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On-Membrane Supramolecular Assemblies Serving as Bioorthogonal Gating for Melphalan.

Hanlin Xu1, Qingxin Yao1, Xiaoqian Hu1

  • 1State Key Laboratory of Chemical Resource Engineering, MOE Key Lab of Biomedical Materials of Natural Macromolecules, Beijing University of Chemical Technology, Beijing, 100029, China.

Angewandte Chemie (International Ed. in English)
|April 24, 2025
PubMed
Summary

This study introduces a cell-selective bioorthogonal prodrug strategy to improve covalent drug targeting. The novel design enhances selectivity for cancer cells, reducing toxicity to normal tissues and improving therapeutic outcomes.

Keywords:
Bioorthogonal prodrugsCancerCovalent drugsEnzyme instructed supramolecular assembliesMembrane transporters

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Area of Science:

  • Biochemistry
  • Medicinal Chemistry
  • Drug Delivery

Background:

  • Covalent drugs offer advantages in pharmacodynamics and targeting challenging proteins.
  • Achieving selectivity, reactivity, and potency balance is crucial for covalent drug safety and efficacy.

Purpose of the Study:

  • To develop a cell-selective bioorthogonal prodrug system to enhance covalent inhibitor selectivity.
  • To maintain reactivity and potency while minimizing off-target effects.

Main Methods:

  • Utilized enzyme-instructed supramolecular assemblies (EISA) on cancer cell membranes.
  • Employed a bioorthogonal prodrug (TCO-Mel) activated by tetrazine (Tz) localized by EISA.
  • Investigated disruption of LAT1-mediated transport and Melphalan influx.

Main Results:

  • The prodrug design reduced TCO-Mel permeability and cytotoxicity in normal cells.
  • Cell-selective EISA enabled targeted Melphalan release and influx into cancer cells.
  • Demonstrated potent tumor suppression and good biocompatibility in vivo.

Conclusions:

  • The bioorthogonal prodrug strategy successfully enhances selectivity for covalent drugs.
  • Regulating the cellular influx of active pharmaceutical ingredients (APIs) is a viable approach for covalent drug design.
  • This method offers a promising platform for developing safer and more effective covalent therapies.