A triple-targeting delivery system carrying two anticancer agents

• Published in: Organic & biomolecular chemistry Vol. 19; no. 37; pp. 89 - 813
• Main Authors: Li, Hui, Lee, Chang-Hee, Shin, Injae
• Format: Journal Article
• Language: English
• Published: CAMBRIDGE Royal Soc Chemistry 29.09.2021; Royal Society of Chemistry
• Subjects: Anticancer properties; Antineoplastic Agents - chemistry; Antineoplastic Agents - pharmacology; Antitumor agents; Cancer; Cathepsin B; Cathepsin B - antagonists & inhibitors; Cathepsin B - metabolism; Cell Line, Tumor; Chemistry; Chemistry, Organic; Doxorubicin; Doxorubicin - chemistry; Doxorubicin - pharmacology; Drug Carriers - chemistry; Drug Delivery Systems; Drug Screening Assays, Antitumor; Humans; Hydrogen peroxide; Hydrogen Peroxide - chemistry; Physical Sciences; Science & Technology; Selectivity; Tumors; APOPTOSIS; PRODRUG; SMALL-MOLECULE; HYDROGEN-PEROXIDE; CYSTEINE CATHEPSINS; INHIBITOR; CANCER; PROTEASES
• ISSN: 1477-0520; 1477-0539; 1477-0539
• DOI: 10.1039/d1ob01089a

To improve tumor selectivity, a triple-targeting delivery system (Oct-FK(PBA-Az)-Dox) carrying two anticancer agents (apoptozole (Az) and doxorubicin (Dox)) was designed and synthesized. The results showed that both anticancer agents in Oct-FK(PBA-Az)-Dox are liberated in the presence of both H 2 O 2 and cathepsin B, which are normally present at high levels in tumors. To improve tumor selectivity, we prepared a new triple-targeting delivery system bearing two anticancer agents. Both anticancer agents in this system are released in the presence of both H 2 O 2 and cathepsin B which are highly produced in cancer cells.