Development of matrix metalloproteinase-targeted probes for lung inflammation detection with positron emission tomography.

ABSTRACT: As matrix metalloproteinases (MMPs), especially MMP-9 and MMP-12 are involved in the pathological processes associated with chronic obstructive pulmonary disease (COPD), we developed a novel radiofluorinated probe, ¹⁸F-IPFP, for MMPs-targeted positron emission tomography (PET). ¹⁸F-IPFP was designed by iodination of MMP inhibitor to enhance the affinity, and labelled with a compact prosthetic agent, 4-nitrophenyl 2-¹⁸F-fluoropropionate (¹⁸F-NFP). As a result, IPFP demonstrated the highest affinity toward MMP-12 (IC₅₀ = 1.5 nM) among existing PET probes. A COPD model was employed by exposing mice to cigarette smoke and the expression levels of MMP-9 and MMP-12 were significantly increased in the lungs. Radioactivity accumulation in the

SUBMITTER: Kondo N 

PROVIDER: S-EPMC5778071 | biostudies-literature | 2018 Jan

REPOSITORIES: biostudies-literature