Screening a combinatorial peptide library to develop a human glandular kallikrein 2-activated prodrug as targeted therapy for prostate cancer.

Journal article

OBJECTIVE: Prostate cancer cells secrete the unique protease human glandular kallikrein 2 (hK2) that represents a target for proteolytic activation of cytotoxic prodrugs. The objective of this study was to identify hK2-selective peptide substrates that could be coupled to a cytotoxic analogue of thapsigargin, a potent inhibitor of the sarcoplasmic/endoplasmic reticulum calcium ATPase pump that induces cell proliferation-independent apoptosis through dysregulation of intracellular calcium lev...

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Authors: Janssen, S; Jakobsen, C; Rosen, D; Ricklis, R; Reineke, U

• Journal: Molecular cancer therapeutics
• Volume: 3
• Issue: 11
• Pages: 1439-1450
• Publication date: 2004-11-01
• EISSN: 1538-8514
• ISSN: 1535-7163
• Language: English
• Keywords: Amino Acid Sequence; Prostatic Neoplasms; Prodrugs; Cathepsin B; Mice; Substrate Specificity; Tissue Kallikreins; Trypsin; Thapsigargin; Humans; Peptides; Peptide Library; Antineoplastic Agents; Male; Molecular Structure; Animals; Hydrolysis; Cell Line, Tumor; Drug Evaluation, Preclinical