2. Academic Validation
  3. A Fluorescent Probe Targeting EGFR for the Stratification of Prostate Cancer Cells

A Fluorescent Probe Targeting EGFR for the Stratification of Prostate Cancer Cells

  • J Mol Biol. 2025 Sep 1;437(17):169261. doi: 10.1016/j.jmb.2025.169261.
Xingxing Wang 1,  Peng Liu 1,  Linli Li 1,  Yan Du 1,  Xiaohong Qin 2,  Zhiqun Shang 3,  Li-Zhi Mi 4
Affiliations

Affiliations

  • 1 School of Life Sciences, Faculty of Medicine, Tianjin University, Tianjin 300072, PR China.
  • 2 School of Life Sciences, Faculty of Medicine, Tianjin University, Tianjin 300072, PR China; State Key Laboratory of Synthetic Biology, Tianjin University, Tianjin 300072, PR China. Electronic address: qinxiaohong@tju.edu.cn.
  • 3 Tianjin Institute of Urology, The Second Hospital of Tianjin Medical University, Tianjin 300211, PR China. Electronic address: zhiqun_shang@tmu.edu.cn.
  • 4 School of Life Sciences, Faculty of Medicine, Tianjin University, Tianjin 300072, PR China; State Key Laboratory of Synthetic Biology, Tianjin University, Tianjin 300072, PR China. Electronic address: lizhi.mi@tju.edu.cn.
PMID: 40466906 DOI: 10.1016/j.jmb.2025.169261
Abstract

Effective stratification of Cancer patients is critical yet challenging for evaluating therapeutic strategies. In this study, we designed a competitive, modular fluorescent probe targeting the oncogenic epidermal growth factor receptor (EGFR) kinase. This probe specifically inhibits EGFR kinase activity in a dose-dependent manner, selectively labels EGFR-overexpressing cells in flow cytometry, and sensitively binds to EGFR oncogenic mutants. Utilizing probe-based cytometry to subtype urine samples from prostate Cancer patients, we discovered that samples with overexpressed wild-type EGFR did not respond sensitively to the probe, aligning with findings from an early multi-center clinical study. Notably, one sample with low EGFR expression exhibited the highest sensitivity to the probe, leading to the identification of three non-characterized mutations, including the activating mutation V745M, on the EGFR kinase. This case involved a tumor that had progressed to the castration-resistant metastatic stage.

Keywords

cancer stratification; receptor tyrosine kinase; structure-based probe design.

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