Prostate-specific antigen-activated thapsigargin prodrug as targeted therapy for prostate cancer.

Journal article

BACKGROUND: Standard anti-proliferative chemotherapy is relatively ineffective against slowly proliferating androgen-independent prostate cancer cells within metastatic sites. In contrast, the lipophilic cytotoxin thapsigargin, which causes apoptosis by disrupting intracellular free Ca2+ levels, is effective against both proliferative and quiescent (i.e., G0-arrested) cells. However, thapsigargin's mechanism of action indicates that it is unlikely to be selective for cancer cells or prostate...

Expand abstract

Authors: Denmeade, SR; Jakobsen, C; Janssen, S; Khan, SR; Garrett, E

• Journal: Journal of the National Cancer Institute
• Volume: 95
• Issue: 13
• Pages: 990-1000
• Publication date: 2003-07-01
• DOI: 10.1093/jnci/95.13.990
• EISSN: 1460-2105
• ISSN: 0027-8874
• Language: English
• Keywords: Prostate-Specific Antigen; Animals; Mice, Nude; Prodrugs; Mice; Transplantation, Heterologous; Disease Models, Animal; Hydrolysis; Thapsigargin; Humans; Antineoplastic Agents; Male; Prostatic Neoplasms; Treatment Outcome