title: MrIC, a novel α-conotoxin agonist in the presence of PNU at endogenous α7 nicotinic acetylcholine receptors.
abstract: α-Conotoxins are competitive antagonists of nicotinic acetylcholine receptors (nAChRs). Their high selectivity and affinity for the various subtypes of nAChRs have led to significant advances in our understanding of the structure and function of these key ion channels. Here we report the discovery of a novel 4/7 α-conotoxin, MrIC from the venom duct of Conus marmoreus, which acts as an agonist at the endogenous human α7 nAChR in SH-SY5Y cells pretreated with PNU120596 (PNU). This unique agonist activity of MrIC at α7 nAChRs may guide the development of novel α7 nAChR modulators.
authors.affiliation: Institute for Molecular Bioscience, The University of Queensland , Brisbane, QLD 4072, Australia , and Discipline of Pharmacology, The University of Sydney , Sydney, NSW 2006, Australia.
authors.forename: Ai-Hua
authors.initials: AH
authors.lastname: Jin
authors.forename: Irina
authors.initials: I
authors.lastname: Vetter
authors.forename: Sébastien
authors.initials: S
authors.lastname: Dutertre
authors.forename: Nikita
authors.initials: N
authors.lastname: Abraham
authors.forename: Nayara B
authors.initials: NB
authors.lastname: Emidio
authors.forename: Marco
authors.initials: M
authors.lastname: Inserra
authors.forename: Swetha S
authors.initials: SS
authors.lastname: Murali
authors.forename: MacDonald J
authors.initials: MJ
authors.lastname: Christie
authors.forename: Paul F
authors.initials: PF
authors.lastname: Alewood
authors.forename: Richard J
authors.initials: RJ
authors.lastname: Lewis
mesh_terms: D000595:Amino Acid Sequence; D000818:Animals; D045744:Cell Line, Tumor; D020916:Conotoxins / Q000737:chemistry* / Q000494:pharmacology; D052078:Conus Snail; D006801:Humans; D007555:Isoxazoles / Q000494:pharmacology; D008969:Molecular Sequence Data; D010671:Phenylurea Compounds / Q000494:pharmacology; D064569:alpha7 Nicotinic Acetylcholine Receptor / Q000819:agonists*
chemical_list: C508388:1-(5-chloro-2,4-dimethoxyphenyl)-3-(5-methylisoxazol-3-yl)urea; D020916:Conotoxins; D007555:Isoxazoles; C587016:MrIC conotoxin, Conus marmoreus; D010671:Phenylurea Compounds; D064569:alpha7 Nicotinic Acetylcholine Receptor