Cell‐ and Tissue‐Based Proteome Profiling and Bioimaging with Probes Derived from a Potent AXL Kinase Inhibitor |
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| Authors: | Binbin Zheng Haijun Guo Dr. Nan Ma Yun Ni Jiaqian Xu Prof. Lin Li Prof. Piliang Hao Prof. Ke Ding Prof. Zhengqiu Li |
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| Affiliation: | 1. School of Pharmacy, Jinan University, Guangzhou City Key Laboratory of Precision Chemical Drug Development, International Cooperative Laboratory of Traditional Chinese Medicine Modernization and Innovative Drug Development, Ministry of Education (MOE) of People's Republic of China, Guangzhou, China;2. Institute of Advanced Materials (IAM), Nanjing Tech University, China;3. School of Life Science and Technology, ShanghaiTech University, China |
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| Abstract: | AXL has been defined as a novel target for cancer therapeutics. However, only a few potent and selective inhibitors targeting AXL are available to date. Recently, our group has developed a lead compound, 9im, capable of displaying potent and specific inhibition of AXL. To further identify the cellular on/off targets, in this study, competitive affinity‐based proteome profiling was carried out, leading to the discovery of several unknown cellular targets such as BCAP31, LPCAT3, POR, TM9SF3, SCCPDH and CANX. In addition, trans‐cyclooctene (TCO) and acedan‐containing probes were developed to image the binding between 9im and its target proteins inside live cells and tumor tissues. These probes would be useful tools in the detection of AXL in various biosystems. |
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| Keywords: | AXL imaging probes proteomics target identification |
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