β-Glucuronide Linkers


The design of novel conjugates for the selective release of therapeutic drugs at the lesion site offers a highly attractive pharmacological approach for future treatment of cancer and other indications. The β-glucuronide linkers can regulate the distribution and level of the drug in tissues and promote the release of the drug from the non-internalizing conjugate. Under the action of β-glucuronidase, the drug-linker would be hydrolyzed at the glycosidic bond and undergo 1,6-elimination with loss of carbon dioxide to liberate drug. β-glucuronide linkers with its high aqueous solubility, long plasma half-life, and facile drug release, is a complementary alternative to PABC dipeptide, disulfide, and hydrazone-based linkers.

CD Bioparticles' services with customized delivery strategies, precise designs and modifications of drugs or drug-contained cargos, and advanced technical platforms can help you to solve:

The challenges you might meet:

  • The efficacy and safety of the drug delivery system are inadequate
  • The drug carrier is not stable in the blood
  • Cleavable linkers are not cleaved at the target tumor site
  • Drugs cannot penetrate deep into tumor tissue to reach tumor cells
  • Intracellular drug release is difficult to achieve
  • The drug carrier itself is highly toxic
  • Complex β-glucuronide linkers are difficult to synthesize
  • Cleavable linkers cannot break under mild conditions

Key features:

Key benefits:

  • High bioavailability and biocompatibility
  • Improve the hydrophilicity of the drugs delivered
  • β-Glucuronide Linkers are not toxic in vivo
  • Interact with or to manipulate the biological target
  • Suitable for in vitro and in vivo experiments
  • Ready-to-use

Application candidates:

  • As an important indicator of body development and disease occurrence
  • Study on metabolism of glucuronidation and drug metabolism in vivo
  • To detect the cytotoxic activity of the compound
  • Treatment of various cancers
  • Be reactive groups for protein crosslinking, ligation or for click chemistry

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