Picosecond time-resolved fluorescence studies characterize the binding between the novel fluorescent anti-angiogenic drug PNU151484 and human basic fibroblast growth factor

Abraham H. Parola, Moreno Zamai, Valeria R. Caiolt, V. Dîna Pines, Ehud Pines

Research output: Contribution to journalArticlepeer-review

Abstract

PNU15 1484. an anti-angiogemc compound named suradista. exerts its activit)' by interacting with hcparin binding gro\\th factors. The in-vitro complex fonnation between PNU 151484 and lui man recombinant basic fibroblasl growth factor (bFGF) \\as studied due to ils relevance to tumoral angiogenesis Titration experiments \\ere followed by quantitati\e higli performance affinity Chromatograph), ps time-resoked fluorescence emission and anisotrop) studies in PBS (pH 7.1) at 20!0 Affimh chromatography revealed a dissociation constant of 1 5 \10-7 M The binding isotherm, constructed b> the method of fluorescence lifetime titration. yielded a dissociation constant of I 0 \10-7 M Time-resolved decay of anisotrop) stud) resulted m a similar dissociation constant after correction for drug dimerization at the relative!) higher drug concentration emplo) cd PNU 15 14X4 bFGF is a tight complex with a I I stoichiometry, and studies of solvent effect on the ding's lifetime highlights the mode of mteracion of suradista with HBGFs. Since it does not cause protein aggregation, suradista has a potential clinical applicability.

Original languageEnglish
Pages (from-to)A1426
JournalFASEB Journal
Volume11
Issue number9
StatePublished - 1 Dec 1997

ASJC Scopus subject areas

  • Biotechnology
  • Biochemistry
  • Molecular Biology
  • Genetics

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