{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2025,11,26]],"date-time":"2025-11-26T23:56:31Z","timestamp":1764201391010,"version":"3.46.0"},"reference-count":22,"publisher":"Georg Thieme Verlag KG","issue":"06","funder":[{"DOI":"10.13039\/501100004681","name":"Higher Education Commission, Pakistan","doi-asserted-by":"crossref","award":["NRPU # 17226"],"award-info":[{"award-number":["NRPU # 17226"]}],"id":[{"id":"10.13039\/501100004681","id-type":"DOI","asserted-by":"crossref"}]}],"content-domain":{"domain":[],"crossmark-restriction":false},"short-container-title":["Nuklearmedizin"],"published-print":{"date-parts":[[2025,12]]},"abstract":"<jats:title>Abstract<\/jats:title>\n                  <jats:p>To develop a site-specifically radiolabeled version of IMMU-132 (sacituzumab govitecan) using zirconium-89 (\u2078\u2079Zr) with the chelator 3,4,3-LI(1,2-HOPO) and evaluate its stability, specificity, and quantitative targeting ability in TROP-2\u2013positive prostate cancer models.<\/jats:p>\n                  <jats:p>IMMU-132 was conjugated to 3,4,3-LI(1,2-HOPO)-maleimide and its integrity was confirmed by SDS-PAGE, SE-HPLC and mass spectrometry. Radiolabeling with \u2078\u2079Zr was performed, and radiochemical yield and purity were measured. In vitro stability was assessed in human serum at 37\u202f\u00b0C for 120 h. Binding affinity and specificity were evaluated using PC3 (TROP-2\u207a) and A549 (TROP-2\u207b) cells. Immunoreactivity was determined by Lindmo assay. In vivo PET imaging and ex vivo biodistribution were conducted in PC3-TROP-2\u207a xenograft-bearing mice.<\/jats:p>\n                  <jats:p>Radiolabeling with \u2078\u2079Zr yielded 71.88 \u00b1 0.21% with a radiochemical purity of 98.70 \u00b1 0.55%. The radioconjugate maintained &gt;90% stability in serum over 120 h. High-specific binding was observed in PC3 cells (Bmax \u2248 4750 CPM; Kd = 0.4 \u00d7 10\u2076 cells\/mL), with minimal uptake in A549 cells. The immunoreactive fraction was 88.10%. PET imaging revealed tumor-specific accumulation with a peak SUV mean of 5.8 \u00b1 0.7 at 72 h post-injection. Biodistribution confirmed high tumor uptake (19.4 \u00b1 2.1 %ID\/g) and significantly reduced bone uptake (3.2 \u00b1 0.5 %ID\/g) compared to conventional \u2078\u2079Zr-DFO tracers (p &lt; 0.01).<\/jats:p>\n                  <jats:p>\u2078\u2079Zr\u2013IMMU-132\u2013HOPO exhibits excellent in vivo stability, specificity, and selective accumulation in TROP-2\u2013positive prostate tumors, while minimizing off-target bone uptake. These findings support its potential as a next-generation immuno-radiopharmaceutical for quantitative TROP-2 imaging and future theranostic applications in prostate cancer.<\/jats:p>","DOI":"10.1055\/a-2723-3284","type":"journal-article","created":{"date-parts":[[2025,11,26]],"date-time":"2025-11-26T23:52:11Z","timestamp":1764201131000},"page":"332-340","source":"Crossref","is-referenced-by-count":0,"title":["Targeting TROP-2 in Prostate Cancer Using Site-Specifically Radiolabeled IMMU-132 with \u2078\u2079Zr via 3,4,3-LI(1,2-HOPO)"],"prefix":"10.1055","volume":"64","author":[{"given":"Syed Qaiser","family":"Shah","sequence":"additional","affiliation":[{"name":"Institute of Chemical Sciences, University of Peshawar Faculty of Life and Environmental Sciences, Peshawar, Pakistan"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Ralph","family":"Santos-Oliveira","sequence":"additional","affiliation":[{"name":"Laboratory of Nano-Radiopharmacy, Nuclear Engineering Institute, Av. Helio de Almeida, 75, Ilha do Fund\u00e3o, Rio de Janeiro, 21941906, Brazil, Brazilian Nuclear Energy Commission, Rio de Janeiro, Brazil"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"DeryaIlem","family":"Ozdemir","sequence":"additional","affiliation":[{"name":"Faculty of Pharmacy Department of Radiopharmacy, Bornova, \u0130zmir, Ege University, Izmir, Turkey"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Saba","family":"Shirin","sequence":"additional","affiliation":[{"name":"Nuclear Medicine Research Laboratory, Institute of Chemical Sciences University of Peshawar, Peshawar, 25120 K.P, Pakistan, University of Peshawar Faculty of Life and Environmental Sciences, Peshawar, Pakistan"}],"role":[{"role":"author","vocabulary":"crossref"}]}],"member":"194","published-online":{"date-parts":[[2025,11,26]]},"reference":[{"issue":"01","key":"ref1","doi-asserted-by":"publisher","first-page":"17","DOI":"10.3322\/caac.21763","article-title":"Cancer statistics, 2023","volume":"73","author":"RL Siegel","year":"2023","journal-title":"CA Cancer J Clin"},{"issue":"09","key":"ref2","doi-asserted-by":"publisher","first-page":"683","DOI":"10.1038\/nrc882","article-title":"Molecular imaging of cancer with positron emission tomography","volume":"2","author":"SS Gambhir","year":"2002","journal-title":"Nat Rev Cancer"},{"issue":"08","key":"ref3","doi-asserted-by":"publisher","first-page":"1096","DOI":"10.1002\/ddr.21870","article-title":"Recent advances in trophoblast cell\u2010surface antigen 2 targeted therapy for solid tumors","volume":"82","author":"S Liao","year":"2021","journal-title":"Drug Dev Res"},{"issue":"48","key":"ref4","doi-asserted-by":"publisher","first-page":"28989","DOI":"10.18632\/oncotarget.25615","article-title":"The emergence of trophoblast cell-surface antigen 2 (TROP-2) as a novel cancer target","volume":"9","author":"DM Goldenberg","year":"2018","journal-title":"Oncotarget"},{"issue":"06","key":"ref5","doi-asserted-by":"crossref","first-page":"746","DOI":"10.1016\/j.annonc.2021.03.005","article-title":"Sacituzumab govitecan, a Trop-2-directed antibody-drug conjugate, for patients with epithelial cancer: final safety and efficacy results from the phase I\/II IMMU-132\u201301 basket trial","volume":"32","author":"A Bardia","year":"2021","journal-title":"Ann Oncol"},{"issue":"12","key":"ref8","doi-asserted-by":"publisher","first-page":"2579","DOI":"10.1021\/acs.bioconjchem.5b00572","article-title":"p-SCN-Bn-HOPO: A superior bifunctional chelator for 89Zr immunoPET","volume":"26","author":"MA Deri","year":"2015","journal-title":"BioconjugChem"},{"key":"ref9","doi-asserted-by":"crossref","first-page":"371","DOI":"10.1007\/978-3-319-98947-1_21","volume-title":"The radiopharmaceutical chemistry of zirconium-89. 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