{"refrec":{"BRefID":220930,"RR":"<b>Peigneur, S.; Billen, B.; Derua, R.; Waelkens, E.; Debaveye, S.; Béress, L.; Tytgat, J.</b> (2011). A bifunctional sea anemone peptide with Kunitz type protease and potassium channel inhibiting properties. <i>Biochem. Pharmacol. 82(1)</i>: 81-90. <a href=\"https://dx.doi.org/10.1016/j.bcp.2011.03.023\" target=\"_blank\">https://dx.doi.org/10.1016/j.bcp.2011.03.023</a>","BEntID":212660,"PublicFlag":1,"CheckedFlag":1,"wosflag":1,"vabbflag":1,"RefStringPartII":". <i>Biochem. Pharmacol. 82(1)</i>: 81-90. <a href=\"https://dx.doi.org/10.1016/j.bcp.2011.03.023\" target=\"_blank\">https://dx.doi.org/10.1016/j.bcp.2011.03.023</a>","DocTypID":8,"DocType":"Journal article","MarineFlag":1,"FreshFlag":0,"BrackishFlag":0,"TerrestrialFlag":0,"Authorstring":"Peigneur, S.; Billen, B.; Derua, R.; Waelkens, E.; Debaveye, S.; Béress, L.; Tytgat, J.","OrigTitleTranslFlag":0,"Authorstringtrunc":"Peigneur, S. <i>et al.</i>","Englishabstract":"Sea anemone venom is a known source of interesting bioactive compounds, including peptide toxins which are invaluable tools for studying structure and function of voltage-gated potassium channels. APEKTx1 is a novel peptide isolated from the sea anemone <em>Anthopleura elegantissima</em>, containing 63 amino acids cross-linked by 3 disulfide bridges. Sequence alignment reveals that APEKTx1 is a new member of the type 2 sea anemone peptides targeting voltage-gated potassium channels (K<sub>V</sub>s), which also include the kalicludines from <em>Anemonia sulcata</em>. Similar to the kalicludines, APEKTx1 shares structural homology with both the basic pancreatic trypsin inhibitor (BPTI), a very potent Kunitz-type protease inhibitor, and dendrotoxins which are powerful blockers of voltage-gated potassium channels. In this study, APEKTx1 has been subjected to a screening on a wide range of 23 ion channels expressed in <em>Xenopus laevis</em> oocytes: 13 cloned voltage-gated potassium channels (K<sub>V</sub>1.1–K<sub>V</sub>1.6, K<sub>V</sub>1.1 triple mutant, K<sub>V</sub>2.1, K<sub>V</sub>3.1, K<sub>V</sub>4.2, K<sub>V</sub>4.3, hERG, the insect channel <em>Shaker</em> IR), 2 cloned hyperpolarization-activated cyclic nucleotide-sensitive cation non-selective channels (HCN1 and HCN2) and 8 cloned voltage-gated sodium channels (Na<sub>V</sub>1.2–Na<sub>V</sub>1.8 and the insect channel DmNa<sub>V</sub>1). Our data show that APEKTx1 selectively blocks K<sub>V</sub>1.1 channels in a very potent manner with an IC<sub>50</sub> value of 0.9 nM. Furthermore, we compared the trypsin inhibitory activity of this toxin with BPTI. APEKTx1 inhibits trypsin with a dissociation constant of 124 nM. In conclusion, this study demonstrates that APEKTx1 has the unique feature to combine the dual functionality of a potent and selective blocker of K<sub>V</sub>1.1 channels with that of a competitive inhibitor of trypsin.","AbstractOtherLang":null,"BibLvlCode":"AS","StandardTitle":"A bifunctional sea anemone peptide with Kunitz type protease and potassium channel inhibiting properties","OrigTitleLangCode":"en","OrigTitleLangCodeExtended":"eng","OrigTitleLangID":15,"DateLastModified":{"date":"2026-04-22 01:31:43.993731","timezone_type":1,"timezone":"+02:00"},"UserAccessRight":null,"UserAccID":null,"AuthorKeywords":"  <i>  Anthopleura elegantissima</i>;     K<sub>V</sub> channel inhibitor;     Sea anemone toxin;     Protease inhibitor","OtherDescriptors":null,"Notes":null,"AnaPub":2011,"MonPub":null,"DateUpdate":"2017-06-14","DateCreate":"2012-12-07","SecASFANote":null,"ConfID":null,"PeerRev":1,"VlizCoreFlag":1,"WoScode":"WOS:000291380000010","VABBcode":null,"OpenAcc":0,"DOI":"10.1016/j.bcp.2011.03.023"},"refs":null,"anarec":{"AnaID":220930,"PubliDate":2011,"Pagination":"81-90","XtraPublOfAnaID":null,"ISBN":null,"Volume":"82","Issue":"1","BRefMon":null,"BRefMonRR":null,"BRefXtra":null,"BRefXtraRR":null,"SerBRefID":42251,"SerRR":"Biochemical Pharmacology. Pergamon Press: London; New York.  ISSN 0006-2952; e-ISSN 1873-2968","StandardTitleSer":"Biochemical Pharmacology","ISSN":"0006-2952","AbbrevSer":"Biochem. Pharmacol.","StandardTitleMon":null,"StartPage":81,"Pages":10,"ToPubliDate":null,"BRefBibLvlCode":"S","SerNotes":null},"monrec":null,"serrec":null,"relations":null,"relationsRev":null,"addrec":null,"othpubs":null,"ownerships":null,"authors":[{"AutName":"Peigneur","Firstname":"Steve","Initials":"S.","Affiliation":"Laboratory of Toxicology, University of Leuven (K.U. Leuven)","Discriminator":null,"CorporateFlag":0,"BEntID":212660,"AutID":155255,"OrderNr":1,"DegrID":null,"EditorFlag":0,"CorrespFlag":0,"IllustratorFlag":0,"ReviserFlag":0,"TranslatorFlag":0,"InsAcronym":null,"InsFSN":"KU Leuven; Departement Farmaceutische en Farmacologische Wetenschappen; Laboratorium voor Toxicologie en Farmacologie","ORCID":"0000-0003-0504-5702","PersID":27019,"InsID":492},{"AutName":"Billen","Firstname":"Bert","Initials":"B.","Affiliation":"Laboratory of Toxicology, University of Leuven (K.U. Leuven)","Discriminator":null,"CorporateFlag":0,"BEntID":212660,"AutID":155146,"OrderNr":2,"DegrID":null,"EditorFlag":0,"CorrespFlag":0,"IllustratorFlag":0,"ReviserFlag":0,"TranslatorFlag":0,"InsAcronym":null,"InsFSN":"KU Leuven; Departement Farmaceutische en Farmacologische Wetenschappen; Laboratorium voor Toxicologie en Farmacologie","ORCID":null,"PersID":27295,"InsID":492},{"AutName":"Derua","Firstname":"Rita","Initials":"R.","Affiliation":"Laboratory of Protein Phosphorylation and Proteomics, University of Leuven (K.U. Leuven)","Discriminator":null,"CorporateFlag":0,"BEntID":212660,"AutID":155147,"OrderNr":3,"DegrID":null,"EditorFlag":0,"CorrespFlag":0,"IllustratorFlag":0,"ReviserFlag":0,"TranslatorFlag":0,"InsAcronym":null,"InsFSN":"KU Leuven; Groep Biomedische Wetenschappen; Department of Cellular and Molecular Medicine; Laboratory of Protein Phosphorylation and Proteomics","ORCID":null,"PersID":34894,"InsID":13956},{"AutName":"Waelkens","Firstname":"Etienne","Initials":"E.","Affiliation":"Laboratory of Protein Phosphorylation and Proteomics, University of Leuven (K.U. Leuven)","Discriminator":null,"CorporateFlag":0,"BEntID":212660,"AutID":259703,"OrderNr":4,"DegrID":null,"EditorFlag":0,"CorrespFlag":0,"IllustratorFlag":0,"ReviserFlag":0,"TranslatorFlag":0,"InsAcronym":null,"InsFSN":"KU Leuven; Groep Biomedische Wetenschappen; Department of Cellular and Molecular Medicine; Laboratory of Protein Phosphorylation and Proteomics","ORCID":null,"PersID":34812,"InsID":13956},{"AutName":"Debaveye","Firstname":"Sarah","Initials":"S.","Affiliation":"Laboratory of Toxicology, University of Leuven (K.U. Leuven)","Discriminator":null,"CorporateFlag":0,"BEntID":212660,"AutID":155153,"OrderNr":5,"DegrID":null,"EditorFlag":0,"CorrespFlag":0,"IllustratorFlag":0,"ReviserFlag":0,"TranslatorFlag":0,"InsAcronym":null,"InsFSN":"KU Leuven; Departement Farmaceutische en Farmacologische Wetenschappen; Laboratorium voor Toxicologie en Farmacologie","ORCID":null,"PersID":27360,"InsID":492},{"AutName":"Béress","Firstname":"László","Initials":"L.","Affiliation":null,"Discriminator":null,"CorporateFlag":0,"BEntID":212660,"AutID":155154,"OrderNr":6,"DegrID":null,"EditorFlag":0,"CorrespFlag":0,"IllustratorFlag":0,"ReviserFlag":0,"TranslatorFlag":0,"InsAcronym":null,"InsFSN":null,"ORCID":null,"PersID":null,"InsID":null},{"AutName":"Tytgat","Firstname":"Jan","Initials":"J.","Affiliation":"Laboratory of Toxicology, University of Leuven (K.U. Leuven)","Discriminator":null,"CorporateFlag":0,"BEntID":212660,"AutID":155257,"OrderNr":7,"DegrID":null,"EditorFlag":0,"CorrespFlag":0,"IllustratorFlag":0,"ReviserFlag":0,"TranslatorFlag":0,"InsAcronym":null,"InsFSN":"KU Leuven; Departement Farmaceutische en Farmacologische Wetenschappen; Laboratorium voor Toxicologie en Farmacologie","ORCID":null,"PersID":717,"InsID":492}],"mapdetails":null,"datasets":null,"monographs":null,"monparts":null,"serparts":null,"BEntOpen":null,"BEntPrivate":null,"availability":[{"BInstID":279777,"LibID":36,"BRefID":220930,"EmbargoDate":null,"FullEmbargoDate":null,"PhysMedID":16,"hasOCRd":1,"ShelfLocCode":"279777","RFID":null,"PaidValue":null,"Medium":"Server","Description":null,"Acronym":"VLIZ","Library":"Vlaams Instituut voor de Zee","DutchTerm":"Open Marien Archief","URL":null,"ClassifID":235,"Classification":"Open Marine Archive","ReqLink":null,"ClassifTypID":5,"URLLocation":"https://www.vliz.be/imisdocs/publications/","SubDir":0,"InternalReq":0,"LoggedInReq":0,"Disclaimer":"Disclaimer_OMA","DutchDisclaimer":null,"FileFormat":".pdf","FileDescr":"pdf","InsPub":1,"InsID":36,"FileFormID":6,"LendableFlag":1,"PublicFlag":1,"orderLib":"A","Notes":null,"AccConID":null,"AccessConstraint":null,"LicURL":null}],"litstyles":null,"thespers":null,"arch2discl":null,"SERpubls":[{"PublName":"Pergamon Press","City":"London; New York"}],"MONpubls":null,"pictures":[],"thestermsPath":null,"thestermsASFA":null,"taxtermsASFA":[{"TaxTerm":"Anthopleura elegantissima"}],"geotermsASFA":null,"collections":[{"Collection":"OMA - Open Marien Archief","ShortName":"OMA"}],"conf":null,"proj":null,"Physdatasets":null,"spcols":{"222":{"SpName":"BMB - Belgische Mariene Bibliografie","SpColID":222,"ParSpColID":null,"TopParID":null,"ShortName":"BMB","URLLocation":null,"LibID":36,"OpenRepoFlag":null,"SpTypID":null,"TopParIDNotWebsite":null,"SpColPath":"BMB"},"221":{"SpName":"OMA - Open Marien Archief","SpColID":221,"ParSpColID":null,"TopParID":null,"ShortName":"OMA","URLLocation":null,"LibID":36,"OpenRepoFlag":1,"SpTypID":null,"TopParIDNotWebsite":null,"SpColPath":"OMA"}},"doi":null,"publs":null,"serparttypes":null,"monauthors":null,"MParts":null,"SParts":null,"hLibs":null,"langs":[{"BEntID":212660,"AbstractFlag":0,"LangID":15,"LangCode":"en","Lang":"English","DutchTerm":"Engels","LangCodeExtended":"eng"},{"BEntID":212660,"AbstractFlag":1,"LangID":15,"LangCode":"en","Lang":"English","DutchTerm":"Engels","LangCodeExtended":"eng"}],"urls":[{"URL":"https://dx.doi.org/10.1016/j.bcp.2011.03.023","externalID":"10.1016/j.bcp.2011.03.023","URLTypeCode":"DOI","URLID":55885,"URLTypID":13,"URLType":"DOI","URLPrefix":"http://dx.doi.org/"}],"thesterms":null,"taxterms":[{"TaxTerm":"Anthopleura elegantissima [clonal anemone]","AphiaID":283347,"TaxtID":34405}],"geoterms":null,"othterms":null,"asfacodes":null,"asfa2codes":null,"thestermsFRIS":null,"taxtermsFRIS":[{"TaxTerm":"Anthopleura elegantissima","DutchTerm":null,"AphiaID":283347,"TaxtID":34405}],"geotermsFRIS":null,"othtermsFRIS":null,"resmessage":"","complete":1,"sessions":{"newSesName":"Bouchti, Zohra, Z.","newSesDate":{"date":"2012-12-07 08:28:26.583000","timezone_type":3,"timezone":"Europe/Brussels"},"updSesName":"Bouchti, Zohra, Z.","updSesDate":{"date":"2017-06-14 09:00:06.557000","timezone_type":3,"timezone":"Europe/Brussels"}}}