A5038987411- Peptidase Inhibition and Analysis
- Radiopharmaceutical Chemistry and Applications
- interferon and immune responses
- Cardiac Structural Anomalies and Repair
- Medical Imaging Techniques and Applications
- Cancer Immunotherapy and Biomarkers
- Neuropeptides and Animal Physiology
- Estrogen and related hormone effects
- Prostate Cancer Treatment and Research
- Cytokine Signaling Pathways and Interactions
- Immune Response and Inflammation
- Nanoplatforms for cancer theranostics
- HER2/EGFR in Cancer Research
- Protease and Inhibitor Mechanisms
- Immunotherapy and Immune Responses
- ATP Synthase and ATPases Research
- Monoclonal and Polyclonal Antibodies Research
- Cancer, Hypoxia, and Metabolism
- Click Chemistry and Applications
- Viral Infections and Vectors
- Orthopedic Infections and Treatments
- Infective Endocarditis Diagnosis and Management
- Ubiquitin and proteasome pathways
- Gastroesophageal reflux and treatments
- Signaling Pathways in Disease
Xiamen University
2019-2025
Central South University
2021
Rütgers (Germany)
2021
Rutgers, The State University of New Jersey
2021
Rutgers Sexual and Reproductive Health and Rights
2021
Xiamen University of Technology
2020
Cancer-associated fibroblasts (CAFs) are crucial components of the tumor microenvironment. Fibroblast activation protein (FAP) is overexpressed in CAFs. FAP-targeted molecular imaging agents, including FAP inhibitors (FAPIs) 04 and 46, have shown promising results diagnosis. However, these molecules a relatively short tumor-retention time for peptide-targeted radionuclide therapy applications. We aimed to design 68Ga-labeled FAPI dimer, 68Ga-DOTA-2P(FAPI)2, optimize pharmacokinetics evaluate...
Radiolabeled fibroblast activation protein (FAP) inhibitors (FAPIs) have shown promise as cancer diagnostic agents; however, the relatively short tumor retention of FAPIs may limit their application in radioligand therapy. In this paper, we report design, synthesis, and evaluation a FAPI tetramer. The aim study was to evaluate tumor-targeting characteristics radiolabeled multimers in vitro in vivo, thereby providing information for design FAP-targeted radiopharmaceuticals based on...
Extensive research has been conducted on radiolabeled fibroblast activation protein (FAP) inhibitors (FAPIs) and p-Cl-Phe-cyclo(d-Cys-Tyr-d-4-amino-Phe(carbamoyl)-Lys-Thr-Cys)d-Tyr-NH<sub>2</sub> (LM3) peptides for imaging of FAP somatostatin receptor 2 (SSTR2)–positive tumors. In this study, we designed synthesized a FAPI-LM3 heterobivalent molecule with <sup>68</sup>Ga evaluated its effectiveness in both tumor xenografts patients nasopharyngeal carcinoma (NPC). <b>Methods:</b> The...
The fibroblast activation protein (FAP), overexpressed on cancer-associated fibroblasts (CAFs), has become a valuable target for tumor diagnosis and therapy. However, most FAP-based radioligands show insufficient uptake retention. In this study, three novel albumin-binding FAP ligands (denoted as FSDD0I, FSDD1I, FSDD3I) were labeled with 68Ga 177Lu to overcome these limitations. Cell-based studies molecular docking assays performed identify the specificity protein-binding properties FAP....
Fibroblast activation protein (FAP), a fundamental component of the tumor stroma, is overexpressed in cancer-associated fibroblasts (CAFs). As promising theranostic probe, we evaluated whether FAP inhibitor (FAPI) dimer (DOTA-2P[FAPI]2) more effective than its monomeric analogs for FAP-targeted radionuclide therapy. [68Ga]Ga/[177Lu]Lu-DOTA-2P(FAPI)2 were assayed stability study, small-animal positron emission tomography (PET) and single-photon computed (SPECT), biodistribution, therapy to...
Due to the complex heterogeneity in different cancer types, heterodimeric strategy has been intensively practiced improve effectiveness of tumor diagnostics. In this study, we developed a series novel 18F-labeled biotin/FAPI-conjugated heterobivalent radioligands ([18F]AlF-NSFB, [18F]AlF-NSFBP2, and [18F]AlF-NSFBP4), synergistically targeting both fibroblast activation protein (FAP) biotin receptor (BR), enhance specific uptake retention. The vitro vivo biological properties these...
Recognizing the significance of SPECT in nuclear medicine and pivotal role fibroblast activation protein (FAP) cancer diagnosis therapy, this study focuses on development 99mTc-labeled dimeric HF2 with high tumor uptake image contrast. The was synthesized radiolabeled 99mTc one pot using various coligands (tricine, TPPTS, EDDA, TPPMS) to yield [99mTc]Tc-TPPTS-HF2, [99mTc]Tc-EDDA-HF2, [99mTc]Tc-TPPMS-HF2 dimers. imaging results indicated that [99mTc]Tc-TPPTS-HF2 exhibited higher...
Fibroblast activation protein (FAP) is a promising target for cancer theranostics, but most FAP-targeted radioprobes showed relatively insufficient tumor uptake and retention, which seriously hampered their further application. Inspired by the squirrel tail, this study developed novel molecule, FSND3, modified with three Asp-peptide adapters to enable both 68Ga ([68Ga]Ga-FSND3) 18F ([18F]AlF-FSND3) PET imaging. Compared [68Ga]Ga-FAPI-04, [68Ga]Ga-FAPI-42, [18F]AlF-FAPI-42, [18F]AlF-FSND3...
Abstract Background: This study developed 68Ga-NK224, a novel peptide-based radiotracer targeting human PD-L1, to evaluate the feasibility of 68Ga-NK224 PET/CT for assessing PD-L1 expression and tumor heterogeneity in prospective investigator-initiated trial. Methods: In preclinical studies, NK224 was labeled with 68Ga. Small-animal PET, biodistribution, blocking studies were performed using models varying levels assess ability specificity vivo. Serial PET assessed target occupancy following...
As a new modality of ligands, bicyclic peptides hold great promise in the discovery novel programmed death ligand 1 (PD-L1) targeted radiotracers, which have not yet been reported. In this study, first-in-class peptide-based radiotracers [18F]AlF-BCY509 and [18F]AlF-BCY10959 were developed evaluated for PET imaging tumor PD-L1 expression. The automatic radiosynthesis was achieved with robust radiochemical yields (55.1-90.2%) high molar activity (42.5-90.8 GBq/μmol). Cell-based assays...
Riboflavin transporter-3 (RFVT3) is a recently discovered and novel biomarker for the theranostics of nervous system diseases. RFVT3 significantly overexpressed in cerebral injury after ischemic stroke. Herein, we first reported an RFVT3-targeted tracer 131I-riboflavin (131I-RFLA) SPECT imaging stroke vivo. 131I-RFLA was radiosynthesized by iodogen-coating method. possessed radiochemical yield 69.2 ± 3.7% greater than 95% purity. The representative SPECT/CT images using demonstrated...
The stimulator of interferon genes (STING) is a pivotal protein in the production STING-dependent type I interferon, which has potential to enhance tumor rejection. visualization STING microenvironment valuable for STING-related treatments, but few imaging probes have been reported date. In this study, we developed novel 18F-labeled agent ([18F]F-CRI1) with an acridone core structure positron emission tomography (PET) CT26 tumors. probe was successfully prepared nanomolar binding affinity Kd...
The stimulator of interferon genes (STING) is pivotal in mediating STING-dependent type I production, which crucial for enhancing tumor rejection. Visualizing STING within the microenvironment valuable STING-related treatments, yet availability suitable imaging probes limited. In this study, we developed [18F]AlF-ABI, a novel 18F-labeled agent featuring an amidobenzimidazole core structure, positron emission tomography (PET) B16F10 and CT26 tumors. [18F]AlF-ABI was synthesized with...