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Click chemistry-driven tumor theranostics: recent advances, challenges, and future perspectives.

Dayong Hou1,2, Xiangpeng Li1,2, Niyuan Zhang1

  • 1CAS Key Laboratory for Biomedical Effects of Nanomaterials and Nanosafety, CAS Center for Excellence in Nanoscience, National Center for Nanoscience and Technology (NCNST), Beijing 100190, China.

Cancer Biology & Medicine
|March 13, 2026
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Summary

Click chemistry enables advanced tumor theranostics by precisely integrating diagnosis and therapy. This review highlights its role in molecular imaging, targeted treatments, and combined approaches for improved cancer care.

Keywords:
Click chemistryclinical translationmolecular imagingmultimodal integrationprecision therapytumor theranostics

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Area of Science:

  • Oncology
  • Chemical Biology
  • Biomedical Engineering

Background:

  • Tumor theranostics combines diagnosis and therapy to enhance cancer treatment efficacy and reduce toxicity.
  • Click chemistry offers high efficiency, selectivity, and biocompatibility, making it ideal for developing theranostic systems.

Purpose of the Study:

  • To systematically review recent advancements in click chemistry-based tumor theranostic systems.
  • To discuss the application of click chemistry in tumor diagnosis, therapy, and integrated theranostics.
  • To identify current challenges and future directions in the field.

Main Methods:

  • Overview of core click reactions and their biomedical applications.
  • Focus on click chemistry applications in molecular imaging, circulating tumor cell detection, chemotherapy, phototherapy, immunotherapy, and gene therapy.
  • Discussion of multimodal imaging-guided combinatorial therapy.

Main Results:

  • Click chemistry facilitates the construction of versatile theranostic systems for various cancer applications.
  • It enables precise molecular imaging, targeted drug delivery, and combination therapies.
  • The review critically examines challenges like catalyst biocompatibility and in vivo efficiency.

Conclusions:

  • Click chemistry is a powerful tool for developing sophisticated tumor theranostic systems.
  • Future directions include stimuli-responsive reactions, AI-assisted design, and personalized medicine.
  • Click chemistry offers spatiotemporal control, modularity, and bioorthogonal precision crucial for clinical translation.