دورية أكاديمية
The Development of a Smart Magnetic Resonance Imaging and Chemical Exchange Saturation Transfer Contrast Agent for the Imaging of Sulfatase Activity
| العنوان: | The Development of a Smart Magnetic Resonance Imaging and Chemical Exchange Saturation Transfer Contrast Agent for the Imaging of Sulfatase Activity |
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| المؤلفون: | Ilse M. Welleman, Friederike Reeβing, Hendrikus H. Boersma, Rudi A. J. O. Dierckx, Ben L. Feringa, Wiktor Szymanski |
| المصدر: | Pharmaceuticals, Vol 16, Iss 10, p 1439 (2023) |
| بيانات النشر: | MDPI AG, 2023. |
| سنة النشر: | 2023 |
| المجموعة: | LCC:Medicine LCC:Pharmacy and materia medica |
| مصطلحات موضوعية: | molecular imaging, sulfatase, MRI, CEST, responsive imaging agents, Medicine, Pharmacy and materia medica, RS1-441 |
| الوصف: | The molecular imaging of biomarkers plays an increasing role in medical diagnostics. In particular, the imaging of enzyme activity is a promising approach, as it enables the use of its inherent catalytic activity for the amplification of an imaging signal. The increased activity of a sulfatase enzyme has been observed in several types of cancers. We describe the development and in vitro evaluation of molecular imaging agents that allow for the detection of sulfatase activity using the whole-body, non-invasive MRI and CEST imaging methods. This approach relies on a responsive ligand that features a sulfate ester moiety, which upon sulfatase-catalyzed hydrolysis undergoes an elimination process that changes the functional group, coordinating with the metal ion. When Gd3+ is used as the metal, the complex can be used for MRI, showing a 25% decrease at 0.23T and a 42% decrease at 4.7T in magnetic relaxivity after enzymatic conversion, thus providing a “switch-off” contrast agent. Conversely, the use of Yb3+ as the metal leads to a “switch-on” effect in the CEST imaging of sulfatase activity. Altogether, the results presented here provide a molecular basis and a proof-of-principle for the magnetic imaging of the activity of a key cancer biomarker. |
| نوع الوثيقة: | article |
| وصف الملف: | electronic resource |
| اللغة: | English |
| تدمد: | 1424-8247 80846890 |
| Relation: | https://www.mdpi.com/1424-8247/16/10/1439; https://doaj.org/toc/1424-8247 |
| DOI: | 10.3390/ph16101439 |
| URL الوصول: | https://doaj.org/article/80846890f5a74183b90930c62f822cc9 |
| رقم الأكسشن: | edsdoj.80846890f5a74183b90930c62f822cc9 |
| قاعدة البيانات: | Directory of Open Access Journals |
Full Text Finder | تدمد: | 14248247 80846890 |
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| DOI: | 10.3390/ph16101439 |