Proteases as Activators for Cytotoxic Prodrugs in Antitumor Therapy

Cancer Genomics - Proteomics

GEORG TIEFENTHALER¹  ULRICH H. WEIDLE¹  GUY GEORGES¹ 

[1] Roche Pharma Research and Early Development (pRED), Roche Diagnostics GmbH, Penzberg, GermanyRoche Pharma Research and Early Development (pRED), Roche Diagnostics GmbH, Penzberg, GermanyRoche Pharma Research and Early Development (pRED), Roche Diagnostics GmbH, Penzberg, Germany

关键词: Antibody-drug conjugates;    antibody-directed enzyme prodrug therapy;    Anthrax toxin;    cytotoxic receptor ligand(s);    granzyme B;    probody;    thapsigargin;    review;   

DOI  :  

来源: Delinasios GJ CO

【 摘 要 】

Proteases are often overexpressed in tumor cells and/or the stromal compartment and can thus be exploited in tumor therapy to activate cytotoxic prodrugs as, for example, in cytolytic fusion proteins, and for tumor imaging. Specifically, we discuss cathepsin B-activated prodrug conjugates, antibody-directed prodrug therapy, protease-activated peptide-thapsigargin conjugates, protease-activated cytotoxic receptor ligands and other cytotoxic proteins, protease-mediated activation of anthrax toxin, granzyme B as a therapeutic principle in cytolytic fusion proteins, and tumor-imaging based on deregulated proteases.

【 授权许可】

Unknown