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Updated: Jan 14, 2026

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Emergence of a Cell-Guided Multivalent Ligand of Enzymes on Cancer Cells Triggered by Click Reaction between Hetero

Rentaro Sakamoto1, Yuki Koba1, Masahiko Nakamoto1,2

  • 1Division of Applied Chemistry, Graduate School of Engineering, The University of Osaka, Suita, Osaka 565-0871, Japan.

ACS Applied Materials & Interfaces
|October 21, 2025
PubMed

Insights

Researchers developed novel stimuli-responsive nanomaterials that form multivalent ligands for cancer-associated enzymes like carbonic anhydrase IX (CAIX). These ligands selectively target and inhibit cancer cell proliferation, offering a promising approach to overcome tumor heterogeneity.

Area of Science:

  • Biomaterials Science
  • Nanotechnology
  • Cancer Biology

Background:

  • Stimuli-responsive nanomaterials with multivalent ligands are crucial for cancer chemotherapy and imaging.
  • Challenges include nonselective responses, triggers in healthy tissues, and tumor heterogeneity impacting target recognition.

Purpose of the Study:

  • To develop an artificial system mimicking biological machinery for targeted cancer therapy.
  • To create stimuli-responsive nanoassemblies that form multivalent ligands for cancer-associated enzymes.

Main Methods:

  • Utilized a bio-orthogonal click reaction between hetero nanoassemblies to trigger complexation and conformational changes.
  • Generated multivalent ligands targeting carbonic anhydrase IX (CAIX).
  • Assessed selective inhibition of CAIX-overexpressing cancer cells under hypoxic conditions.

Main Results:

  • The bio-orthogonal click reaction successfully formed multivalent ligands for CAIX.
  • These ligands selectively inhibited the proliferation of cancer cells overexpressing CAIX.
  • Nanoassembly complexation in the presence of target cells enhanced ligand efficacy compared to pre-formed ligands.

Conclusions:

  • The developed system provides a basis for creating adaptive multivalent ligands with high selectivity and affinity for cancer cells.
  • This approach has the potential to overcome challenges posed by tumor heterogeneity in cancer therapy.
Keywords:
bio-orthogonal chemistrycancerclick reactionmultivalent ligandnanoassembly

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