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Large-Scale Profiling of Kinase Degradation by Using Norbornene-Based Hydrophobic Tag (HyT) Strategy.

Mingxi Gu1,2, Fengfei Miao2, Lvyang Peng1

  • 1School of Pharmaceutical Sciences (Shenzhen), Shenzhen Campus of Sun Yat-Sen University, Shenzhen, China.

Angewandte Chemie (International Ed. in English)
|April 20, 2026
PubMed
Summary

Hydrophobic tags (HyTs) offer a new way to degrade proteins, unlike traditional methods. This study maps 169 human kinases degradable by HyTs, paving the way for novel kinase therapeutics.

Keywords:
chemoproteomicsdrug discoveryhydrophobic tagkinasetargeted protein degradation

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Area of Science:

  • Biochemistry
  • Molecular Biology
  • Drug Discovery

Background:

  • Hydrophobic tags (HyTs) are emerging bifunctional protein degraders.
  • HyTs mimic misfolded proteins for quality control-mediated degradation.
  • Their application across the human kinome is largely unexplored.

Purpose of the Study:

  • To explore the scope and generality of HyT-based targeted protein degradation (TPD) across the human kinome.
  • To develop general HyTs for large-scale kinase degradation studies.
  • To establish a framework for developing novel kinase therapeutics using HyTs.

Main Methods:

  • Development of two general HyTs using a pan-kinase scaffold.
  • Quantitative chemoproteomics for proteome-wide kinase degradation studies.
  • Design and optimization of norbornene-based HyT degraders (e.g., for ABL, AURKA).
  • Engineering of HyT-loaded, tumor microenvironment (TME)-responsive nanoparticles (NPs).

Main Results:

  • Identification of 169 HyT-degradable human kinases, mapping the degradable kinome landscape.
  • Successful design and optimization of potent HyT degraders against ABL and AURKA.
  • Elucidation of the mechanistic insights of novel HyT degraders.
  • Engineered NPs demonstrated improved tumor accumulation and therapeutic efficacy in vivo.

Conclusions:

  • This study provides the first comprehensive map of the degradable kinome using HyTs.
  • HyTs offer rapid target identification and a modular NP-based delivery platform for kinase therapeutics.
  • The developed HyT strategy and NP delivery system present a promising framework for future kinase drug development.