Conorphin-T[N1U,del2-3,R4r,R5r,I7(Cha)] (P06922) Protein Card

General Information
Name Conorphin-T[N1U,del2-3,R4r,R5r,I7(Cha)] (named by ConoServer)
Alternative name(s) 26
Organism synthetic construct
Protein Type Synthetic
Parent Conorphin-T[ribbon]

Classification
Conopeptide class conorphin
Gene superfamily
Pharmacological family

Sequence
ZrrQ(Cha)CC(nh2)
Modified residues
positionsymbolname
1ZPyroglutamic acid
2rD-arginine
3rD-arginine
5ChaCyclohexylalanine
8nh2C-term amidation
Sequence evidence protein level
Average Mass 926.12
Monoisotopic Mass 925.44
Isoelectric Point NA
Extinction Coefficient [280nm] NA

Activity

EC50: Opioid receptors

TargetOrganismEC50Ref
κsynthetic construct(ERK 1/2 phosphorylation assay)1105 nM+/-839Brust A. et al. (2016)
(cAMP inhibition assay)12.6 nM+/-3.6Brust A. et al. (2016)

Ki: Opioid receptors

TargetOrganismKiCompetitorAgonistRef
κsynthetic construct(ERK 1/2 phosphorylation assay)3.9 nM+/-1.5Brust A. et al. (2016)

References
Brust A., Croker D. E., Colless B., Ragnarsson L., Andersson A., Jain K., Garcia-Caraballo S., Castro J., Brierley S. M., Alewood P. F., Lewis R. J. (2016) Conopeptide-Derived κ-Opioid Agonists (Conorphins): Potent, Selective, and Metabolic Stable Dynorphin A Mimetics with Antinociceptive Properties J. Med. Chem.

Internal links
Nucleic acids
Structure

External links

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