{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2025,12,12]],"date-time":"2025-12-12T05:30:30Z","timestamp":1765517430244,"version":"3.48.0"},"reference-count":41,"publisher":"MDPI AG","issue":"12","license":[{"start":{"date-parts":[[2025,12,10]],"date-time":"2025-12-10T00:00:00Z","timestamp":1765324800000},"content-version":"vor","delay-in-days":0,"URL":"https:\/\/creativecommons.org\/licenses\/by\/4.0\/"}],"funder":[{"DOI":"10.13039\/501100001809","name":"National Natural Science Foundation of China","doi-asserted-by":"crossref","award":["U24A20758"],"award-info":[{"award-number":["U24A20758"]}],"id":[{"id":"10.13039\/501100001809","id-type":"DOI","asserted-by":"crossref"}]},{"DOI":"10.13039\/501100004826","name":"Beijing Natural Science Foundation","doi-asserted-by":"publisher","award":["L242062"],"award-info":[{"award-number":["L242062"]}],"id":[{"id":"10.13039\/501100004826","id-type":"DOI","asserted-by":"publisher"}]},{"DOI":"10.13039\/501100012166","name":"National Key R&D Program of China","doi-asserted-by":"publisher","award":["2024YFC2419400"],"award-info":[{"award-number":["2024YFC2419400"]}],"id":[{"id":"10.13039\/501100012166","id-type":"DOI","asserted-by":"publisher"}]},{"name":"Chinese Academy of Medical Sciences Innovation Fund for Medical Sciences","award":["CIFMS-2024-I2M-ZD-001"],"award-info":[{"award-number":["CIFMS-2024-I2M-ZD-001"]}]},{"name":"Chinese Academy of Medical Sciences Innovation Fund for Medical Sciences","award":["CIFMS-2023-I2M-2-002"],"award-info":[{"award-number":["CIFMS-2023-I2M-2-002"]}]},{"name":"Chinese Academy of Medical Sciences Innovation Fund for Medical Sciences","award":["CIFMS-2021-I2M-1-002"],"award-info":[{"award-number":["CIFMS-2021-I2M-1-002"]}]},{"name":"Chinese Academy of Medical Sciences Innovation Fund for Medical Sciences","award":["CIFMS-2021-I2M-1-003"],"award-info":[{"award-number":["CIFMS-2021-I2M-1-003"]}]},{"name":"Chinese Academy of Medical Sciences Innovation Fund for Medical Sciences","award":["CIFMS-2021-I2M-1-025"],"award-info":[{"award-number":["CIFMS-2021-I2M-1-025"]}]},{"name":"National High Level Hospital Clinical Research Funding","award":["2022-PUMCH-D-001"],"award-info":[{"award-number":["2022-PUMCH-D-001"]}]},{"name":"National High Level Hospital Clinical Research Funding","award":["2022-PUMCH-D-002"],"award-info":[{"award-number":["2022-PUMCH-D-002"]}]}],"content-domain":{"domain":[],"crossmark-restriction":false},"short-container-title":["Pharmaceutics"],"abstract":"<jats:p>Background: Inflammatory bowel diseases (IBD) rely on invasive methods for detecting intestinal inflammation, with the needs for non-invasive molecular imaging tools being unmet. Integrin \u03b14\u03b27 is a key target in IBD pathogenesis due to its role in the recruitment of T cells. This study aimed to develop a novel 68Ga-labeled integrin \u03b14\u03b27-targeted radiopharmaceutical (68Ga-A2) and evaluate its feasibility for non-invasive PET\/CT imaging of IBD inflammation in a dextran sulfate sodium (DSS)-induced murine colitis model. Methods: 68Ga-A2 was synthesized via radiolabeling DOTA-A2 with 68Ga. In vitro properties (radiochemical purity, stability, binding specificity, and affinity) of 68Ga-A2 were validated. The DSS-induced colitis model was established and confirmed in C57BL\/6J mice, followed by in vivo PET\/CT imaging, ex vivo biodistribution studies, and histological (HE and IHC) analyses to evaluate the targeting efficacy of 68Ga-A2. Results: 68Ga-A2 was prepared efficiently (20 min) with a radiochemical purity of &gt;95% and demonstrated good in vitro stability. It exhibited specific binding to integrin \u03b14\u03b27 with a Kd of 68.48 \u00b1 6.55 nM. While whole-body PET\/CT showed no visible inflammatory focus uptake, ex vivo imaging and biodistribution of colon tissue revealed significantly higher uptake in DSS-treated mice compared to that in healthy\/blocking groups, which was consistent with histological evidence of inflammation. Conclusions: 68Ga-A2 demonstrated specific targeting of IBD inflammatory foci in vitro and ex vivo. Despite whole-body imaging limitations, further optimization of its structure may enable it to become a promising non-invasive PET agent for IBD. These findings support future clinical investigations to validate its utility in IBD diagnosis and monitoring.<\/jats:p>","DOI":"10.3390\/pharmaceutics17121591","type":"journal-article","created":{"date-parts":[[2025,12,10]],"date-time":"2025-12-10T12:20:57Z","timestamp":1765369257000},"page":"1591","update-policy":"https:\/\/doi.org\/10.3390\/mdpi_crossmark_policy","source":"Crossref","is-referenced-by-count":0,"title":["A Novel 68Ga-Labeled Integrin \u03b14\u03b27-Targeted Radiopharmaceutical for PET\/CT Imaging of DSS-Induced Murine Colitis"],"prefix":"10.3390","volume":"17","author":[{"given":"Guangjie","family":"Yang","sequence":"first","affiliation":[{"name":"Department of Nuclear Medicine, State Key Laboratory of Complex, Severe, and Rare Diseases, Center for Rare Diseases Research, Peking Union Medical College Hospital, Chinese Academy of Medical Science and Peking Union Medical College, Beijing 100730, China"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Haiqiong","family":"Zhang","sequence":"additional","affiliation":[{"name":"Department of Nuclear Medicine, State Key Laboratory of Complex, Severe, and Rare Diseases, Center for Rare Diseases Research, Peking Union Medical College Hospital, Chinese Academy of Medical Science and Peking Union Medical College, Beijing 100730, China"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Li","family":"Huo","sequence":"additional","affiliation":[{"name":"Department of Nuclear Medicine, State Key Laboratory of Complex, Severe, and Rare Diseases, Center for Rare Diseases Research, Peking Union Medical College Hospital, Chinese Academy of Medical Science and Peking Union Medical College, Beijing 100730, China"}],"role":[{"role":"author","vocabulary":"crossref"}]}],"member":"1968","published-online":{"date-parts":[[2025,12,10]]},"reference":[{"key":"ref_1","doi-asserted-by":"crossref","first-page":"371","DOI":"10.1038\/s41575-024-01035-7","article-title":"Understanding the Therapeutic Toolkit for Inflammatory Bowel Disease","volume":"22","author":"Vieujean","year":"2025","journal-title":"Nat. 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