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:

• (2S,3S,4S,5R,6S)-methyl-6-(2-(3-((Fmoc-amino) propanamido)-4-PNP-3,4,5-triacetoxy-tetrahydro-2H-pyran-2-carboxylate
• 4-Formyl-2-nitrophenyl-β-D-Glucopyranosiduronic Acid Methyl Ester 2,3,4-Triacetate
• β-D-Glucopyranosiduronic acid, 2-amino-4-(hydroxymethyl)phenyl, methyl ester, 2,3,4-triacetate
• β-D-tetraacetylgalactopyranoside-PEG2-azide
• β-D-triacetylglucopyranosiduronyl methyl ester-phenol-β-Alanine
• β-tetraacetylglucopyranoside-glycerol
• β-tetraacetylglucopyranoside-glycol

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