Cancer Institute A national cancer institute
designated cancer center

Matthew Bogyo

Publication Details

  • A Nonpeptidic Cathepsin S Activity-Based Probe for Noninvasive Optical Imaging of Tumor-Associated Macrophages CHEMISTRY & BIOLOGY Verdoes, M., Edgington, L. E., Scheeren, F. A., Leyva, M., Blum, G., Weiskopf, K., Bachmann, M. H., Ellman, J. A., Bogyo, M. 2012; 19 (5): 619-628

    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.

    View details for DOI 10.1016/j.chembiol.2012.03.012

    View details for Web of Science ID 000304794600013

    View details for PubMedID 22633413

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