| http://purl.uniprot.org/citations/20950587 | http://www.w3.org/1999/02/22-rdf-syntax-ns#type | http://purl.uniprot.org/core/Journal_Citation |
| http://purl.uniprot.org/citations/20950587 | http://www.w3.org/1999/02/22-rdf-syntax-ns#type | http://purl.uniprot.org/core/Journal_Citation |
| http://purl.uniprot.org/citations/20950587 | http://www.w3.org/2000/01/rdf-schema#comment | "In contrast to all classical long-chain α-neurotoxins possessing the critical fifth disulfide bond, α-elapitoxin-Aa2a (α-EPTX-Aa2a), a novel long-chain α-neurotoxin from the common death adder Acanthophis antarcticus, lacks affinity for neuronal α7-type nicotinic acetylcholine receptors (nAChRs). α-EPTX-Aa2a (8850Da; 0.1-1μM) caused a concentration-dependent inhibition of indirect twitches, and blocked contractures to cholinergic agonists in the isolated chick biventer cervicis nerve-muscle preparation, consistent with a postsynaptic curaremimetic mode of action. α-EPTX-Aa2a (1-10nM) produced a potent pseudo-irreversible antagonism of chick muscle nAChRs, with an estimated pA(2) value of 8.311±0.031, which was not reversed by monovalent death adder antivenom. This is only 2.5-fold less potent than the prototypical long-chain α-neurotoxin, α-bungarotoxin. In contrast, α-EPTX-Aa2a produced complete, but weak, inhibition of (125)I-α-bungarotoxin binding to rat hippocampal α7 nAChRs (pK(I)=3.670), despite high sequence homology and similar mass to a wide range of long-chain α-neurotoxins. The mostly likely cause for the loss of α7 binding affinity is a leucine substitution, in loop II of α-EPTX-Aa2a, for the highly conserved Arg(33) in long-chain α-neurotoxins. Arg(33) has been shown to be critical for both neuronal and muscle activity. Despite this substitution, α-EPTX-Aa2a retains high affinity for muscle (α1)(2)βγδ nAChRs. This is probably as a result of an Arg(29) residue, previously shown to be critical for muscle (α1)(2)βγδ nAChR affinity, and highly conserved across all short-chain, but not long-chain, α-neurotoxins. α-EPTX-Aa2a therefore represents a novel atypical long-chain α-neurotoxin that includes a fifth disulfide but exhibits differential affinity for nAChR subtypes."xsd:string |
| http://purl.uniprot.org/citations/20950587 | http://purl.org/dc/terms/identifier | "doi:10.1016/j.bcp.2010.10.004"xsd:string |
| http://purl.uniprot.org/citations/20950587 | http://purl.org/dc/terms/identifier | "doi:10.1016/j.bcp.2010.10.004"xsd:string |
| http://purl.uniprot.org/citations/20950587 | http://purl.uniprot.org/core/author | "Blacklow B."xsd:string |
| http://purl.uniprot.org/citations/20950587 | http://purl.uniprot.org/core/author | "Blacklow B."xsd:string |
| http://purl.uniprot.org/citations/20950587 | http://purl.uniprot.org/core/author | "Escoubas P."xsd:string |
| http://purl.uniprot.org/citations/20950587 | http://purl.uniprot.org/core/author | "Escoubas P."xsd:string |
| http://purl.uniprot.org/citations/20950587 | http://purl.uniprot.org/core/author | "Graudins A."xsd:string |
| http://purl.uniprot.org/citations/20950587 | http://purl.uniprot.org/core/author | "Graudins A."xsd:string |
| http://purl.uniprot.org/citations/20950587 | http://purl.uniprot.org/core/author | "Hains P.G."xsd:string |
| http://purl.uniprot.org/citations/20950587 | http://purl.uniprot.org/core/author | "Hains P.G."xsd:string |
| http://purl.uniprot.org/citations/20950587 | http://purl.uniprot.org/core/author | "Kornhauser R."xsd:string |
| http://purl.uniprot.org/citations/20950587 | http://purl.uniprot.org/core/author | "Kornhauser R."xsd:string |
| http://purl.uniprot.org/citations/20950587 | http://purl.uniprot.org/core/author | "Loiacono R."xsd:string |
| http://purl.uniprot.org/citations/20950587 | http://purl.uniprot.org/core/author | "Loiacono R."xsd:string |
| http://purl.uniprot.org/citations/20950587 | http://purl.uniprot.org/core/author | "Nicholson G.M."xsd:string |
| http://purl.uniprot.org/citations/20950587 | http://purl.uniprot.org/core/author | "Nicholson G.M."xsd:string |
| http://purl.uniprot.org/citations/20950587 | http://purl.uniprot.org/core/date | "2011"xsd:gYear |
| http://purl.uniprot.org/citations/20950587 | http://purl.uniprot.org/core/date | "2011"xsd:gYear |
| http://purl.uniprot.org/citations/20950587 | http://purl.uniprot.org/core/name | "Biochem. Pharmacol."xsd:string |
| http://purl.uniprot.org/citations/20950587 | http://purl.uniprot.org/core/name | "Biochem. Pharmacol."xsd:string |
| http://purl.uniprot.org/citations/20950587 | http://purl.uniprot.org/core/pages | "314-325"xsd:string |
| http://purl.uniprot.org/citations/20950587 | http://purl.uniprot.org/core/pages | "314-325"xsd:string |