A nonpeptidic cathepsin S activity-based probe for noninvasive optical imaging of tumor-associated macrophages |
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Authors: | Verdoes Martijn Edgington Laura E Scheeren Ferenc A Leyva Melissa Blum Galia Weiskopf Kipp Bachmann Michael H Ellman Jonathan A Bogyo Matthew |
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Affiliation: | Department of Pathology, Stanford University School of Medicine, Stanford, CA 94305, USA. |
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Abstract: | Macrophage infiltration into tumors has been correlated with poor clinical outcome in multiple cancer types. Therefore, tools to image tumor-associated macrophages could be valuable for diagnosis and prognosis of cancer. Herein, we describe the synthesis and characterization of a cathepsin S-directed, quenched activity-based probe (qABP), BMV083. This probe makes use of an optimized nonpeptidic scaffold leading to enhanced in vivo properties relative to previously reported peptide-based probes. In a syngeneic breast cancer model, BMV083 provides high tumor-specific fluorescence that can be visualized using noninvasive optical imaging methods. Furthermore, analysis of probe-labeled cells demonstrates that the probe primarily targets macrophages with an M2 phenotype. Thus, BMV083 is a potential valuable in vivo reporter for tumor-associated macrophages that could greatly facilitate the future studies of macrophage function in the process of tumorigenesis. |
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