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Pyroglutamate aminopeptidase (PGP) specifically cleaves the peptide bond of pyroglutamic acid linked to the N-terminal end of a polypeptide or protein. Previous studies showed that PGP was associated with several physiological processes and diseases especially those involving inflammation. Utilizing a 'caging' strategy, we designed and synthesized a bioluminescence probe (PBL) with a limit-of-detection of 3.7 * 10 mU/mL. In vivo imaging in a mouse model of inflammatory liver disease revealed that the probe has excellent sensitivity and selectivity and provides a powerful tool for studying the physiological and pathological processes involving PGP.
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http://dx.doi.org/10.1016/j.bmcl.2021.128049 | DOI Listing |
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.
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 PDFNucleic Acids Res
September 2025
Key Laboratory of Clinical Laboratory Diagnostics (Chinese Ministry of Education), College of Laboratory Medicine, Chongqing Medical University, Chongqing 400016, P. R. China.
Local pH variations play a pivotal role in numerous critical biological processes. However, achieving the tunability and selectivity of pH detection remains a challenge. Here, we present a DNA-based strategy that enables programmable and selective pH responses, which is termed shadow-strand hybridization-actuated displacement engineering (SHADE).
View Article and Find Full Text PDFTop Magn Reson Imaging
October 2025
BIOSPACE LAB, Nesles-la-Vallée, France.
Aims: Cardiac tumors are aggressive and asymptomatic in early stages, causing late diagnosis and locoregional metastasis. Currently, the standard of care uses gadolinium-based contrast agents for MRI, and the associated hypersensitivity reactions are a significant concern, such as gadolinium deposition disease. In addition, the proximity of cardiac lesions closer to vital structures complicates surgical interventions.
View Article and Find Full Text PDFMol Pharm
September 2025
Guangdong Provincial Engineering Research Center of Molecular Imaging, The Fifth Affiliated Hospital, Sun Yat-Sen University, Zhuhai, Guangdong 519000, China.
Rheumatoid arthritis (RA) is a chronic autoimmune disease characterized by joint inflammation. This study aimed to use the sphingosine 1-phosphate receptor 1 (S1PR1) targeted tracer [F]TZ4877 with PET/CT to assess synovial inflammation in a collagen-induced arthritis (CIA) mouse model. [F]TZ4877 and [F]FDG PET/CT imaging were performed on RA ( = 6) and control ( = 6) mice.
View Article and Find Full Text PDF