{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,3,25]],"date-time":"2026-03-25T17:57:31Z","timestamp":1774461451309,"version":"3.50.1"},"reference-count":23,"publisher":"Wiley","issue":"16","license":[{"start":{"date-parts":[[2001,12,25]],"date-time":"2001-12-25T00:00:00Z","timestamp":1009238400000},"content-version":"vor","delay-in-days":511,"URL":"http:\/\/onlinelibrary.wiley.com\/termsAndConditions#vor"}],"content-domain":{"domain":[],"crossmark-restriction":false},"short-container-title":["European Journal of Biochemistry"],"published-print":{"date-parts":[[2000,8]]},"abstract":"<jats:p>Pi1 is a 35\u2010residue toxin cross\u2010linked by four disulfide bridges that has been isolated from the venom of the chactidae scorpion <jats:italic>Pandinus imperator<\/jats:italic>. Due to its very low abundance in the venom, we have chemically synthesized this toxin in order to study its biological activity. Enzyme\u2010based proteolytic cleavage of the synthetic Pi1 (sPi1) demonstrates half\u2010cystine pairings between Cys4\u2013Cys25, Cys10\u2013Cys30, Cys14\u2013Cys32 and Cys20\u2013Cys35, which is in agreement with the disulfide bridge organization initially reported on the natural toxin. <jats:italic>In vivo<\/jats:italic>, intracerebroventricular injection of sPi1 in mice produces lethal effects with an LD<jats:sub>50<\/jats:sub> of 0.2\u2003\u00b5g per mouse. <jats:italic>In vitro<\/jats:italic>, the application of sPi1 induces drastic inhibition of <jats:italic>Shaker<\/jats:italic> B (IC<jats:sub>50<\/jats:sub> of 23\u2003n<jats:sc>m<\/jats:sc>) and rat Kv1.2 channels (IC<jats:sub>50<\/jats:sub> of 0.44\u2003n<jats:sc>m<\/jats:sc>) heterologously expressed in <jats:italic>Xenopus laevis<\/jats:italic> oocytes. No effect was observed on rat Kv1.1 and Kv1.3 currents upon synthetic peptide application. Also, sPi1 is able to compete with <jats:sup>125<\/jats:sup>I\u2010labeled apamin for binding onto rat brain synaptosomes with an IC<jats:sub>50<\/jats:sub> of 55\u2003p<jats:sc>m<\/jats:sc>. Overall, these results demonstrate that sPi1 displays a large spectrum of activities by blocking both SK\u2010 and Kv1\u2010types of K<jats:sup>+<\/jats:sup> channels; a selectivity reminiscent of that of maurotoxin, another structurally related four disulfide\u2010bridged scorpion toxin that exhibits a different half\u2010cystine pairing pattern.<\/jats:p>","DOI":"10.1046\/j.1432-1327.2000.01577.x","type":"journal-article","created":{"date-parts":[[2003,3,11]],"date-time":"2003-03-11T17:52:08Z","timestamp":1047405128000},"page":"5149-5155","source":"Crossref","is-referenced-by-count":31,"title":["Chemical synthesis and characterization of Pi1, a scorpion toxin from <i>Pandinus imperator<\/i> active on K<sup>+<\/sup> channels"],"prefix":"10.1111","volume":"267","author":[{"given":"Ziad","family":"Fajloun","sequence":"first","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Edmond","family":"Carlier","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Catherine","family":"Lecomte","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Sandrine","family":"Geib","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Eric","family":"di Luccio","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Delphine","family":"Bichet","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Kamel","family":"Mabrouk","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Herv\u00e9","family":"Rochat","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Michel","family":"De Waard","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Jean\u2010Marc","family":"Sabatier","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]}],"member":"311","published-online":{"date-parts":[[2001,12,25]]},"reference":[{"key":"e_1_2_7_2_2","doi-asserted-by":"publisher","DOI":"10.1042\/bj3150977"},{"key":"e_1_2_7_3_2","first-page":"1167","article-title":"Three new toxins from the scorpion Pandinus imperator selectively block certain voltage\u2010gated K+ channels","volume":"50","author":"Rogowski R.S.","year":"1996","journal-title":"Mol. 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