ArticleEJNMMI radiopharmacy and chemistry2026
Development and preclinical evaluation of selective vinyl sulfone-based probes for PET imaging of tumor-associated cathepsins.
Article in EJNMMI radiopharmacy and chemistry, 2026. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Not yet cited in PubMed.
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Abstract
backgroundCysteine cathepsin L (CatL) is emerging as a key biomarker of cancer progression, making it an attractive candidate for non-invasive molecular imaging. To monitor enzymatic activity directly, rather than merely protein expression, activity-based probes (ABPs) enable selective targeting of enzymes through covalent binding at their active sites. Despite vinyl sulfones are well-established irreversible inhibitors of cathepsins, their application as positron emission tomography (PET) ABPs remains unexplored. In this study we describe the design, synthesis, and evaluation of a novel class of
resultsA series of ABPs were synthesized based on the established vinyl sulfone scaffold K11777 (K777). Structure-activity relationship (SAR) analysis revealed that retaining a homophenylalanine (hPhe) residue at the P1 position resulted in greater CatL potency compared to its corresponding leucine (Leu) analogue. Evaluation of different linkers at the P3 position further revealed that polyethylene glycol (PEG) linkers preserved high CatL selectivity, whereas a piperazine linker increased off-target binding to cathepsin B (CatB). Based on these findings, two representative radiotracers were selected for further biological evaluation: the PEG2-linked [
conclusionsA novel class of
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