Please use this identifier to cite or link to this item: http://hdl.handle.net/20.500.12779/4704
DC FieldValueLanguage
dc.contributor.authorBracci, Luisaen_us
dc.contributor.authorLozzi, Luisaen_us
dc.contributor.authorPini, Alessandroen_us
dc.contributor.authorLelli, Ben_us
dc.contributor.authorFalciani, Chiaraen_us
dc.contributor.authorNiccolai, Nerien_us
dc.contributor.authorBernini, Aen_us
dc.contributor.authorSpreafico, Aen_us
dc.contributor.authorSoldani, Patriziaen_us
dc.contributor.authorNeri, Paoloen_us
dc.date.accessioned2021-03-30T15:44:05Z-
dc.date.available2021-03-30T15:44:05Z-
dc.date.issued2002-
dc.identifier.issn0006-2960en_US
dc.identifier.urihttp://hdl.handle.net/20.500.12779/4704-
dc.description37382en_US
dc.description.abstractWe previously produced synthetic peptides mimicking the snake neurotoxin binding site of the nicotinic receptor. These peptide mimotopes bind the snake neurotoxin alpha-bungarotoxin with higher affinity than peptides reproducing native receptor sequences and inhibit toxin binding to nicotinic receptors in vitro; yet their efficiency in vivo is low. Here we synthesized one of the peptide mimotopes in a tetrabranched MAP form. The MAP peptide binds alpha-bungarotoxin in solution and inhibits its binding to the receptor with a K(A) and an IC(50) similar to the monomeric peptide. Nonetheless, it is at least 100 times more active in vivo. The MAP completely neutralizes toxin lethality when injected in mice at a dose compatible with its use as a synthetic antidote in humans. The in vivo efficacy of the tetrameric peptide cannot be ascribed to a kinetic and thermodynamic effect and is probably related to different pharmacokinetic behavior of the tetrameric molecule, with respect to the monomer. Our findings bring new perspectives to the therapeutic use of multimeric peptides.en_US
dc.language.isoenen_US
dc.relationNoneen_US
dc.relation.ispartofBIOCHEMISTRYen_US
dc.titleA branched peptide mimotope of the nicotinic receptor binding site is a potent synthetic antidote against the snake neurotoxin alpha-bungarotoxinen_US
dc.typeArticleen_US
dc.identifier.doi10.1021/bi0256025en_US
dc.identifier.pmid12162733en_US
dc.identifier.scopus2-s2.0-0037072268en_US
dc.identifier.isiWOS:000177337600002en_US
dc.relation.volume41en_US
dc.relation.issue32en_US
dc.description.firstpage10194en_US
dc.description.lastpage10199en_US
dc.description.thirdmissionNot applicableen_US
item.cerifentitytypePublications-
item.grantfulltextnone-
item.languageiso639-1en-
item.openairecristypehttp://purl.org/coar/resource_type/c_18cf-
item.openairetypeArticle-
item.fulltextNo Fulltext-
crisitem.author.orcid0000-0002-6919-6908-
crisitem.author.orcid0000-0002-4320-9950-
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