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Kinase-mediated trapping of bi-functional conjugates of paclitaxel or vinblastine with thymidine in cancer cells
Authors:Aspland Simon E  Ballatore Carlo  Castillo Rosario  Desharnais Joel  Eustaquio Trisha  Goelet Philip  Guo Zijian  Li Qing  Nelson David  Sun Chengzao  Castellino Angelo J  Newman Michael J
Affiliation:Acidophil LLC, 2330 W. Joppa Road, Suite 330, Lutherville, MD 21093, USA. saspland@acidophil.com
Abstract:In the present work, we explore the possibility of introducing selectivity to existing chemotherapeutics via the design of non-pro-drug, bi-functional molecules comprising a microtubule-binding agent and a substrate for a disease-associated kinase. The design, synthesis, and in vitro biological evaluation of paclitaxel-thymidine and vinblastine-thymidine bi-functional conjugates are reported here. This work provides the first account of 'kinase-mediated trapping' of cancer therapeutics.
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