Journal
ACS MEDICINAL CHEMISTRY LETTERS
Volume 11, Issue 4, Pages 535-540Publisher
AMER CHEMICAL SOC
DOI: 10.1021/acsmedchemlett.9b00658
Keywords
DDR1; bioimaging; chemoproteomics; target identification; photoaffinity labeling
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Funding
- National Key R&D Program of China [2019YFC1711000]
- National Natural Science Foundation of China [21877050]
- Science and Technology Program o f Guangdong Province [2 017A05 0 50 6 0 28, 2019B151502025]
- Science and Technology Program of Guangzhou [201704030060, 201805010007]
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Target identification of small molecules is a great challenge but an essential step in drug discovery. Here, a quantitative proteomics approach has been used to characterize the cellular targets of DR, a DDR1 inhibitor. By taking advantage of competitive affinity-based protein profiling coupled with bioimaging, Cathepsin D (CTSD) was found to be the principle off-target of DR in human cancer cells. Further findings suggest the potential of DR as a novel CTSD inhibitor for breast cancer treatment. In addition, a trans-cyclooctene (TCO) containing probe was developed to track the binding between DR and its target proteins in living systems and could be a useful tool for DDR1 detection.
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