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Herein, we report the application of heterogeneous copper catalysts in azide\u2013alkyne cycloaddition processes in biological systems ranging from cells to zebrafish, with reactions spanning from fluorophore activation to the first reported in\u2005situ generation of a triazole\u2010containing anticancer agent from two benign components, opening up many new avenues of exploration for CuAAC chemistry.<\/jats:p>","DOI":"10.1002\/anie.201609837","type":"journal-article","created":{"date-parts":[[2016,11,16]],"date-time":"2016-11-16T18:30:18Z","timestamp":1479321018000},"page":"15662-15666","source":"Crossref","is-referenced-by-count":192,"title":["Copper Catalysis in Living Systems and In\u2005Situ Drug Synthesis"],"prefix":"10.1002","volume":"55","author":[{"given":"Jessica","family":"Clavadetscher","sequence":"first","affiliation":[{"name":"EaStCHEM School of Chemistry University of Edinburgh  David Brewster Road EH9 3FJ Edinburgh UK"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Scott","family":"Hoffmann","sequence":"additional","affiliation":[{"name":"University of Edinburgh\/BHF Centre for Cardiovascular Science Queen's Medical Research Institute  47 Little France Crescent EH16 4TJ Edinburgh UK"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Annamaria","family":"Lilienkampf","sequence":"additional","affiliation":[{"name":"EaStCHEM School of Chemistry University of Edinburgh  David Brewster Road EH9 3FJ Edinburgh UK"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Logan","family":"Mackay","sequence":"additional","affiliation":[{"name":"EaStCHEM School of Chemistry University of Edinburgh  David Brewster Road EH9 3FJ Edinburgh UK"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Rahimi M.","family":"Yusop","sequence":"additional","affiliation":[{"name":"School of Chemical Sciences and Food Technology Faculty of Science and Technology Universiti Kebangsaan Malaysia  43600 Bangi Selangor Malaysia"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Sebastien A.","family":"Rider","sequence":"additional","affiliation":[{"name":"University of Edinburgh\/BHF Centre for Cardiovascular Science Queen's Medical Research Institute  47 Little France Crescent EH16 4TJ Edinburgh UK"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"John J.","family":"Mullins","sequence":"additional","affiliation":[{"name":"University of Edinburgh\/BHF Centre for Cardiovascular Science Queen's Medical Research Institute  47 Little France Crescent EH16 4TJ Edinburgh UK"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Mark","family":"Bradley","sequence":"additional","affiliation":[{"name":"EaStCHEM School of Chemistry University of Edinburgh  David Brewster Road EH9 3FJ Edinburgh UK"}],"role":[{"vocabulary":"crossref","role":"author"}]}],"member":"311","published-online":{"date-parts":[[2016,11,15]]},"reference":[{"key":"e_1_2_2_1_1","doi-asserted-by":"publisher","DOI":"10.1038\/nchembio0605-13"},{"key":"e_1_2_2_2_1","doi-asserted-by":"publisher","DOI":"10.1038\/nmeth.1657"},{"key":"e_1_2_2_3_1","doi-asserted-by":"publisher","DOI":"10.1039\/b925931g"},{"key":"e_1_2_2_4_1","doi-asserted-by":"publisher","DOI":"10.1002\/1521-3773(20010601)40:11<2004::AID-ANIE2004>3.0.CO;2-5"},{"key":"e_1_2_2_4_2","doi-asserted-by":"publisher","DOI":"10.1002\/1521-3757(20010601)113:11<2056::AID-ANGE2056>3.0.CO;2-W"},{"key":"e_1_2_2_5_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.cbpa.2014.07.002"},{"key":"e_1_2_2_6_1","first-page":"263","volume-title":"Pept. 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