Journal Highlight: Tetrazole-based probes for integrated phenotypic screening, affinity-based proteome profiling, and sensitive detection of a cancer biomarker

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  • Published: Nov 27, 2017
  • Author: separationsNOW
  • Channels: Proteomics & Genomics
thumbnail image: Journal Highlight: Tetrazole-based probes for integrated phenotypic screening, affinity-based proteome profiling, and sensitive detection of a cancer biomarker

Phenotypic screening of a fully functionalized small-molecule library has been combined with competitive affinity-based proteome profiling to map and functionally characterize the targets of screening hits in drug discovery.

Tetrazole-based probes for integrated phenotypic screening, affinity-based proteome profiling, and sensitive detection of a cancer biomarker

Angewandte Chemie International Edition, 2017, 56, 15044-15048
Ke Cheng, Jun-Seok Lee, Piliang Hao, Shao Q. Yao, Ke Ding and Zhengqiu Li

Abstract: 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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