ArticlePloS one2012
Probing the binding sites of antibiotic drugs doxorubicin and N-(trifluoroacetyl) doxorubicin with human and bovine serum albumins.
Article in PloS one, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 47 papers.
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Who cites it
47 citing papers in PubMed, 211 citations in OpenAlex.
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- Albumin conjugated with WQPDTAHHWATL and GRFLTGGTGRLLRIS peptide improves targeted docetaxel delivery for prostate cancer: anResearch in pharmaceutical sciences · 2025Article
- Spectrophotometric and smartphone-based colorimetric methods utilizing polyvinylpyrrolidone-capped silver nanoparticles for determining doxorubicin in human plasma samples.Scientific reports · 2025Article
- In vivo and in situ monitoring of doxorubicin pharmacokinetics with an implantable bioresorbable optical sensor.Science advances · 2025Article
- Cyclooxygenase-2/prostaglandin E2 inhibition remodulated photodynamic therapy-associated immunosuppression for enhanced cancer immunotherapy.Materials today. Bio · 2025Article
- Article
- Human Serum Albumin and Human Serum Albumin Nanoparticles as Carriers of 10-(2'-Pyrimidyl)-3,6-diazaphenothiazine: In Vitro Spectroscopic Studies.Molecules (Basel, Switzerland) · 2025Article
- Conjugated Human Serum Albumin/Gold-Silica Nanoparticles as Multifunctional Carrier of a Chemotherapeutic Drug.International journal of molecular sciences · 2024Article
- Chitosan/Alginate Nanogels Containing Multicore Magnetic Nanoparticles for Delivery of Doxorubicin.Pharmaceutics · 2023Article
- A Synergistic pH-Responsive Serum Albumin-Based Drug Delivery System Loaded with Doxorubicin and Pentacyclic Triterpene Betulinic Acid for Potential Treatment of NSCLC.Biotech (Basel (Switzerland)) · 2023Article
- Diffusion of small molecule drugs is affected by surface interactions and crowder proteins.iScience · 2022Article
- Aptamer-armed nanostructures improve the chemotherapy outcome of triple-negative breast cancer.Molecular therapy : the journal of the American Society of Gene Therapy · 2022Article
- Albumin Binds Doxorubicin via Self-Assembling Dyes as Specific Polymolecular Ligands.International journal of molecular sciences · 2022Article
- Doxorubicin-NO Releaser Molecular Hybrid Activatable by Green Light to Overcome Resistance in Breast Cancer Cells.ACS omega · 2022Article
- Interaction of Supramolecular Congo Red and Congo Red-Doxorubicin Complexes with Proteins for Drug Carrier Design.Pharmaceutics · 2021Article
- Controlled Release of Doxorubicin for Targeted Chemo-Photothermal Therapy in Breast Cancer HS578T Cells Using Albumin Modified Hybrid Nanocarriers.International journal of molecular sciences · 2021Article
- Dual-Targeted Hyaluronic Acid/Albumin Micelle-Like Nanoparticles for the Vectorization of Doxorubicin.Pharmaceutics · 2021Article
- A graphene-sandwiched DNA nano-system: regulation of intercalated doxorubicin for cellular localization.Nanoscale advances · 2020Article
- Effect of the Heteroaromatic Antenna on the Binding of Chiral Eu(III) Complexes to Bovine Serum Albumin.Inorganic chemistry · 2020Article
Corrections and comments
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Authors and funding
6 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
We located the binding sites of doxorubicin (DOX) and N-(trifluoroacetyl) doxorubicin (FDOX) with bovine serum albumin (BSA) and human serum albumins (HSA) at physiological conditions, using constant protein concentration and various drug contents. FTIR, CD and fluorescence spectroscopic methods as well as molecular modeling were used to analyse drug binding sites, the binding constant and the effect of drug complexation on BSA and HSA stability and conformations. Structural analysis showed that doxorubicin and N-(trifluoroacetyl) doxorubicin bind strongly to BSA and HSA via hydrophilic and hydrophobic contacts with overall binding constants of K(DOX-BSA) = 7.8 (± 0.7) × 10(3) M(-1), K(FDOX-BSA) = 4.8 (± 0.5)× 10(3) M(-1) and K(DOX-HSA) = 1.1 (± 0.3)× 10(4) M(-1), K(FDOX-HSA) = 8.3 (± 0.6)× 10(3) M(-1). The number of bound drug molecules per protein is 1.5 (DOX-BSA), 1.3 (FDOX-BSA) 1.5 (DOX-HSA), 0.9 (FDOX-HSA) in these drug-protein complexes. Docking studies showed the participation of several amino acids in drug-protein complexation, which stabilized by H-bonding systems. The order of drug-protein binding is DOX-HSA > FDOX-HSA > DOX-BSA > FDOX>BSA. Drug complexation alters protein conformation by a major reduction of α-helix from 63% (free BSA) to 47-44% (drug-complex) and 57% (free HSA) to 51-40% (drug-complex) inducing a partial protein destabilization. Doxorubicin and its derivative can be transported by BSA and HSA in vitro.
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