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The HBED\u2010CC is an acyclic chelating agent that is rapidly labeled with <jats:sup>68<\/jats:sup>Ga under mild conditions. To target cancer cells, bioactive substances can be conjugated to the carboxyl terminus of HBED\u2010CC. Because folic acid strongly binds to folate receptors that are overexpressed on the surfaces of many types of cancer cells, it was coupled with HBED\u2010CC through a small polyethylene glycol\u2010based linker (EDBE) to generate an active, receptor\u2010selective targeting system. The HBED\u2010CC\u2010EDBE\u2010folate (HCEF) precursor was readily labeled with <jats:sup>68<\/jats:sup>Ga in 5\u00a0minutes at room temperature (98% radiochemical yield; 99% radiochemical purity after isolation). In cellular uptake tests, higher uptakes of <jats:sup>68<\/jats:sup>Ga\u2010HCEF were observed for the CT26 and KB cell lines (which express folate receptors) than for the A549 cell line (which does not). Finally, <jats:italic>in vivo<\/jats:italic> micro\u2010PET measurements over 2\u00a0hours of binding in BALB\/c mice into which CT26 tumors had been transplanted showed the selective accumulation of <jats:sup>68<\/jats:sup>Ga\u2010HCEF in the folate receptor\u2010expressing CT26 tumors. These results confirmed the potential of <jats:sup>68<\/jats:sup>Ga\u2010HCEF as a PET diagnostic agent for tumors that express folate receptors.<\/jats:p>","DOI":"10.1002\/jlcr.3563","type":"journal-article","created":{"date-parts":[[2017,9,13]],"date-time":"2017-09-13T07:04:43Z","timestamp":1505286283000},"page":"4-10","source":"Crossref","is-referenced-by-count":15,"title":["Synthesis and evaluation of <sup>68<\/sup><scp>Ga\u2010HBED\u2010CC\u2010EDBE<\/scp>\u2010folate for <scp>positron\u2010emission tomography<\/scp> imaging of overexpressed folate receptors on CT26 tumor cells"],"prefix":"10.1002","volume":"61","author":[{"ORCID":"https:\/\/orcid.org\/0000-0003-2953-4703","authenticated-orcid":false,"given":"Pyeong Seok","family":"Choi","sequence":"first","affiliation":[{"name":"Department of Advanced Materials Chemistry Dongguk University  Gyeongju Republic of Korea"},{"name":"Radiation Instrumentation Research Division Korea Atomic Energy Research Institute  Jeongeup Republic of Korea"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Jun Young","family":"Lee","sequence":"additional","affiliation":[{"name":"Radiation Instrumentation Research Division Korea Atomic Energy Research Institute  Jeongeup Republic of Korea"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Jeong Hoon","family":"Park","sequence":"additional","affiliation":[{"name":"Radiation Instrumentation Research Division Korea Atomic Energy Research Institute  Jeongeup Republic of Korea"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Sang Wook","family":"Kim","sequence":"additional","affiliation":[{"name":"Department of Advanced Materials Chemistry Dongguk University  Gyeongju Republic of Korea"}],"role":[{"vocabulary":"crossref","role":"author"}]}],"member":"311","published-online":{"date-parts":[[2017,12,29]]},"reference":[{"key":"e_1_2_6_2_1","doi-asserted-by":"publisher","DOI":"10.1021\/cr1000755"},{"key":"e_1_2_6_3_1","doi-asserted-by":"publisher","DOI":"10.1007\/s00259-010-1597-8"},{"key":"e_1_2_6_4_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.ica.2012.01.061"},{"key":"e_1_2_6_5_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.nucmedbio.2012.01.003"},{"key":"e_1_2_6_6_1","doi-asserted-by":"crossref","first-page":"18","DOI":"10.5005\/jp-journals-10028-1052","article-title":"68Ge\/68Ga generators and 68Ga radiopharmaceutical chemistry on their way into a new century","volume":"47","author":"R\u00f6sch F","year":"2013","journal-title":"J Postgrad Med Educ Res"},{"key":"e_1_2_6_7_1","first-page":"3","article-title":"68Ga somatostatin analog radiolabeling: the radiopharmacist's point of view","volume":"39","author":"Lamesa C","year":"2015","journal-title":"Med 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