期刊
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION
卷 56, 期 47, 页码 15044-15048出版社
WILEY-V C H VERLAG GMBH
DOI: 10.1002/anie.201709584
关键词
affinity-based probes; cancer biomarkers; phenotypic screening; target identification; tetrazole
资金
- National Natural Science Foundation of China [21602079]
- Science and Technology Program of Guangdong province [2017A050506028]
- Science and Technology Program of Guangzhou [201704030060]
- KIST [2E26632/2E26110, CAP- 16-02-KIST]
- Bio & Medical Technology Development Program of the National Research Foundation from Ministry of Science, Korea [NRF- 2016M3A9B6902060, NRF-2017M3A9D8029942]
- National Research Foundation of Korea [2016M3A9B6902060, 2017M3A9D8029942] Funding Source: Korea Institute of Science & Technology Information (KISTI), National Science & Technology Information Service (NTIS)
Target-identification phenotypic screening has been a powerful approach in drug discovery; however, it is hindered by difficulties in identifying the underlying cellular targets. To address this challenge, we have combined phenotypic screening of a fully functionalized small-molecule library with competitive affinity-based proteome profiling to map and functionally characterize the targets of screening hits. Using this approach, we identified ANXA2, PDIA3/4, FLAD1, and NOS2 as primary cellular targets of two bioactive molecules that inhibit cancer cell proliferation. We further demonstrated that a panel of probes can label and/or image annexin A2 (a cancer biomarker) from different cancer cell lines, thus providing opportunities for potential cancer diagnosis and therapy.
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