Antitumor drug-protein interactions. Binding of 1-β-D-arabinofuranosyl cytosine to albumin and chemically modified albumin

M. Szekerke, M. Horvath, F. Hudecz

Research output: Contribution to journalArticle

6 Citations (Scopus)

Abstract

Equilibrium dialysis measurements were carried out to study the binding of 1-β-D-arabinofuranosyl cytosine (ara-C) to human and bovine serum albumin (HSA, BSA) and to chemically modified albumin. The binding of 4-phenylbutyric acid to HSA was studied, too. Binding data were presented as Scatchard plots. There are two types of binding sites of different affinity for ara-C both on HSA and BSA. The relatively small value of affinity constant indicates that the pharmacological properties of ara-C might not be influenced very strongly by the HSA interaction or by competitive binding of other drugs. Selective chemical modifications of HSA with diethylpyrocarbonate (DEP) or o-nitrophenylsulfenyl chloride (NSP-Cl) reduce significantly the affinity of the strong binding area. On the other hand, the attachment of poly-a-L-glutamyl or poly-DL-alanyl side-chains to BSA increase the number of the strong and secondary binding sites and also the affinity at the first group of sites. Experimental results suggest a correlation between the binding affinity and therapeutic efficacy of various cytotoxic drug-protein complexes.

Original languageEnglish
Pages (from-to)19-21
Number of pages3
JournalArzneimittel-Forschung
Volume29
Issue number1
Publication statusPublished - 1979

Fingerprint

Cytosine
Drug Interactions
Antineoplastic Agents
Albumins
Binding Sites
Diethyl Pyrocarbonate
Proteins
Competitive Binding
Dialysis
Chemical modification
Bovine Serum Albumin
Pharmaceutical Preparations
Chlorides
Pharmacology
Therapeutics

ASJC Scopus subject areas

  • Chemistry(all)
  • Organic Chemistry
  • Drug Discovery
  • Pharmacology

Cite this

Antitumor drug-protein interactions. Binding of 1-β-D-arabinofuranosyl cytosine to albumin and chemically modified albumin. / Szekerke, M.; Horvath, M.; Hudecz, F.

In: Arzneimittel-Forschung, Vol. 29, No. 1, 1979, p. 19-21.

Research output: Contribution to journalArticle

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