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β-Glucuronidase-responsive prodrugs for selective cancer chemotherapy: an update

Isabelle Tranoy-Opalinski1, Thibaut Legigan1, Romain Barat1

  • 1Université de Poitiers, UMR-CNRS 7285, Institut de Chimie des Milieux et des Matériaux de Poitiers (IC2MP), Groupe "Systèmes Moléculaires Programmés", 4 rue Michel Brunet, 86022 Poitiers, France.

European Journal of Medicinal Chemistry
|February 1, 2014
PubMed

Insights

Novel prodrugs activated by beta-glucuronidase offer a promising strategy for cancer therapy. These agents selectively target tumor cells, minimizing damage to healthy tissues, representing a significant advance in medicinal chemistry.

Area of Science:

  • Medicinal Chemistry
  • Oncology
  • Drug Delivery

Background:

  • Developing targeted antitumor agents that spare healthy tissues is a key challenge.
  • Beta-glucuronidase (GUS) is highly concentrated in the tumor microenvironment, making it a promising target for selective drug activation.
  • Prodrug strategies utilizing GUS activation offer a potential solution for targeted cancer therapy.

Purpose of the Study:

  • To review advancements in GUS-activated prodrugs for cancer treatment over the last decade.
  • To highlight novel prodrug designs and their therapeutic applications.
  • To discuss emerging concepts in GUS-responsive drug delivery systems.

Main Methods:

  • Literature review of scientific publications from the past 10 years.
  • Focus on prodrugs designed for selective activation by beta-glucuronidase.
  • Analysis of various prodrug strategies, including those for combined therapy and albumin binding.

Main Results:

  • Significant progress in designing novel prodrugs for diverse anticancer drugs.
  • Development of prodrugs for combined therapeutic approaches.
  • Introduction of dendritic glucuronide prodrugs and beta-glucuronidase-responsive albumin binding prodrugs.

Conclusions:

  • Beta-glucuronidase-activated prodrugs represent a significant advancement in targeted cancer therapy.
  • These strategies enhance drug selectivity, improving the therapeutic index.
  • Future research holds promise for further optimizing these prodrug systems for clinical application.
Keywords:
Cancer chemotherapyGlucuronide prodrugsSelf-immolative linkersTumor targeting

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