Academic Journal

Gadolinium-Cyclic 1,4,7,10-Tetraazacyclododecane-1,4,7,10-Tetraacetic Acid-Click-Sulfonyl Fluoride for Probing Serine Protease Activity in Magnetic Resonance Imaging

التفاصيل البيبلوغرافية
العنوان: Gadolinium-Cyclic 1,4,7,10-Tetraazacyclododecane-1,4,7,10-Tetraacetic Acid-Click-Sulfonyl Fluoride for Probing Serine Protease Activity in Magnetic Resonance Imaging
المؤلفون: Phuong Tu Huynh, Huy Duc Vu, Junghwa Ryu, Hee Su Kim, Hoesu Jung, Sung Won Youn
المصدر: Molecules; Volume 28; Issue 8; Pages: 3538
بيانات النشر: Multidisciplinary Digital Publishing Institute
سنة النشر: 2023
المجموعة: MDPI Open Access Publishing
مصطلحات موضوعية: gadolinium contrast agent, elastase, serine protease, T1-weighted magnetic resonance imaging
جغرافية الموضوع: agris
الوصف: Serine protease is linked to a wide range of diseases, prompting the development of robust, selective, and sensitive protease assays and sensing methods. However, the clinical needs for serine protease activity imaging have not yet been met, and the efficient in vivo detection and imaging of serine protease remain challenging. Here, we report the development of the gadolinium-cyclic 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid-click-Sulfonyl Fluoride (Gd-DOTA-click-SF) MRI contrast agent targeting serine protease. The HR-FAB mass spectrum confirmed the successful formation of our designed chelate. The molar longitudinal relaxivity (r1) of the Gd-DOTA-click-SF probe (r1 = 6.82 mM−1 s−1) was significantly higher than that of Dotarem (r1 = 4.63 mM−1 s−1), in the range of 0.01–0.64 mM at 9.4 T. The in vitro cellular study and the transmetallation kinetics study showed that the safety and stability of this probe are comparable to those of conventional Dotarem. Ex vivo abdominal aortic aneurysm (AAA) MRI revealed that this probe has a contrast-agent-to-noise ratio (CNR) that is approximately 51 ± 23 times greater than that of Dotarem. This study of superior visualization of AAA suggests that it has the potential to detect elastase in vivo and supports the feasibility of probing serine protease activity in T1-weighted MRI.
نوع الوثيقة: text
وصف الملف: application/pdf
اللغة: English
Relation: https://dx.doi.org/10.3390/molecules28083538
DOI: 10.3390/molecules28083538
الاتاحة: https://doi.org/10.3390/molecules28083538
Rights: https://creativecommons.org/licenses/by/4.0/
رقم الانضمام: edsbas.8A5CD11D
قاعدة البيانات: BASE
الوصف
DOI:10.3390/molecules28083538