Quantitative Proteomics Reveals Cellular Off-Targets of a DDR1 Inhibitor.
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ABSTRACT:
SUBMITTER: Xu J
PROVIDER: S-EPMC7153277 | biostudies-literature | 2020 Apr
REPOSITORIES: biostudies-literature
Publications
Quantitative Proteomics Reveals Cellular Off-Targets of a DDR1 Inhibitor.
Xu Jiaqian J Zhang Zhang Z Lin Ligen L Sun Hongyan H White Lorenzo V LV Ding Ke K Li Zhengqiu Z
ACS medicinal chemistry letters 20200205 4
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 ...[more]
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