Category Ranking
98%
Total Visits
921
Avg Visit Duration
2 minutes
Citations
20
Article Abstract
Expression of the cellular transmembrane receptor αvβ6 integrin is mostly restricted to malignant epithelial cells in a wide variety of carcinomas, including pancreatic and others derived from epithelial tissues. Thus, this protein is considered an attractive target for tumour imaging and therapy. Two different Ga hexadentate tris (3,4-hydroxypyridinone) (THP) chelators were produced in this study and coupled to the αvβ6 integrin-selective peptide (FRGDLAFp(NMe)K) NHS chemistry. Radiolabelling experiments confirmed a high radiochemical yield of the two PET probes. In addition, cellular binding studies showed high binding affinities in the nanomolar range. The two integrin αvβ6-peptide-THP synthesized and radiolabeled in this study will facilitate monitoring of transmembrane receptor αvβ6 integrin by using the advantage of THP chemistry for rapid, efficient and stable gallium chelation.
Download full-text PDF |
Source |
|---|---|
| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC9425781 | PMC |
| http://dx.doi.org/10.1039/d2dt00980c | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
F-FDG Versus Tissue Factor-Targeted PET/CT in Longitudinal Evaluation of the Formation of DEN-Induced Rat Hepatocellular Carcinoma.
Mol Pharm
September 2025
Department of Nuclear Medicine, Tongji Hospital, Tongji Medical College, Huazhong University of Science and Technology, Wuhan 430030, China.
Tissue factor (TF) has emerged as a promising target for the diagnosis and treatment of hepatocellular carcinoma (HCC). However, there is limited data available on TF-related PET imaging for longitudinal monitoring of the pathophysiological changes during HCC formation. Herein, we aimed to explore the TF-expression feature and compare a novel TF-targeted PET probe with F-FDG through longitudinal imaging in diethylnitrosamine (DEN)-induced rat HCC.
View Article and Find Full Text PDFSynthesis, preclinical evaluation and clinical application of a novel heterodimeric tracer Ga-pentixafor-c(RGDfK) for PET-CT imaging.
Eur J Nucl Med Mol Imaging
September 2025
Department of PET-CT/MRI, NHC Key Laboratory of Molecular Probe and Targeted Theranostics, Harbin Medical University Cancer Hospital, Harbin, 150081, Heilongjiang, China.
Objective: CXCR4 and integrin αβ play important roles in tumor biology and are highly expressed in multiple types of tumors. This study aimed to synthesize, preclinically evaluate, and clinically validate a novel dual-targeted PET imaging probe Ga-pentixafor-c(RGDfK) for its potential in imaging tumors.
Methods: The effects of Ga-pentixafor-c(RGDfK) on cell viability, targeting specificity, and affinity were assessed in the U87MG cells.
Synergistic Methylene Blue-Driven FAPI Uptake Mechanism Advancing the Detection of Myocardial Fibrosis in Hypertensive Heart Disease.
Mol Pharm
September 2025
Center for Orthopedic Surgery, The Third Affiliated Hospital of Southern Medical University, Guangzhou 510630, China.
Myocardial fibrosis, a key pathological feature of hypertensive heart disease (HHD), remains diagnostically challenging due to limited clinical tools. In this study, a FAPI-targeted uptake mechanism previously reported by our group, originally developed for tumor imaging, is extended to the detection of myocardial fibrosis in HHD using [F]F-NOTA-FAPI-MB. The diagnostic performance of this tracer is compared with those of [F]F-FDG, [F]F-FAPI-42, and [F]F-NOTA-FAP2286, and its potential for fluorescence imaging is also evaluated.
View Article and Find Full Text PDFCu/Cu redox-cycling-driven dual-mode sensor for simultaneous monitoring of acetylcholinesterase activity and pesticide exposure.
Front Pharmacol
August 2025
Shenzhen Institute for drug Control, Shenzhen, China.
Introduction: The procedural complexity and time-consuming of conventional pesticide residue detection methods in traditional Chinese medicines (TCMs) significantly impeded their application in modern systems. To address this, this study presented an innovative dual-mode sensor driven by Cu/Cu redox-cycling, which achieved efficient signal transduction from enzyme inhibition to optical response for rapid acetylcholinesterase (AChE) activity and organophosphorus pesticide (OP) residue detection.
Methods: The AB-Cu NPs sensor, a dynamic redox-responsive system, was constructed via coordination-driven assembly of Azo-Bodipy 685 (AB 685) and Cu.
10P3Me: A GPC3-Targeted Peptide PET Probe for Subcutaneous and Orthotopic HCC Imaging.
J Med Chem
September 2025
Key Laboratory of Preclinical Study for New Drugs of Gansu Province, School of Basic Medical Sciences & Research Unit of Peptide Science, Chinese Academy of Medical Sciences, 2019RU066, Lanzhou University, Lanzhou, Gansu 730000, P. R. China.
Hepatocellular carcinoma (HCC) remains a growing global health threat, necessitating the development of precise molecular probes for its prevention, early diagnosis, and treatment. Glypican-3 (GPC3) is highly expressed in various HCC subtypes and exhibits minimal expression in normal liver tissue, making it a promising biomarker for early-stage HCC diagnosis. Herein, we report a novel cyclic peptide molecular probe, 10P3Me, exhibiting high binding affinity for GPC3, with a of 93.
View Article and Find Full Text PDF