Enhanced cytotoxicity of a polymer-drug conjugate with triple payload of paclitaxel

Rotem Erez, Ehud Segal, Keren Miller, Ronit Satchi-Fainaro, Doron Shabat*

*Corresponding author for this work

Research output: Contribution to journalArticlepeer-review


The development of targeting approaches to selectively release chemotherapeutic drugs into malignant tissue is a major challenge in anticancer therapy. We have synthesized an N-(2-hydroxypropyl)-methacrylamide (HPMA) copolymer-drug conjugate with an AB3 self-immolative dendritic linker. HPMA copolymers are known to accumulate selectively in tumors. The water-soluble polymer-drug conjugate was designed to release a triple payload of the hydrophobic drug paclitaxel as a result of cleavage by the endogenous enzyme cathepsin B. The polymer-drug conjugate exhibited enhanced cytotoxicity on murine prostate adenocarcinoma (TRAMP C2) cells in comparison to a classic monomeric drug-polymer conjugate.

Original languageEnglish
Pages (from-to)4327-4335
Number of pages9
JournalBioorganic and Medicinal Chemistry
Issue number13
StatePublished - 1 Jul 2009


  • Conjugate
  • HPMA copolymer
  • Paclitaxel
  • Polymer therapeutics
  • Prodrug
  • Self-immolative


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