Jakub Toczek, Kiran Gona, Yongjian Liu, Azmi Ahmad, Mean Ghim, Devi Ojha, Gunjan Kukreja, Mani Salarian, Hannah Luehmann, Gyu Seong Heo, Raul J Guzman, Cassius I Ochoa Chaar, George Tellides, Abdulrahman H M Hassab, Yunpeng Ye, Kooresh I Shoghi, Mohamed A Zayed, Robert J Gropler, Mehran M Sadeghi
BACKGROUND: Matrix metalloproteinases (MMPs) play a key role in the pathogenesis of abdominal aortic aneurysm (AAA). Imaging aortic MMP activity, especially using positron emission tomography to access high sensitivity, quantitative data, could potentially improve AAA risk stratification. Here, we describe the design, synthesis, characterization, and evaluation in murine AAA and human aortic tissue of a first-in-class MMP-targeted positron emission tomography radioligand, 64 Cu-RYM2. METHODS: The broad spectrum MMP inhibitor, RYM2 was synthetized, and its potency as an MMP inhibitor was evaluated by a competitive inhibition assay...
January 2023: Circulation. Cardiovascular Imaging