A Short Review on the Delivery of Breast Anticancer Drug Tamoxifen and its Metabolites by Serum Proteins
| Autor: | Thomas Tj, Bourassa P, Tajmir Riahi Ha |
|---|---|
| Rok vydání: | 2016 |
| Předmět: |
0301 basic medicine
Drug 030103 biophysics Materials science biology media_common.quotation_subject Nanotechnology 02 engineering and technology 021001 nanoscience & nanotechnology Human serum albumin Blood proteins 03 medical and health sciences Biochemistry Nanotoxicology Dendrimer medicine biology.protein Bovine serum albumin 0210 nano-technology Tamoxifen medicine.drug media_common Conjugate |
| Zdroj: | Journal of Nanomedicine Research. 4 |
| ISSN: | 2377-4282 |
| DOI: | 10.15406/jnmr.2016.04.00080 |
| Popis: | The loading of tamoxifen (Tam), 4-hydroxytamoxifen (4-OH-Tam) and endoxifen (End) by carrier proteins, human serum albumin (HSA) and bovine serum albumin (BSA) was reviewed in aqueous solution at physiological pH. The binding study is directly related to the conjugation of tamoxifen and its metabolites with serum proteins. Tamoxifen and its metabolites bind serum proteins via hydrophobic, hydrophilic and H-bonding contacts. The loading efficacy (LE) was 45-52% 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 -11.25 Kcal/mol for drug-HSA and -13.79 to -12.72 Kcal/mol for drug-BSA conjugates. Drug conjugation induced major perturbations on the conformation of serum proteins. Our studies indicate that serum proteins can transport tamoxifen and its metabolites to target tissues in the human body. |
| Databáze: | OpenAIRE |
| Externí odkaz: |
|