Development of a novel albumin-binding prodrug that is cleaved by urokinase-type-plasminogen activator (uPA)

Bioorg Med Chem Lett. 2006 Oct 1;16(19):5157-63. doi: 10.1016/j.bmcl.2006.07.023. Epub 2006 Jul 27.

Abstract

A water-soluble albumin-binding prodrug of doxorubicin [EMC-Gly-Gly-Gly-Arg-Arg-DOXO (EMC, 6-maleimidocaproic acid)] was developed that is cleaved specifically by the tumor-associated protease urokinase-type plasminogen activator (uPA).

MeSH terms

  • Antineoplastic Agents / administration & dosage*
  • Antineoplastic Agents / pharmacokinetics
  • Doxorubicin / administration & dosage*
  • Doxorubicin / blood
  • Doxorubicin / pharmacokinetics
  • Drug Delivery Systems
  • Humans
  • Prodrugs / metabolism*
  • Prodrugs / pharmacokinetics
  • Protein Binding
  • Serum Albumin / metabolism*
  • Solubility
  • Structure-Activity Relationship
  • Urokinase-Type Plasminogen Activator / metabolism*

Substances

  • Antineoplastic Agents
  • Prodrugs
  • Serum Albumin
  • Doxorubicin
  • Urokinase-Type Plasminogen Activator