Novel Matrix Metalloproteinase 12 Selective Radiotracers for Vascular Molecular Imaging.

ABSTRACT: Matrix metalloproteinase-12 (MMP-12) is highly upregulated in several inflammatory diseases, including abdominal aortic aneurysm (AAA). Here we report four novel ^99mTc-labeled radiotracers derived from a highly selective competitive MMP-12 inhibitor. These tracers in their ^99gTc version were assessed in vitro on a set of human metalloproteases and displayed high affinity and selectivity toward MMP-12. Their radiolabeling with ^99mTc was shown to be efficient and stable in both buffer and mouse blood. The tracers showed major differences in their biodistribution and blood clearance. On the basis of its in vivo performance, [^99mTc]-1 was selected for evaluation in murine AAA, where MMP-12 gene expression is upregulated. Autoradiography of aor

SUBMITTER: Toczek J 

PROVIDER: S-EPMC7054845 | biostudies-literature | 2019 Nov

REPOSITORIES: biostudies-literature