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Figure 1 | Molecular Cancer

Figure 1

From: Synthesis, identification and in vivo studies of tumor-targeting agent peptide doxorubicin (PDOX) to treat peritoneal carcinomatosis of gastric cancer with similar efficacy but reduced toxicity

Figure 1

PDOX structure (shown in the box), chemical synthesis and action mechanism. PDOX was successfully synthesized according to the 7-step chemical process. Its chemical structure is Ac-Phe-Lys-PABC-Dox·HCl (shown in the box), and the molecular formula is C52H60ClN5O16. PDOX contains a CTSB-cleavable dipeptide Ac-Phe-Lys (double red slashes) a PABC spacer (red slash) and anti-cancer drug DOX. When PDOX reaches CTSB-enriched area such as the invasion front of cancer, the Ac-Phe-Lys dipeptide is cleaved by CTSB at the Lys-PABC bond, exposing the PABC spacer that is then hydrolyzed spontaneously (red slash), releasing free DOX at the cancer invasion front. Thus PDOX could exert cytotoxicity to invading cancer cells while protecting normal cells from excessive drug exposure, a strategy called passive targeted therapy. CTSB: cathepsin B.

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Molecular Cancer

ISSN: 1476-4598