Energetic characterization of 1,3,6-naphtalene trisulfonate binding to human acidic fi broblast growth factor: implications for its anti-angiogenic use

Authors

  • M GARCÍA-MIRA Departamento de Química-Física e Instituto de Biotecnología, Facultad de Ciencias
  • M GUZMÁN-CASADO Departamento de Química-Física e Instituto de Biotecnología, Facultad de Ciencias
  • G GIMÉNEZ-GALLEGO Centro de Investigaciones Biológicas (CSIC), Madrid
  • A PARODY-MORREALE Departamento de Química-Física e Instituto de Biotecnología, Facultad de Ciencias

Keywords:

1, 3, 6-naphatalene trisulfonate, Human acidic fibroblast growth factor, Isothermal titration calorimetry, Anti-angiogenesis, Energetically driven drug design

Abstract

The equilibrium interaction of anti-cancer agent 1,3,6-naphatalene trisulfonate with human acidic fi broblast growthfactor has been studied by calorimetry. The affi nity decreases with increasing ionic strength. At pH 7.0 and 0.15 MNaCl concentration, a binding constant of the protein with the ligand was estimated in the 102 – 103 M-1 range, anaffi nity two orders of magnitude lower than that of aFGF with heparin. The interaction is enthalpically driven, andthe entropy change is unfavorable. A small heat capacity change with an unusual positive value of 90 cal K-1mol-1 wasdetermined from the temperature dependence of the enthalpies. Changes in accessible apolar and polar surface areasin the interaction were calculated from the thermodynamic data obtained and parametric equations in the literature.The results were compared with those measured from NMR data. The study includes structural bioenergetic considerationsabout the possible use of 1,3,6-naphatalene trisulfonate as an anti-angiogenic agent itself, or as a lead for thedevelopment of anti-angiogenic drugs.

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Published

2006-09-20

How to Cite

1.
GARCÍA-MIRA M, GUZMÁN-CASADO M, GIMÉNEZ-GALLEGO G, PARODY-MORREALE A. Energetic characterization of 1,3,6-naphtalene trisulfonate binding to human acidic fi broblast growth factor: implications for its anti-angiogenic use. Ars Pharm [Internet]. 2006 Sep. 20 [cited 2024 May 19];47(3):321-37. Available from: https://revistaseug.ugr.es/index.php/ars/article/view/5036

Issue

Vol. 47 No. 3 (2006)

Section

Original Articles

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