ArticleEuropean journal of nuclear medicine and molecular imaging2024
A rationally designed nuclei-targeting FAPI 04-based molecular probe with enhanced tumor uptake for PET/CT and fluorescence imaging.
Article in European journal of nuclear medicine and molecular imaging, 2024. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 12 papers, 1 of them a synthesis that pooled it.
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Who cites it
12 citing papers in PubMed, 1 synthesis or guideline pooled it, 36 citations in OpenAlex.
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- Novel dimeric dual-modality FAP-targeted agents with favorable tumor retention for image-guided surgery: a preclinical study.European journal of nuclear medicine and molecular imaging · 2026Article
- Preclinical and pilot clinical evaluation of novel dual-modality pet/fluorescence probes targeting FAP for accurate tumor margin delineation.European journal of nuclear medicine and molecular imaging · 2026Article
- Synthesis and preclinical evaluation of FAP-targeting radiotracers for PET and optical imaging.EJNMMI radiopharmacy and chemistry · 2025Article
- Cancer-Associated Fibroblasts: Heterogeneity, Cancer Pathogenesis, and Therapeutic Targets.MedComm · 2025Review
- Next generation drug clearance insights: real-time tracking in hepatobiliary and renal systems.Light, science & applications · 2025Article
- Quantitative pharmacodynamics functional evaluation of Chinese medicine Qizhu formula in mice with dynamic near-infrared photoacoustic imaging.Photoacoustics · 2025Article
- FAP-Targeted Fluorescent Imaging Agents to Study Cancer-Associated Fibroblasts In Vivo.Bioconjugate chemistry · 2025Article
- Article
- Early diagnosis and staging of paraquat-induced pulmonary fibrosis using [EJNMMI research · 2024Article
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Authors and funding
8 authors at 3 institutions in 1 country.
Funding
Abstract
purposeFibroblast activation protein inhibitor (FAPI) -based probes have been widely studied in the diagnosis of various malignant tumors with positron emission tomography/computed tomography (PET/CT). However, current imaging studies of FAPI-based probes face challenges in rapid clearance rate and potential false-negative results. Furthermore, FAPI has been rarely explored in optical imaging. Considering this, further modifications are imperative to improve the properties of FAPI-based probes to address existing limitations and broaden their application scenarios. In this study, we rationally introduced methylene blue (MB) to FAPIs, thereby imparting nuclei-targeting and fluorescence imaging capabilities to the probes. Furthermore, we evaluated the added value of FAPI-based fluorescence imaging to traditional PET/CT, exploring the potential application of FAPI-based probes in intraoperative fluorescence imaging.
methodsA new FAPI-based probe, namely NOTA-FAPI-MB, was designed for both PET/CT and fluorescence imaging by conjugation of MB. The targeting efficacy of the probe was evaluated on fibroblast activation protein (FAP)-transfected cell line and human primary cancer-associated fibroblasts (CAFs). Subsequently, PET/CT and fluorescence imaging were conducted on tumor-bearing mice. The tumor detection and boundary delineation were assessed by fluorescence imaging of tissues from hepatocellular carcinoma (HCC) patients.
resultsNOTA-FAPI-MB demonstrated exceptional targeting ability towards FAP-transfected cells and CAFs in comparison to NOTA-FAPI. This benefit arises from the cationic methylene blue (MB) affinity for anionic nucleic acids. PET/CT imaging of tumor-bearing mice revealed significantly higher tumor uptake of [
conclusionsThe NOTA-FAPI-MB was successfully synthesized, in which FAPI and MB simultaneously contributed to the targeting effect. Notably, the nuclear delivery mechanism of the probes improved intracellular retention time and targeting efficacy, broadening the imaging time window for fluorescence imaging. In vivo PET/CT demonstrated favorable performance of NOTA-FAPI-MB compared to [
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