{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,9,15]],"date-time":"2026-09-15T16:05:06Z","timestamp":1789488306025,"version":"build-2803163510"},"reference-count":18,"publisher":"American Chemical Society (ACS)","issue":"36","license":[{"start":{"date-parts":[[2026,9,8]],"date-time":"2026-09-08T00:00:00Z","timestamp":1788825600000},"content-version":"stm-asf","delay-in-days":0,"URL":"https:\/\/doi.org\/10.15223\/policy-029"},{"start":{"date-parts":[[2026,9,8]],"date-time":"2026-09-08T00:00:00Z","timestamp":1788825600000},"content-version":"stm-asf","delay-in-days":0,"URL":"https:\/\/doi.org\/10.15223\/policy-037"},{"start":{"date-parts":[[2026,9,8]],"date-time":"2026-09-08T00:00:00Z","timestamp":1788825600000},"content-version":"stm-asf","delay-in-days":0,"URL":"https:\/\/doi.org\/10.15223\/policy-045"}],"funder":[{"DOI":"10.13039\/501100012600","name":"ShanghaiTech University","doi-asserted-by":"publisher","award":["2021F0209-000-04"],"award-info":[{"award-number":["2021F0209-000-04"]}],"id":[{"id":"10.13039\/501100012600","id-type":"DOI","asserted-by":"publisher"}]},{"DOI":"10.13039\/501100015377","name":"Shanghai Key Laboratory of Molecular Imaging","doi-asserted-by":"publisher","award":["18DZ2260400"],"award-info":[{"award-number":["18DZ2260400"]}],"id":[{"id":"10.13039\/501100015377","id-type":"DOI","asserted-by":"publisher"}]}],"content-domain":{"domain":[],"crossmark-restriction":false},"short-container-title":[],"published-print":{"date-parts":[[2026,9,15]]},"abstract":"<jats:title>Abstract<\/jats:title>\n                  <jats:p>The colony-stimulating factor 1 receptor (CSF1R) is a highly promising target for the noninvasive imaging of macrophage-driven inflammatory diseases. To develop a targeted molecular tracer, we first discovered a high-affinity peptide ligand (CP, KD = 0.188 \u03bcM) toward CSF1R using mRNA display. We then designed and synthesized a series of DOTA-conjugated peptides (CP0-CP4) featuring systematically extended hydrophilic (2-(2-aminoethoxy)ethoxy)acetic acid (AEEA) linkers. Upon 68Ga-labeling, linker elongation progressively enhanced the tracer\u2019s hydrophilicity and dramatically improved its serum stability (intact fraction at 60 min increased from 12.0% for 68Ga-CP0 to 84.1% for 68Ga-CP4). The optimized candidate, 68Ga-CP4, demonstrated specific binding and internalization in CSF1R-overexpressing cells. In normal mice, increasing linker length effectively reduced nonspecific uptake and promoted rapid renal clearance. In a murine model of LPS-induced pulmonary inflammation, 68Ga-CP4 clearly visualized inflamed lungs, with significantly higher uptake (SUV 2.40 \u00b1 0.39 at 60 min) compared to sham controls (1.81 \u00b1 0.10). Specificity was confirmed by effective blockade with unlabeled peptide (SUV 0.89 \u00b1 0.16) and ex vivo biodistribution. CSF1R protein upregulation in inflamed lungs was further validated by immunohistochemical staining and Western blot. This work presents 68Ga-CP4 as a novel, peptide-based PET tracer for imaging CSF1R-positive inflammation.<\/jats:p>","DOI":"10.1021\/acs.analchem.6c04084","type":"journal-article","created":{"date-parts":[[2026,9,8]],"date-time":"2026-09-08T12:01:48Z","timestamp":1788868908000},"page":"27009-27020","source":"Crossref","is-referenced-by-count":0,"title":["Development\nof CSF1R-Targeted Peptide Tracers for\nPET Imaging of LPS-Induced Pulmonary Inflammation"],"prefix":"10.1021","volume":"98","author":[{"given":"Junyu","family":"Bao","sequence":"first","affiliation":[{"name":"Academy of Traditional Chinese Medicine of Tianjin University of Traditional Chinese Medicine , ,","place":["Tianjin, China, 301617"]},{"name":"Shanghai Institute of Materia Medica, Chinese Academy of Sciences , , ,","place":["Shanghai, China, 201203"]},{"name":"ShanghaiTech University , , ,","place":["Shanghai, China, 201210"]}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0009-0009-2034-5878","authenticated-orcid":true,"given":"Jiawen","family":"Huang","sequence":"additional","affiliation":[{"name":"ShanghaiTech University , , ,","place":["Shanghai, China, 201210"]}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Chuan","family":"Chen","sequence":"additional","affiliation":[{"name":"Academy of Traditional Chinese Medicine of Tianjin University of Traditional Chinese Medicine , ,","place":["Tianjin, China, 301617"]},{"name":"Shanghai Institute of Materia Medica, Chinese Academy of Sciences , , ,","place":["Shanghai, China, 201203"]},{"name":"ShanghaiTech University , , ,","place":["Shanghai, China, 201210"]}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Wenxue","family":"Hui","sequence":"additional","affiliation":[{"name":"ShanghaiTech University , , ,","place":["Shanghai, China, 201210"]}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Xiaochuan","family":"Zha","sequence":"additional","affiliation":[{"name":"ShanghaiTech University , , ,","place":["Shanghai, China, 201210"]}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Kezhi","family":"Ding","sequence":"additional","affiliation":[{"name":"ShanghaiTech University , , ,","place":["Shanghai, China, 201210"]}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Yabin","family":"Yang","sequence":"additional","affiliation":[{"name":"ShanghaiTech University , , ,","place":["Shanghai, China, 201210"]}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0001-8177-9463","authenticated-orcid":true,"given":"Zhen","family":"Cheng","sequence":"additional","affiliation":[{"name":"Shanghai Institute of Materia Medica, Chinese Academy of Sciences , , ,","place":["Shanghai, China, 201203"]},{"name":"ShanghaiTech University , , ,","place":["Shanghai, China, 201210"]}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0009-0004-0064-775X","authenticated-orcid":true,"given":"Zonghua","family":"Luo","sequence":"additional","affiliation":[{"name":"ShanghaiTech University , , ,","place":["Shanghai, China, 201210"]},{"name":"Shanghai Clinical Research and Trial Center , ,","place":["Shanghai, China, 201210"]}],"role":[{"vocabulary":"crossref","role":"author"}]}],"member":"316","published-online":{"date-parts":[[2026,9,8]]},"reference":[{"key":"2026091511074000300_cit1","doi-asserted-by":"publisher","first-page":"117187","DOI":"10.1016\/j.bcp.2025.117187","article-title":"Recent advances\nin colony stimulating factor-1 receptor (CSF1R) inhibitors","volume":"242","author":"Peng","year":"2025","journal-title":"Biochem. 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Blood Flow Metab"},{"issue":"8","key":"2026091511074000300_cit7","doi-asserted-by":"publisher","first-page":"3979","DOI":"10.1021\/acs.molpharmaceut.4c00337","article-title":"Evaluation\nof a positron emission tomography tracer targeting colony-stimulating\nfactor 1 receptor for detecting pulmonary inflammation","volume":"21","author":"Hui","year":"2024","journal-title":"Mol. Pharmaceutics"},{"issue":"4","key":"2026091511074000300_cit8","doi-asserted-by":"publisher","first-page":"614","DOI":"10.1021\/acsptsci.3c00003","article-title":"Discovery\nof a high-affinity fluoromethyl analog of [11C]5-cyano-N-(4-(4-methylpiperazin-1-yl)-2-(piperidin-1-yl)phenyl)furan-2-carboxamide\n([11C]CPPC) and their comparison in mouse and monkey as\ncolony-stimulating factor 1 receptor positron emission tomography\nradioligands","volume":"6","author":"Altomonte","year":"2023","journal-title":"ACS Pharmacol. Transl. 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