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Targeted Engineering of Medicinal Chemistry for Cancer Therapy: Recent Advances and Perspectives

Weihua Chen1, Zhen Sun1, Lehui Lu1

  • 1State Key Laboratory of Electroanalytical Chemistry, Changchun Institute of Applied Chemistry, University of Science and Technology of China, Changchun, 130022, China.

Angewandte Chemie (International Ed. in English)
|February 26, 2020
PubMed

Insights

Current anticancer drugs have severe side effects and poor efficacy. This review explores cancer targeting strategies and drug properties needed for improved therapeutic outcomes in precision medicine.

Area of Science:

  • Oncology
  • Pharmacology
  • Biomedical Engineering

Background:

  • Current anticancer drugs suffer from severe side effects and limited therapeutic efficacy.
  • Drug targeting strategies can mitigate these drawbacks, but current targeting efficacy requires significant improvement.

Purpose of the Study:

  • To review current cancer targeting strategies for both tissues and organelles.
  • To analyze the systematic targeting process of anticancer drugs and identify key properties for optimizing drug structures.
  • To present future challenges and opportunities in targeted cancer therapy and precision medicine.

Main Methods:

  • Systematic review of existing literature on cancer targeting strategies.
  • Analysis of the multi-step cascade (Circulation, Targeting, Internalization, Offloading - CTIO) in targeted drug delivery.
  • Evaluation of drug properties essential for efficacy at each step of the CTIO cascade.

Main Results:

  • A typical targeted drug delivery via intravenous injection follows a CTIO cascade of at least four steps.
  • Specific drug properties are crucial for successful progression through each step of the CTIO cascade.
  • Guidelines for structure optimization are proposed to enhance the targeting efficacy of anticancer drugs.

Conclusions:

  • Improving the targeting efficacy of anticancer drugs is critical for enhancing therapeutic outcomes and reducing side effects.
  • Understanding and optimizing the CTIO cascade is essential for developing more effective targeted cancer therapies.
  • This review provides a framework for advancing precision medicine in oncology through improved drug design.
Keywords:
cancer therapydrug deliverymedicinal chemistrymolecular engineeringtargeting strategies

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