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| Content Provider | World Health Organization (WHO)-Global Index Medicus |
|---|---|
| Author | Dömötör, Orsolya Hartinger, Christian G. Bytzek, Anna K. Kiss, Tamás Keppler, Bernhard K. Enyedy, Eva A. |
| Description | Country affiliation: Hungary Author Affiliation: Dömötör O ( Department of Inorganic and Analytical Chemistry, University of Szeged, Dóm tér 7, Szeged 6720, Hungary.) |
| Abstract | Indazolium trans-[tetrachloridobis(1H-indazole)ruthenate(III)] (KP1019) and its $Na^{+}$ analogue (KP1339) are two of the most prominent non-platinum antitumor metal complexes currently undergoing clinical trials. After intravenous administration, they are known to bind to human serum albumin (HSA) in a noncovalent manner. To elucidate their HSA binding sites, displacement reactions with the established site markers warfarin and dansylglycine as well as bilirubin were monitored by spectrofluorimetry, ultrafiltration–UV–vis spectrophotometry, and/or capillary zone electrophoresis. Conditional stability constants for the binding of KP1019 and KP1339 to sites I and II of HSA were determined, indicating that both Ru(III) compounds bind to both sites with moderately strong affinity (log K $_{1}′ = 5.3–5.8).$ No preference for either binding site was found, and similar results were obtained for both metal complexes, demonstrating low influence of the counter ion on the binding event. |
| File Format | HTM / HTML |
| ISSN | 09498257 |
| Issue Number | 1 |
| Volume Number | 18 |
| e-ISSN | 14321327 |
| Journal | JBIC Journal of Biological Inorganic Chemistry |
| Language | English |
| Publisher | Springer |
| Publisher Date | 2013-01-01 |
| Publisher Place | Germany |
| Access Restriction | One Nation One Subscription (ONOS) |
| Subject Keyword | Discipline Biochemistry Antineoplastic Agents Metabolism Binding, Competitive Indazoles Organometallic Compounds Ruthenium Chemistry Serum Albumin Bilirubin Heme Humans Spectrometry, Fluorescence Journal Article Research Support, Non-u.s. Gov't |
| Content Type | Text |
| Resource Type | Article |
| Subject | Biochemistry Inorganic Chemistry |
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