Pre-association of polynuclear platinum anticancer agents on a protein, human serum albumin. Implications for drug design†
| Autor: | Yun Qu, Michael J. Oehlsen, Nicholas Farrell, John B. Mangrum, Eva I. Montero, Brad T. Benedetti |
|---|---|
| Jazyk: | angličtina |
| Rok vydání: | 2007 |
| Předmět: |
Drug
Circular dichroism Spectrometry Mass Electrospray Ionization media_common.quotation_subject Electrospray ionization Circular Dichroism chemistry.chemical_element Antineoplastic Agents Human serum albumin Sulfur Medicinal chemistry Fluorescence Article Inorganic Chemistry Spectrometry Fluorescence chemistry Nucleophile Drug Design medicine Organic chemistry Platinum Serum Albumin medicine.drug media_common |
| Popis: | The interactions of polynuclear platinum complexes with human serum albumin were studied. The compounds examined were the "non-covalent" analogs of the trinuclear BBR3464 as well as the dinuclear spermidine-bridged compounds differing in only the presence or absence of a central -NH(2)-(+) (BBR3571 and analogs). Thus, closely-related compounds could be compared. Evidence for pre-association, presumably through electrostatic and hydrogen-bonding, was obtained from fluorescence and circular dichroism spectroscopy and Electrospray Ionization Mass Spectrometry (ESI-MS). In the case of those compounds containing Pt-Cl bonds, further reaction took place presumably through displacement by sulfur nucleophiles. The implications for protein pre-association and plasma stability of polynuclear platinum compounds are discussed. |
| Databáze: | OpenAIRE |
| Externí odkaz: |
|