F L Fierens

Summary

Affiliation: Vrije Universiteit Brussel
Country: Belgium

Publications

  1. ncbi Distinct binding properties of the AT(1) receptor antagonist [(3)H]candesartan to intact cells and membrane preparations
    Frederik L P Fierens
    Department of Molecular and Biochemical Pharmacology, Free University of Brussels VUB, 65 Paardenstraat, B 1640 Sint Genesius Rode, Belgium
    Biochem Pharmacol 63:1273-9. 2002
  2. ncbi Insurmountable angiotensin AT1 receptor antagonists: the role of tight antagonist binding
    F L Fierens
    Department of Molecular and Biochemical Pharmacology, Free University of Brussels VUB, Belgium
    Eur J Pharmacol 372:199-206. 1999
  3. ncbi Lys(199) mutation of the human angiotensin type 1 receptor differentially affects the binding of surmountable and insurmountable non-peptide antagonists
    F L Fierens
    Department of Molecular and Biochemical Pharmacology, Free University of Brussels, Rode, B 1640, Belgium
    J Renin Angiotensin Aldosterone Syst 1:283-8. 2000
  4. ncbi Tight binding of the angiotensin AT(1) receptor antagonist
    F L Fierensa
    Department of Molecular and Biochemical Pharmacology, Institute for Molecular Biology, Free University of Brussels, Paardenstraat 65, B 1640, Sint Genesius Rode, Belgium
    Biochem Pharmacol 61:1227-35. 2001
  5. ncbi The effects of candesartan on human AT1 receptor-expressing Chinese hamster ovary cells
    G Vauquelin
    Department of Molecular and Biochemical Pharmacology, Institute of Molecular Biology, Free University of Brussels VUB, Sint Genesius Rode, Belgium
    J Am Soc Nephrol 10:S15-7. 1999
  6. ncbi Reversible and syntopic interaction between angiotensin receptor antagonists on Chinese hamster ovary cells expressing human angiotensin II type 1 receptors
    P M Vanderheyden
    Department of Molecular Pharmacology, Free University of Brussels, Sint Genesius Rode, Belgium
    Biochem Pharmacol 59:927-35. 2000
  7. ncbi Interaction between the partially insurmountable antagonist valsartan and human recombinant angiotensin II type 1 receptors
    I Verheijen
    Department of Molecular and Biochemical Pharmacology, Free University of Brussels, Belgium
    Fundam Clin Pharmacol 14:577-85. 2000
  8. ncbi A two-state receptor model for the interaction between angiotensin II type 1 receptors and non-peptide antagonists
    G Vauquelin
    Department of Molecular and Biochemical Pharmacology, Free University of Brussels VUB, Sint Genesius Rode, Belgium
    Biochem Pharmacol 61:277-84. 2001
  9. ncbi Angiotensin II type 1 receptor antagonists. Why do some of them produce insurmountable inhibition?
    P M Vanderheyden
    Department of Molecular and Biochemical Pharmacology, Free University of Brussels, Sint Genesius Rode, Belgium
    Biochem Pharmacol 60:1557-63. 2000
  10. pmc Distinction between surmountable and insurmountable selective AT1 receptor antagonists by use of CHO-K1 cells expressing human angiotensin II AT1 receptors
    P M Vanderheyden
    Department of Protein Chemistry, Free University of Brussels VUB, Sint Genesius Rode, Belgium
    Br J Pharmacol 126:1057-65. 1999

Collaborators

Detail Information

Publications12

  1. ncbi Distinct binding properties of the AT(1) receptor antagonist [(3)H]candesartan to intact cells and membrane preparations
    Frederik L P Fierens
    Department of Molecular and Biochemical Pharmacology, Free University of Brussels VUB, 65 Paardenstraat, B 1640 Sint Genesius Rode, Belgium
    Biochem Pharmacol 63:1273-9. 2002
    ..Whereas the binding was almost completely enthalpy-driven on intact cells, there was a mixed contribution of both enthalpy and entropy on membranes...
  2. ncbi Insurmountable angiotensin AT1 receptor antagonists: the role of tight antagonist binding
    F L Fierens
    Department of Molecular and Biochemical Pharmacology, Free University of Brussels VUB, Belgium
    Eur J Pharmacol 372:199-206. 1999
    ..Our data indicate that antagonist-receptor complexes are divided into a fast reversible/surmountable population and a tight binding/insurmountable population at the very onset of the incubation with angiotensin II...
  3. ncbi Lys(199) mutation of the human angiotensin type 1 receptor differentially affects the binding of surmountable and insurmountable non-peptide antagonists
    F L Fierens
    Department of Molecular and Biochemical Pharmacology, Free University of Brussels, Rode, B 1640, Belgium
    J Renin Angiotensin Aldosterone Syst 1:283-8. 2000
    ..His256 -->Ala substitution had only minor effects. This suggests that Lys199 is important for the tight binding of non-peptide antagonists...
  4. ncbi Tight binding of the angiotensin AT(1) receptor antagonist
    F L Fierensa
    Department of Molecular and Biochemical Pharmacology, Institute for Molecular Biology, Free University of Brussels, Paardenstraat 65, B 1640, Sint Genesius Rode, Belgium
    Biochem Pharmacol 61:1227-35. 2001
    ..Insurmountable antagonism of candesartan is therefore independent from receptor internalization via clathrin-coated pits...
  5. ncbi The effects of candesartan on human AT1 receptor-expressing Chinese hamster ovary cells
    G Vauquelin
    Department of Molecular and Biochemical Pharmacology, Institute of Molecular Biology, Free University of Brussels VUB, Sint Genesius Rode, Belgium
    J Am Soc Nephrol 10:S15-7. 1999
    ..The insurmountable effect of candesartan can therefore be ascribed to its long-lasting inhibition of the AT1 receptor...
  6. ncbi Reversible and syntopic interaction between angiotensin receptor antagonists on Chinese hamster ovary cells expressing human angiotensin II type 1 receptors
    P M Vanderheyden
    Department of Molecular Pharmacology, Free University of Brussels, Sint Genesius Rode, Belgium
    Biochem Pharmacol 59:927-35. 2000
    ..In addition, similar kinetic data were obtained from the slowing of the [(3)H]candesartan association rate to antagonist preincubated cells...
  7. ncbi Interaction between the partially insurmountable antagonist valsartan and human recombinant angiotensin II type 1 receptors
    I Verheijen
    Department of Molecular and Biochemical Pharmacology, Free University of Brussels, Belgium
    Fundam Clin Pharmacol 14:577-85. 2000
    ..These kinetic data suggest that the insurmountable inhibition by valsartan is related to its relatively slow dissociation from the human AT1 receptors...
  8. ncbi A two-state receptor model for the interaction between angiotensin II type 1 receptors and non-peptide antagonists
    G Vauquelin
    Department of Molecular and Biochemical Pharmacology, Free University of Brussels VUB, Sint Genesius Rode, Belgium
    Biochem Pharmacol 61:277-84. 2001
    ..In conclusion, these findings provide further support for the concept that insurmountable and surmountable AT1 antagonists are mutually competitive and that insurmountable antagonist-receptor complexes may adopt different states...
  9. ncbi Angiotensin II type 1 receptor antagonists. Why do some of them produce insurmountable inhibition?
    P M Vanderheyden
    Department of Molecular and Biochemical Pharmacology, Free University of Brussels, Sint Genesius Rode, Belgium
    Biochem Pharmacol 60:1557-63. 2000
    ..In addition to the relatively slow dissociation of candesartan, reassociation to the receptor, which is measurable in CHO-AT(1) cells, likely contributes to its long-lasting blood pressure lowering effect in vivo...
  10. pmc Distinction between surmountable and insurmountable selective AT1 receptor antagonists by use of CHO-K1 cells expressing human angiotensin II AT1 receptors
    P M Vanderheyden
    Department of Protein Chemistry, Free University of Brussels VUB, Sint Genesius Rode, Belgium
    Br J Pharmacol 126:1057-65. 1999
    ....
  11. ncbi Binding characteristics of [(3)H]-irbesartan to human recombinant angiotensin type 1 receptors
    P M Vanderheyden
    Department of Molecular and Biochemical Pharmacology, Free University of Brussels, Rode, B 1640, Belgium
    J Renin Angiotensin Aldosterone Syst 1:159-65. 2000
    ..In contrast, other phenomena such as the plasma half life and tissue-related factors are necessary to explain its sustained in vivo antihypertensive effect...
  12. ncbi Inhibition of angiotensin II-induced inositol phosphate production by triacid nonpeptide antagonists in CHO cells expressing human AT1 receptors
    P M Vanderheyden
    Department of Molecular and Biochemical Pharmacology, Institute of Molecular Biology and Biotechnology, Free University of Brussels, Sint Genesius Rode, Belgium
    Pharm Res 17:1482-8. 2000
    ..The aim of the present work is to describe the inhibitory properties of LY301875 and LY303336, two polysubstituted 4-aminoimidazole AT1 receptor antagonists, on CHO cells expressing human recombinant AT1 receptors...