Unlocking the potential of platinum drugs: organelle-targeted small-molecule platinum complexes for improved

Zhiqin Deng1,2,3, Shu Chen1,2, Gongyuan Liu1,2

  • 1Department of Chemistry, City University of Hong Kong Hong Kong SAR P. R. China guangzhu@cityu.edu.hk.

RSC Chemical Biology
|November 30, 2023
PubMed

Insights

Organelle-targeted platinum complexes offer a promising strategy to enhance cancer chemotherapy by improving efficacy and overcoming resistance. These targeted platinum drugs show potential for reduced toxicity and novel mechanisms of action.

Area of Science:

  • Medicinal Chemistry
  • Oncology
  • Cell Biology

Background:

  • Platinum-based drugs are mainstays in cancer chemotherapy but face limitations like severe side effects and acquired drug resistance.
  • Organelle-targeting strategies represent a novel approach to enhance the therapeutic index of platinum-based anticancer agents.

Purpose of the Study:

  • To review organelle-targeting strategies for platinum complexes in cancer therapy.
  • To discuss mechanisms by which these strategies improve anticancer activity, overcome resistance, and alter drug action.
  • To guide the design and development of novel platinum-based anticancer drugs.

Main Methods:

  • Literature review of organelle-targeting strategies for platinum complexes.
  • Analysis of studies demonstrating enhanced anticancer activity, overcoming resistance, and altered mechanisms.
  • Discussion of design principles for targeted platinum complexes.

Main Results:

  • Organelle-targeted platinum complexes accumulate in specific intracellular sites like the nucleus, mitochondria, endoplasmic reticulum (ER), and lysosomes.
  • Targeting specific organelles enhances anticancer activity and overcomes drug resistance.
  • These strategies can lead to novel molecular mechanisms and potentially reduced toxicity compared to conventional platinum drugs.

Conclusions:

  • Organelle-specific targeting of platinum complexes is a viable strategy to improve cancer chemotherapy.
  • Understanding design principles for targeted platinum delivery is crucial for developing next-generation anticancer agents.
  • This review provides a foundation for researchers to innovate in the field of platinum-based cancer therapeutics.

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