Publication: Non-invasive in vivo imaging of tumour-associated cathepsin B by a highly selective inhibitory DARPin
Non-invasive in vivo imaging of tumour-associated cathepsin B by a highly selective inhibitory DARPin
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Kramer, L., Renko, M., Završnik, J., Turk, D., Seeger, M. A., Vasiljeva, O., Grütter, M. G., Turk, V., & Turk, B. (2017). Non-invasive in vivo imaging of tumour-associated cathepsin B by a highly selective inhibitory DARPin. Theranostics, 7(11), 2806–2821. https://doi.org/10.7150/thno.19081
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Cysteine cathepsins often contribute to cancer progression due to their overexpression in the tumour microenvironment and therefore present attractive targets for non-invasive diagnostic imaging. However, the development of highly selective and versatile small molecule probes for cathepsins has been challenging. Here, we targeted tumour-associated cathepsin B using designed ankyrin repeat proteins (DARPins). The selective DARPin 8h6 inhibited cathepsin B with picomolar affinity (Ki = 35 pM) by binding to a site with low structural con
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Kramer, L., Renko, M., Završnik, J., Turk, D., Seeger, M. A., Vasiljeva, O., Grütter, M. G., Turk, V., & Turk, B. (2017). Non-invasive in vivo imaging of tumour-associated cathepsin B by a highly selective inhibitory DARPin. Theranostics, 7(11), 2806–2821. https://doi.org/10.7150/thno.19081