Full Text Journal Articles by
Author Anny Cleeren

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Capacity of type I and II ligands to confer to estrogen receptor alpha an appropriate conformation for the recruitment of coactivators containing a LxxLL motif-Relationship with the regulation of receptor level and ERE-dependent transcription in MCF-7 cells.

Sandrine Bourgoin-Voillard, Dominique Gallo, Ioanna Laïos, Anny Cleeren, Latifa El Bali, Yves Jacquot, Denis Nonclercq, Guy Laurent, Jean-Claude Tabet, Guy Leclercq,

Estrogen receptor alpha (ERalpha) belongs to the superfamily of nuclear receptors and as such acts as a ligand-modulated transcription factor. Ligands elicit in ERalpha conformational changes leading to the recruitment of coactivators required for the transactivation of target genes via cognate response elements. In many cells, activated ERalpha also undergoes ... Read more >>

Biochem. Pharmacol. (Biochemical pharmacology)
[2010, 79(5):746-757]

Cited: 13 times

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Effect of fluorination on the pharmacological profile of 11beta isomers of fulvestrant in breast carcinoma cells.

Vangelis Agouridas, Emmanuel Magnier, Jean-Claude Blazejewski, Ioanna Laïos, Anny Cleeren, Denis Nonclercq, Guy Laurent, Guy Leclercq,

We describe the synthesis of an 11beta isomer 3 of the steroidal antiestrogen fulvestrant 2. Partial fluorination of the 11beta side chain in 3 leads to 4, which still shows strong antiproliferative activity on MCF-7 cells. However, unlike 2 and 3, compound 4 fails to down-regulate estrogen receptor alpha (ERalpha). ... Read more >>

J Med Chem (Journal of medicinal chemistry)
[2009, 52(3):883-887]

Cited: 3 times

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Calmodulin-independent, agonistic properties of a peptide containing the calmodulin binding site of estrogen receptor alpha.

Dominique Gallo, Françoise Jacquemotte, Anny Cleeren, Ioanna Laïos, Samira Hadiy, Martin G Rowlands, Olivier Caille, Denis Nonclercq, Guy Laurent, Yves Jacquot, Guy Leclercq,

Calmodulin (CaM) contributes to estrogen receptor alpha (ER)-mediated transcription. In order to study the underlying mechanisms, we synthesized a peptide including the CaM binding site: ERalpha17p (P(295)-T(311)). This peptide inhibited ER-CaM association, unlike two analogs in which two amino acids required for CaM binding were substituted. Exposure of MCF-7 cells ... Read more >>

Mol. Cell. Endocrinol. (Molecular and cellular endocrinology)
[2007, 268(1-2):37-49]

Cited: 13 times

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Fluorous tolerance of the estrogen receptor alpha as probed by 11-polyfluoroalkylestradiol derivatives.

Vangelis Agouridas, Jean-Claude Blazejewski, Anny Cleeren, Ioanna Laïos, Guy Leclercq, Emmanuel Magnier,

The concern of this work was to try to delineate factors, inherent to fluorination, susceptible to influence estradiol binding to the estrogen receptor alpha (ERalpha). For this purpose, fluorinated chains were linked at 11beta position of the steroid (i.e., C(6)F(13), CH(2)CH(2)C(4)F(9), CH(2)CH(2)C(8)F(17)). Relative binding affinity (RBA) for ERalpha of these ... Read more >>

Steroids (Steroids)
[2008, 73(3):320-327]

Cited: 3 times

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Synthesis, structure, and estrogenic activity of 4-amino-3-(2-methylbenzyl)coumarins on human breast carcinoma cells.

Yves Jacquot, Ioanna Laïos, Anny Cleeren, Denis Nonclercq, Laurent Bermont, Bernard Refouvelet, Kamal Boubekeur, Alain Xicluna, Guy Leclercq, Guy Laurent,

A number of coumarins exhibit interesting pharmacological activities and are therefore of therapeutic use. We report here the synthesis and the structural analysis of new N-substituted 4-amino-3-(2-methylbenzyl)coumarins (compounds 8a-8e) that present structural analogies with estrothiazine and 11- or 7-substituted 17beta-estradiol. These derivatives were tested with respect to estrogenic activity on ... Read more >>

Bioorg. Med. Chem. (Bioorganic & medicinal chemistry)
[2007, 15(6):2269-2282]

Cited: 11 times

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Effects of (R,S)/(S,R)-4,5-bis(2-chloro-4-hydroxyphenyl)-2-imidazolines and (R,S)/(S,R)-2,3-bis(2-chloro-4-hydroxyphenyl)piperazines on estrogen receptor alpha level and transcriptional activity in MCF-7 cells.

Ioanna Laïos, Anny Cleeren, Guy Leclercq, Denis Nonclercq, Guy Laurent, Miriam Schlenk, Anja Wellner, Ronald Gust,

4,5-Diaryl-2-imidazolines (Im(s)) and 2,3-diarylpiperazines (Pip(s)) belong to the type II class of estrogens. These compounds enhance ERalpha-mediated transcription of ERE-driven reporter genes in MCF-7 cells but do not compete with [(3)H]estradiol (E(2)) for receptor binding, because of distinct anchoring modes. The present study examined whether the estrogenic action of Im(s) ... Read more >>

Biochem. Pharmacol. (Biochemical pharmacology)
[2007, 74(7):1029-1038]

Cited: 6 times

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Loss of antagonistic activity of tamoxifen by replacement of one N-methyl of its side chain by fluorinated residues.

Vangelis Agouridas, Ioanna Laïos, Anny Cleeren, Elyane Kizilian, Emmanuel Magnier, Jean-Claude Blazejewski, Guy Leclercq,

Efforts to limit the metabolic alteration of the aminoalkyl side chain of tamoxifen by fluorination largely decrease its ER-mediated antagonistic properties in MCF-7 cells (i.e., ability to inhibit growth, to stabilize ER, and to modulate ERE and AP-1 transcriptional activity). This loss is associated with an enhancement of agonistic activity. ... Read more >>

Bioorg Med Chem (Bioorganic & medicinal chemistry)
[2006, 14(22):7531-7538]

Cited: 8 times

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Pharmacological profile of 6,12-dihydro-3-methoxy-1-benzopyrano[3,4-b] [1,4]benzothiazin-6-one, a novel human estrogen receptor agonist.

Yves Jacquot, Anny Cleeren, Ioanna Laios, Ma Yan, Athem Boulahdour, Laurent Bermont, Bernard Refouvelet, Gérard Adessi, Guy Leclercq, Alain Xicluna,

Pharmacological studies were carried out to characterize further the endocrinological profile and the binding mode to the estrogen receptor (ER) of 6,12-dihydro-3-methoxy-1-benzopyrano[3,4-b][1,4]benzothiazin-6-one (1). Binding experiments were conducted with highly purified recombinant human estrogen receptors hERa and beta. Potent estrogenic activity of compound 1 was assessed by testing its ability to ... Read more >>

Biol. Pharm. Bull. (Biological & pharmaceutical bulletin)
[2002, 25(3):335-341]

Cited: 7 times

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Synthesis, characterization and biological evaluation of 7 alpha-perfluoroalkylestradiol derivatives.

Jean-Claude Blazejewski, Martin P Wilmshurst, Matthew D Popkin, Claude Wakselman, Guy Laurent, Denis Nonclercq, Anny Cleeren, Yan Ma, Hye-Sook Seo, Guy Leclercq,

Linkage of a long CH(2 )side chain ('spacer') onto C-7 alpha of estradiol-17 beta (E(2)) does not abrogate the binding affinity of this hormone for its receptor. Our purpose was to assess whether the linkage of a CF(2 )side chain, which is more bulky and rigid, could also be accommodated ... Read more >>

Bioorg Med Chem (Bioorganic & medicinal chemistry)
[2003, 11(3):335-345]

Cited: 9 times

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