Cheng, Ke Lee, Jun-Seok Hao, Piliang Yao, Shao Q. Ding, Ke Li, Zhengqiu 2024-01-20T00:03:06Z 2024-01-20T00:03:06Z 2021-09-03 2017-11-20 1433-7851 https://pubs.kist.re.kr/handle/201004/122051 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. English John Wiley & Sons Ltd. PHOTO-CROSS-LINKERS SMALL-MOLECULE PROBES PHOTOAFFINITY LINKERS TARGET IDENTIFICATION KINASE INHIBITORS HUMAN-CELLS ANNEXIN A2 BINDING DISCOVERY PROTEINS Tetrazole-Based Probes for Integrated Phenotypic Screening, Affinity-Based Proteome Profiling, and Sensitive Detection of a Cancer Biomarker Article 10.1002/anie.201709584 1 Angewandte Chemie International Edition, v.56, no.47, pp.15044 - 15048 Angewandte Chemie International Edition 56 47 15044 15048 scie scopus 000445812900046 2-s2.0-85033785007 Chemistry, Multidisciplinary Chemistry Article PHOTO-CROSS-LINKERS SMALL-MOLECULE PROBES PHOTOAFFINITY LINKERS TARGET IDENTIFICATION KINASE INHIBITORS HUMAN-CELLS ANNEXIN A2 BINDING DISCOVERY PROTEINS affinity-based probes cancer biomarkers phenotypic screening target identification tetrazole