Cathepsin B-sensitive dipeptide prodrugs. 1. A model study of structural requirements for efficient release of doxorubicin

Bioorg Med Chem Lett. 1998 Dec 1;8(23):3341-6. doi: 10.1016/s0960-894x(98)00609-x.

Abstract

A series of lysosomal protease-sensitive peptides attached to doxorubicin (DOX) was prepared as model substrates for internalizing anticancer immunoconjugates and potential antimetastasis prodrugs. Rates of cathepsin B-mediated release of free drug was measured for each, and human plasma stabilities for representative examples.

MeSH terms

  • Cathepsin B / metabolism*
  • Dipeptides / chemical synthesis*
  • Dipeptides / chemistry
  • Doxorubicin / chemical synthesis*
  • Doxorubicin / chemistry
  • Doxorubicin / metabolism
  • Drug Carriers
  • Drug Stability
  • Humans
  • Models, Molecular
  • Prodrugs / chemical synthesis*
  • Prodrugs / chemistry
  • Prodrugs / metabolism

Substances

  • Dipeptides
  • Drug Carriers
  • Prodrugs
  • Doxorubicin
  • Cathepsin B