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Synthesis and Bioconjugation of Thiol-Reactive Reagents for the Creation of Site-Selectively Modified Immunoconjugates
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Recent Advances in the Linkers of Drug Conjugates

Shirui Deng1, Xiaoan Wen1, Jinzheng Wang2

  • 1State Key Laboratory of Natural Medicines, School of China Pharmaceutical University, Nanjing, China.

Current Medicinal Chemistry
|September 18, 2024
PubMed

Insights

Drug conjugates enhance cancer therapy by improving drug efficacy and reducing side effects. Linker stability and cleavage are key to their targeted action and therapeutic potential.

Area of Science:

  • Oncology
  • Medicinal Chemistry
  • Drug Delivery

Background:

  • Drug conjugates are crucial in targeted cancer therapy.
  • They act as prodrugs, improving the therapeutic index and minimizing side effects.
  • Linker stability and selective cleavage are vital for efficacy.

Purpose of the Study:

  • To review and categorize drug conjugate linkers based on cleavage mechanisms.
  • To summarize the chemical properties, benefits, and drawbacks of various cleavable linkers.
  • To highlight specific linker types with development potential.

Main Methods:

  • Literature review and categorization of cleavable linkers.
  • Analysis of chemical properties, advantages, and limitations.
  • Case studies illustrating linker applications.

Main Results:

  • Classification of linkers by cleavage mode.
  • Detailed summary of diverse cleavable linker characteristics.
  • Identification of promising linkers for future drug conjugate development.

Conclusions:

  • Cleavable linkers are essential components of effective drug conjugates.
  • Understanding linker properties guides the design of targeted cancer therapeutics.
  • This review provides a framework for selecting and developing optimal linkers.
Keywords:
Linkersantibody-drug conjugatescleavable linkersnon-cleavable linkerspeptide-drug conjugatestargeted therapy.

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