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.