475160-83-9Relevant articles and documents
Near-Infrared Fluorescent Molecular Probe for Sensitive Imaging of Keloid
Miao, Qingqing,Yeo, David C.,Wiraja, Christian,Zhang, Jianjian,Ning, Xiaoyu,Xu, Chenjie,Pu, Kanyi
, p. 1256 - 1260 (2018)
Early detection of skin diseases is imperative for their effective treatment. However, fluorescence molecular probes that allow this are rare. The first activatable near-infrared (NIR) fluorescent molecular probe is reported for sensitive imaging of keloi
DIRECTED CONJUGATION TECHNOLOGIES
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Paragraph 0989; 0990, (2021/05/29)
Among other things, the present disclosure provides technologies for site-directed conjugation of various moieties of interest to target agents. In some embodiments, the present disclosure utilizes target binding moieties to provide high conjugation efficiency and selectivity. In some embodiments, provided technologies are useful for preparing antibody conjugates.
Synthesis and biological characterization of protease-activated prodrugs of doxazolidine
Barthel, Benjamin L.,Rudnicki, Daniel L.,Kirby, Thomas Price,Colvin, Sean M.,Burkhart, David J.,Koch, Tad H.
experimental part, p. 6595 - 6607 (2012/10/07)
Doxazolidine (doxaz) is a new anthracycline anticancer agent. While structurally similar to doxorubicin (dox), doxaz acts via a distinct mechanism to selectively enhance anticancer activity over cardiotoxicity, the most significant clinical impediment to successful anthracycline treatment. Here, we describe the synthesis and characterization of a prodrug platform designed for doxaz release mediated by secreted proteolytic activity, a common association with invasiveness and poor prognosis in cancer patients. GaFK-Doxaz is hydrolyzable by the proteases plasmin and cathepsin B, both strongly linked with cancer progression, as well as trypsin. We demonstrate that activation of GaFK-Doxaz releases highly potent doxaz that powerfully inhibits the growth of a wide variety of cancer cells (average IC50 of 8 nM). GaFK-Doxaz is stable in human plasma and is poorly membrane permeable, thereby limiting activation to locally secreted proteolytic activity and reducing the likelihood of severe side effects.