicus118 nM1100 uM nicotineNicke,A. et al. (2003)

Ki: Nicotinic acetylcholine receptors

TargetOrganismKiCompetitorAgonistRef
AChBPA. californica26.92 nM[19.95-36.31]1 nM [3H]-epibatidineHo,T.N.T. et al. (2021)
L. stagnalis>100 uM1 nM [3H]-epibatidineHo,T.N.T. et al. (2021)

References
Hu,S.H., Loughnan,M., Miller,R., Weeks,C.M., Blessing,R.H., Alewood,P.F., Lewis,R.J. and Martin,J.L. (1998) The 1.1 A resolution crystal structure of [Tyr15]EpI, a novel alpha-conotoxin from Conus episcopatus, solved by direct methods Biochemistry 37:11425-11433
Nicke,A., Samochocki,M., Loughnan,M.L., Bansal,P.S., Maelicke,A. and Lewis,R.J. (2003) Alpha-conotoxins EpI and AuIB switch subtype selectivity and activity in native versus recombinant nicotinic acetylcholine receptors. FEBS Lett. 554:219-223
Ho,T.N.T., Lee,H.S., Swaminathan,S., Goodwin,L., Rai,N., Ushay,B., Lewis,R.J. and Conibear,A.C. (2021) Posttranslational modifications of α-conotoxins: sulfotyrosine and C-terminal amidation stabilise structures and increase acetylcholine receptor binding. RSC Med Chem 12:1574-1584

Internal links
Nucleic acids
Structure 1.1 ANGSTROM CRYSTAL STRUCTURE OF A-CONOTOXIN [TYR15]-EPI
NMR structure of EpI-[Y(SO3)15Y]-NH2

External links
Ncbi 1A0M_A, 1A0M_B

Tools