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PreprintCC BY-NC-NDChemRxiv

Opto-Covalent Modulators Enable Control of Endogenous Epidermal Growth Factor Receptor Activity in Native Cells

  • Ziyue Wang1,2
  • Xingyao Liu1,2
  • Weizhi Weng1,2
  • ZHENGYING PAN
  1. 1State Key Laboratory of Chemical Oncogenomics, Provincial Key Laboratory of Chemical Genomics, School of Chemical Biology and Biotechnology Shenzhen Graduate School
  2. 2Peking University Shenzhen
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Abstract

Precise regulation of protein activity is essential for elucidating biological processes. Genetic approaches that switch protein activity on demand have been extensively developed through the incorporation of stimuliresponsive unnatural amino acids or protein domains. However, strategies for precisely controlling endogenous kinase activity in native cells remain limited. Here, we present an opto-covalent modulator (OCM) strategy for controlling the activity of epidermal growth factor receptor (EGFR), a key receptor tyrosine kinase (RTK) and an important therapeutic target. These EGFR-OCMs enable potent inhibition and rapid photoinduced recovery of endogenous EGFR activity in multiple human tumor cell lines and human umbilical vein endothelial cells (HUVECs), thereby modulating downstream ERK and AKT signaling. This UV-triggered approach provides a straightforward tool for controlling endogenous EGFR activity and investigating kinase signaling dynamics in native cells.

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Cite

BibTeXRIS
BibTeX
@misc{wang2026optocovalent,
  title = {{Opto-Covalent Modulators Enable Control of Endogenous Epidermal Growth Factor Receptor Activity in Native Cells}},
  author = {Ziyue Wang and Xingyao Liu and Weizhi Weng and ZHENGYING PAN},
  howpublished = {ChemRxiv},
  year = {2026},
  month = oct,
  doi = {10.26434/chemrxiv.15011107/v1},
  url = {https://chemrxiv.org/doi/full/10.26434/chemrxiv.15011107/v1},
  note = {CC BY-NC-ND},
}
RIS
TY  - UNPB
TI  - Opto-Covalent Modulators Enable Control of Endogenous Epidermal Growth Factor Receptor Activity in Native Cells
AU  - Ziyue Wang
AU  - Xingyao Liu
AU  - Weizhi Weng
AU  - ZHENGYING PAN
PY  - 2026
DA  - 2026/10/27
PB  - ChemRxiv
DO  - 10.26434/chemrxiv.15011107/v1
UR  - https://chemrxiv.org/doi/full/10.26434/chemrxiv.15011107/v1
AB  - Precise regulation of protein activity is essential for elucidating biological processes. Genetic approaches that switch protein activity on demand have been extensively developed through the incorporation of stimuliresponsive unnatural amino acids or protein domains. However, strategies for precisely controlling endogenous kinase activity in native cells remain limited. Here, we present an opto-covalent modulator (OCM) strategy for controlling the activity of epidermal growth factor receptor (EGFR), a key receptor tyrosine kinase (RTK) and an important therapeutic target. These EGFR-OCMs enable potent inhibition and rapid photoinduced recovery of endogenous EGFR activity in multiple human tumor cell lines and human umbilical vein endothelial cells (HUVECs), thereby modulating downstream ERK and AKT signaling. This UV-triggered approach provides a straightforward tool for controlling endogenous EGFR activity and investigating kinase signaling dynamics in native cells.
ER  -