2023
DOI: 10.1021/acs.molpharmaceut.3c00321
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Automated Synthesis and Preclinical Evaluation of Optimized Integrin α6-Targeted Positron Emission Tomography Imaging of Pancreatic Cancer

Abstract: Integrin α6 has been considered a promising biomarker, is overexpressed in many tumors, and plays a vital role in tumor formation, recurrence, and metastasis. In this study, we identified a novel high-affinity integrin α6-targeted peptide named RD2 (Arg-Trp-Tyr-Asp-PEG4)2-Lys-Lys and developed a 18F-radiolabeled peptide tracer ([18F]-AlF-NOTA-RD2) and evaluated its potential application in positron emission tomography (PET) imaging of pancreatic cancer. [18F]-AlF-NOTA-RD2 was produced using GMP (Good Manufactu… Show more

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Cited by 5 publications
(3 citation statements)
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“…We then further verified the systemic immunostimulatory effect of the MLSV system in vivo . To this end, mice were injected with DMP, tumor cell lysate, or the MLSV system, and related expression in LNs and spleens was monitored for 72 h. As shown in Figure D, the percentage of CD11c + cells in LNs in the MLSV group was 66.9 ± 2.9% (peak value at 72 h), which was higher than those of the tumor cell lysate group (56.5 ± 2.7%, P < 0.001, peak value at 72 h), the DMP group (43.8 ± 3.6%, P < 0.001, peak value at 72 h), and the NS group (8.4 ± 1.4%, P < 0.001, peak value at 72 h). The percentage of CD11c + CD80 + cells in the MLSV group was 76.4 ± 1.5% (peak value at 72 h), which exceeded those of the tumor cell lysate group (47.4 ± 2.1%, P < 0.001, peak value at 72 h), the DMP group (25.2 ± 1.1%, P < 0.001, peak value at 72 h), and the NS group (16.9 ± 1.8%, P < 0.001, peak value at 72 h) (Figure D).…”
Section: Resultsmentioning
confidence: 98%
“…We then further verified the systemic immunostimulatory effect of the MLSV system in vivo . To this end, mice were injected with DMP, tumor cell lysate, or the MLSV system, and related expression in LNs and spleens was monitored for 72 h. As shown in Figure D, the percentage of CD11c + cells in LNs in the MLSV group was 66.9 ± 2.9% (peak value at 72 h), which was higher than those of the tumor cell lysate group (56.5 ± 2.7%, P < 0.001, peak value at 72 h), the DMP group (43.8 ± 3.6%, P < 0.001, peak value at 72 h), and the NS group (8.4 ± 1.4%, P < 0.001, peak value at 72 h). The percentage of CD11c + CD80 + cells in the MLSV group was 76.4 ± 1.5% (peak value at 72 h), which exceeded those of the tumor cell lysate group (47.4 ± 2.1%, P < 0.001, peak value at 72 h), the DMP group (25.2 ± 1.1%, P < 0.001, peak value at 72 h), and the NS group (16.9 ± 1.8%, P < 0.001, peak value at 72 h) (Figure D).…”
Section: Resultsmentioning
confidence: 98%
“…Noninvasive molecular imaging techniques, such as fluorescence (FL), , PET, MRI, and photoacoustic imaging (PAI) can monitor cathepsin B activity in vivo . Among them, PET imaging has ideal intrinsic properties to image the activity of the enzyme because of its high sensitivity and deep tissue penetration, providing practical information to differentiate changes in cancer . Tracers designed for PET imaging of cathepsin B activity are still rarely reported, and lots of work is still required to improve the tumor targeting and imaging quality.…”
Section: Introductionmentioning
confidence: 99%
“…Among them, PET imaging has ideal intrinsic properties to image the activity of the enzyme because of its high sensitivity and deep tissue penetration, providing practical information to differentiate changes in cancer. 31 Tracers designed for PET imaging of cathepsin B activity are still rarely reported, and lots of work is still required to improve the tumor targeting and imaging quality. In 2022, our group designed a novel stimulus-responsive SF scaffold for imaging enzyme activity and biologically related substances in vivo and in vitro.…”
Section: ■ Introductionmentioning
confidence: 99%