{"refrec":{"BRefID":310368,"RR":"<b>Peigneur, S.; Cheneval, O.; Maiti, M.; Leipold, E.; Heinemann, S.H.; Lescrinier, E.; Herdewijn, P.; de Lima, M.E.; Craik, D.J.; Schroeder, C.I.; Tytgat, J.</b> (2019). Where cone snails and spiders meet: design of small cyclic sodium-channel inhibitors. <i>FASEB J. 33(3)</i>: 3693-3703. <a href=\"https://dx.doi.org/10.1096/fj.201801909R\" target=\"_blank\">https://dx.doi.org/10.1096/fj.201801909R</a>","BEntID":302699,"PublicFlag":1,"CheckedFlag":1,"wosflag":1,"vabbflag":1,"RefStringPartII":". <i>FASEB J. 33(3)</i>: 3693-3703. <a href=\"https://dx.doi.org/10.1096/fj.201801909R\" target=\"_blank\">https://dx.doi.org/10.1096/fj.201801909R</a>","DocTypID":8,"DocType":"Journal article","MarineFlag":0,"FreshFlag":0,"BrackishFlag":0,"TerrestrialFlag":0,"Authorstring":"Peigneur, S.; Cheneval, O.; Maiti, M.; Leipold, E.; Heinemann, S.H.; Lescrinier, E.; Herdewijn, P.; de Lima, M.E.; Craik, D.J.; Schroeder, C.I.; Tytgat, J.","OrigTitleTranslFlag":0,"Authorstringtrunc":"Peigneur, S. <i>et al.</i>","Englishabstract":"A 13 aa residue voltage-gated sodium (Na<sub>V</sub>) channel inhibitor peptide, Pn, containing 2 disulfide bridges was designed by using a chimeric approach. This approach was based on a common pharmacophore deduced from sequence and secondary structural homology of 2 Na<sub>V</sub> inhibitors: <i>Conus kinoshitai</i> toxin IIIA, a 14 residue cone snail peptide with 3 disulfide bonds, and <i>Phoneutria nigriventer</i> toxin 1, a 78 residue spider toxin with 7 disulfide bonds. As with the parent peptides, this novel Na<sub>V</sub> channel inhibitor was active on Na<sub>V</sub>1.2. Through the generation of 3 series of peptide mutants, we investigated the role of key residues and cyclization and their influence on Na<sub>V</sub> inhibition and subtype selectivity. Cyclic PnCS1, a 10 residue peptide cyclized <i>via</i> a disulfide bond, exhibited increased inhibitory activity toward therapeutically relevant Na<sub>V</sub> channel subtypes, including Na<sub>V</sub>1.7 and Na<sub>V</sub>1.9, while displaying remarkable serum stability. These peptides represent the first and the smallest cyclic peptide Na<sub>V</sub> modulators to date and are promising templates for the development of toxin-based therapeutic agents.","AbstractOtherLang":null,"BibLvlCode":"AS","StandardTitle":"Where cone snails and spiders meet: design of small cyclic sodium-channel inhibitors","OrigTitleLangCode":"en","OrigTitleLangCodeExtended":"eng","OrigTitleLangID":15,"DateLastModified":{"date":"2026-04-17 01:32:24.852338","timezone_type":1,"timezone":"+02:00"},"UserAccessRight":null,"UserAccID":null,"AuthorKeywords":"voltage-gated sodium channel; peptide cyclization; toxin-basedtherapeutics; peptide toxin","OtherDescriptors":null,"Notes":null,"AnaPub":2019,"MonPub":null,"DateUpdate":"2019-04-24","DateCreate":"2019-04-17","SecASFANote":null,"ConfID":null,"PeerRev":1,"VlizCoreFlag":1,"WoScode":"WOS:000459794800049","VABBcode":null,"OpenAcc":0,"DOI":"10.1096/fj.201801909R"},"refs":null,"anarec":{"AnaID":310368,"PubliDate":2019,"Pagination":"3693-3703","XtraPublOfAnaID":null,"ISBN":null,"Volume":"33","Issue":"3","BRefMon":null,"BRefMonRR":null,"BRefXtra":null,"BRefXtraRR":null,"SerBRefID":220986,"SerRR":"The FASEB Journal. 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