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In the work reported here, we established an efficient total chemical synthesis of the Ts1 protein using modern chemical ligation methods and demonstrated that it was fully active in modifying the voltage dependence of the rat skeletal muscle voltage\u2010gated sodium channel rNav1.4 expressed in oocytes. Total synthesis combined with click chemistry was used to label the Ts1 protein molecule with the fluorescent dyes Alexa\u2010Fluor 488 and Bodipy. Dye\u2010labeled Ts1 proteins retained their optical properties and bound to and modified the voltage dependence of the sodium channel Nav. Because of the highly specific binding of Ts1 toxin to Nav, successful chemical synthesis and labeling of Ts1 toxin provides an important tool for biophysical studies, histochemical studies, and opto\u2010pharmacological studies of the Nav protein.<\/jats:p>","DOI":"10.1002\/anie.201404438","type":"journal-article","created":{"date-parts":[[2014,7,2]],"date-time":"2014-07-02T21:05:37Z","timestamp":1404335137000},"page":"8970-8974","source":"Crossref","is-referenced-by-count":28,"title":["Total Chemical Synthesis of Biologically Active Fluorescent Dye\u2010Labeled Ts1 Toxin"],"prefix":"10.1002","volume":"53","author":[{"given":"Bobo","family":"Dang","sequence":"first","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Tomoya","family":"Kubota","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Ana M.","family":"Correa","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Francisco","family":"Bezanilla","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Stephen B. 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