Kód: 18179281
Targeted delivery of anticancer drugs in vivo remains a major challenge. Serum proteins are emerging as potential carriers for drug delivery. In this book, the loading efficacies of anticancer drugs doxorubicin (Dox) tamoxifen (Ta ... celý popis
Nákupem získáte 76 bodů
Targeted delivery of anticancer drugs in vivo remains a major challenge. Serum proteins are emerging as potential carriers for drug delivery. In this book, the loading efficacies of anticancer drugs doxorubicin (Dox) tamoxifen (Tam), 4-hydroxytamoxifen (4-OH-Tam) and endoxifen (End) by carrier proteins, human serum albumin(HSA), bovine serum albumin (BSA) and beta-lactoglobulin (b-LG) were compared in aqueous solution at physiological condition. Doxorubicin, tamoxifen and its metabolites bind serum proteins via hydrophobic, hydrophilic and H-bonding contacts. The loading efficacy (LE) was 45-55% for drug-protein conjugates. Modeling showed the presence of H-bonding, which stabilized drug-protein complexation with the free binding energy of -11.79 to -10.75 for drug-HSA, -13.79 to -9.30 for drug-BSA and -8.12 Kcal/mol for drug-b-LG adducts. Drug conjugation induced major perturbations of the protein conformation. The results indicated that serum proteins are capable of transporting anticancer drugs to target molecules.
755 Kč
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