{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,9,25]],"date-time":"2026-09-25T19:41:35Z","timestamp":1790365295213,"version":"4.1.0"},"reference-count":43,"publisher":"MDPI AG","issue":"16","license":[{"start":{"date-parts":[[2023,8,11]],"date-time":"2023-08-11T00:00:00Z","timestamp":1691712000000},"content-version":"vor","delay-in-days":0,"URL":"https:\/\/creativecommons.org\/licenses\/by\/4.0\/"}],"funder":[{"name":"Ministry of Science and ICT of the Republic of Korea","award":["50543-2023"],"award-info":[{"award-number":["50543-2023"]}]}],"content-domain":{"domain":[],"crossmark-restriction":false},"short-container-title":["Diagnostics"],"abstract":"<jats:p>Background: This study compared the effects of 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid (DOTA) and 1,4,7-triazacyclononane-1,4,7-triacetic acid (NOTA) as 64Cu-chelating agents in newly developed prostate-specific membrane antigen (PSMA) target compounds, 64Cu-cudotadipep and 64Cu-cunotadipep, on pharmacokinetics. Methods: The in vitro stability of the chelators was evaluated using human and mouse serum. In vitro PSMA-binding affinity and cell uptake were compared using human 22Rv1 cells. To evaluate specific PSMA-expressing tumor-targeting efficiency, micro-positron emission tomography (mcroPET)\/computed tomography (CT) and biodistribution analysis were performed using PSMA+ PC3-PIP and PSMA\u2212 PC3-flu tumor xenografts. Results: The serum stability of DOTA- or NOTA-conjugated 64Cu-cudotadipep and 64Cu-cunotadipep was &gt;97%. The Ki value of the NOTA derivative, cunotadipep, in the in vitro affinity binding analysis was higher (2.17 \u00b1 0.25 nM) than that of the DOTA derivative, cudotadipep (6.75 \u00b1 0.42 nM). The cunotadipep exhibited a higher cellular uptake (6.02 \u00b1 0.05%\/1 \u00d7 106 cells) compared with the cudotadipep (2.93 \u00b1 0.06%\/1 \u00d7 106 cells). In the biodistribution analysis and microPET\/CT imaging, the 64Cu-labeled NOTA derivative, 64Cu-cunotadipep, demonstrated a greater tumor uptake and lower liver uptake than the DOTA derivative. Conclusions: This study indicates that the PSMA-targeted 64Cu-cunotadipep can be applied in clinical practice owing to its high diagnostic power for prostate cancer.<\/jats:p>","DOI":"10.3390\/diagnostics13162649","type":"journal-article","created":{"date-parts":[[2023,8,11]],"date-time":"2023-08-11T10:33:23Z","timestamp":1691750003000},"page":"2649","update-policy":"https:\/\/doi.org\/10.3390\/mdpi_crossmark_policy","source":"Crossref","is-referenced-by-count":15,"title":["Comparison of the Effects of DOTA and NOTA Chelators on 64Cu-Cudotadipep and 64Cu-Cunotadipep for Prostate Cancer"],"prefix":"10.3390","volume":"13","author":[{"given":"Inki","family":"Lee","sequence":"first","affiliation":[{"name":"Department of Nuclear Medicine, Korea Institute of Radiological & Medical Sciences, Seoul 01812, Republic of Korea"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Min Hwan","family":"Kim","sequence":"additional","affiliation":[{"name":"Research Institute of Radiopharmaceuticals, FutureChem Co., Ltd., Seoul 04793, Republic of Korea"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Kyongkyu","family":"Lee","sequence":"additional","affiliation":[{"name":"Research Institute of Radiopharmaceuticals, FutureChem Co., Ltd., Seoul 04793, Republic of Korea"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Keumrok","family":"Oh","sequence":"additional","affiliation":[{"name":"Research Institute of Radiopharmaceuticals, FutureChem Co., Ltd., Seoul 04793, Republic of Korea"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Hyunwoo","family":"Lim","sequence":"additional","affiliation":[{"name":"Research Institute of Radiopharmaceuticals, FutureChem Co., Ltd., Seoul 04793, Republic of Korea"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Jae Hun","family":"Ahn","sequence":"additional","affiliation":[{"name":"Division of Applied RI, Korea Institute of Radiological & Medical Sciences, Seoul 01812, Republic of Korea"},{"name":"Graduate School of Translational Medicine, Seoul National University College of Medicine, Seoul 03080, Republic of Korea"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Yong Jin","family":"Lee","sequence":"additional","affiliation":[{"name":"Division of Applied RI, Korea Institute of Radiological & Medical Sciences, Seoul 01812, Republic of Korea"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Gi Jeong","family":"Cheon","sequence":"additional","affiliation":[{"name":"Department of Nuclear Medicine, Seoul National University College of Medicine, Seoul 03080, Republic of Korea"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Dae Yoon","family":"Chi","sequence":"additional","affiliation":[{"name":"Research Institute of Radiopharmaceuticals, FutureChem Co., Ltd., Seoul 04793, Republic of Korea"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Sang Moo","family":"Lim","sequence":"additional","affiliation":[{"name":"Department of Nuclear Medicine, Korea Institute of Radiological & Medical Sciences, Seoul 01812, Republic of Korea"}],"role":[{"vocabulary":"crossref","role":"author"}]}],"member":"1968","published-online":{"date-parts":[[2023,8,11]]},"reference":[{"key":"ref_1","first-page":"235","article-title":"Current State of Biomarkers for the Diagnosis and Assessment of Treatment Efficacy of Prostate Cancer","volume":"27","author":"Liu","year":"2019","journal-title":"Discov. 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