Chlorambucil-taurocholate is transported by bile acid carriers expressed in human hepatocellular carcinomas
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Research progress in the application of bile acid-drug conjugates: A “trojan horse” strategy
2021, SteroidsCitation Excerpt :After coupling with BAs, the kidney elimination mode of chlorambucil is transformed to the hepatobiliary mode. Studies have shown that human HCCs express Na+-dependent basolateral BA transporters, which can mediate the uptake of the cytostatic agent chlorambucil coupled to taurocholate [41]. In 1997, Criado et al. [85,88] used this strategy to target platinum-metal anticarcinogens in the hepatobiliary system, which solved the application limitation of nephrotoxicity, myelotoxicity, neurotoxicity, nausea, and vomiting caused by its lack of selectivity and susceptibility to drug resistance.
Bile acid transporter as a bioinspired method for oral therapeutics delivery system
2021, Bioinspired and Biomimetic Materials for Drug DeliveryMetabolomics study of the metabolic changes in hepatoblastoma cells in response to NTCP/SLC10A1 overexpression
2020, International Journal of Biochemistry and Cell BiologyUrsodeoxycholic acid and cancer: From chemoprevention to chemotherapy
2019, Pharmacology and TherapeuticsCitation Excerpt :Bile acids-chlorambucil conjugates were also designed to change the normal route of elimination of chlorambucil (kidney excretion) to a hepatobiliary one. A chlorambucil-taurocholate conjugate was shown to maintain the pharmacological activity of the parent DNA alkylating drug (Kullak-Ublick et al., 1997). Very recently, bile acids were conjugated to dihydroartemisinin (DHA) to afford a series of cytotoxic hybrid molecules (Marchesi et al., 2019).