Contrasting effects of prenyltransferase inhibitors on estrogen-dependent cell cycle progression and estrogen receptor-mediated transcriptional activity in MCF-7 cells
Identifieur interne : 00B235 ( Main/Exploration ); précédent : 00B234; suivant : 00B236Contrasting effects of prenyltransferase inhibitors on estrogen-dependent cell cycle progression and estrogen receptor-mediated transcriptional activity in MCF-7 cells
Auteurs : Sophie F. Doisneau-Sixou [France, Australie] ; Philippe Cestac [France] ; Sarah Chouini [France] ; Jason S. Carroll [France, Australie] ; Andrew D. Hamilton [États-Unis] ; Said M. Sebti [États-Unis] ; Marc Poirot [France] ; Patrick Balaguer [France] ; Jean-Charles Faye [France] ; Robert L. Sutherland [Australie] ; Gilles Favre [France]Source :
- Endocrinology : (Philadelphia) [ 0013-7227 ] ; 2003.
Abstract
Activation of estrogen receptors (ERs) by estrogens triggers both ER nuclear transcriptional activity and Src/Ras/Erks pathway-dependent mitogenic activity. The present study implicates prenylated proteins in both estrogenic actions. The farnesyltransferase and geranylgeranyltransferase I inhibitors (FTI-277 and GGTI-298, respectively) antagonize estradiol-stimulated cell cycle progression, progesterone receptor, cyclin D1, and c-Myc expression. In contrast, the inhibitors markedly stimulate transcription from two genes containing estrogen response elements, both in the absence and presence of estradiol. The pure antiestrogen ICI 182,780 inhibits by more than 85% these effects on transcription. We demonstrate that both FTI-277 and GGTI-298 increase the association of steroid receptor coactivator-1 with ERa and FTI-277 decreases the association of ERa with the histone deacetylase 1, a known transcriptional repressor. In addition, FTI-277 has no marked effect on the association of the two corepressors, nuclear receptor corepressor and silencing mediator of retinoid and thyroid receptor with ERa, whereas GGTI-298, similar to tamoxifen, clearly increased these associations. Together, these results demonstrate that prenylated proteins play a role in estradiol stimulation of proliferation and progesterone receptor expression. However, they antagonize the ability of ERa to stimulate estrogen response element-dependent transcriptional activity, acting presumably through coregulator complex formation.
Affiliations:
- Australie, France, États-Unis
- Floride, Languedoc-Roussillon, Midi-Pyrénées, Occitanie (région administrative)
- Montpellier, Tampa, Toulouse
- Université de Floride du Sud
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Carroll</name><affiliation wicri:level="1"><inist:fA14 i1="01"><s1>Département "Innovation Thérapeutique et Oncologie Moléculaire", Centre de Physiopathologie de Toulouse Purpan, Institut National de la Santé et de la Recherche Médicale U563, and Institut Claudius Regaud</s1><s2>31052 Toulouse</s2><s3>FRA</s3><sZ>1 aut.</sZ><sZ>2 aut.</sZ><sZ>3 aut.</sZ><sZ>4 aut.</sZ><sZ>7 aut.</sZ><sZ>9 aut.</sZ><sZ>11 aut.</sZ></inist:fA14><country>France</country><wicri:noRegion>31052 Toulouse</wicri:noRegion><placeName><settlement type="city">Toulouse</settlement><region type="region" nuts="2">Occitanie (région administrative)</region><region type="old region" nuts="2">Midi-Pyrénées</region></placeName></affiliation><affiliation wicri:level="1"><inist:fA14 i1="02"><s1>Cancer Research Program, Garvan Institute of Medical Research, St. Vincent's Hospital, Darlinghurst</s1><s2>Sydney, New South Wales 2010</s2><s3>AUS</s3><sZ>1 aut.</sZ><sZ>4 aut.</sZ><sZ>10 aut.</sZ></inist:fA14><country>Australie</country><wicri:noRegion>Sydney, New South Wales 2010</wicri:noRegion></affiliation></author><author><name sortKey="Hamilton, Andrew D" sort="Hamilton, Andrew D" uniqKey="Hamilton A" first="Andrew D." last="Hamilton">Andrew D. Hamilton</name><affiliation wicri:level="1"><inist:fA14 i1="03"><s1>Department of Chemistry, Yale University</s1><s2>New Haven, Connecticut 06511</s2><s3>USA</s3><sZ>5 aut.</sZ></inist:fA14><country>États-Unis</country><wicri:noRegion>New Haven, Connecticut 06511</wicri:noRegion></affiliation></author><author><name sortKey="Sebti, Said M" sort="Sebti, Said M" uniqKey="Sebti S" first="Said M." last="Sebti">Said M. Sebti</name><affiliation wicri:level="4"><inist:fA14 i1="04"><s1>Drug Discovery Program, H. Lee Moffitt Cancer Center and Research Institute and Department of Biochemistry and Molecular Biology, University of South Florida</s1><s2>Tampa, Florida 33612</s2><s3>USA</s3><sZ>6 aut.</sZ></inist:fA14><country>États-Unis</country><placeName><settlement type="city">Tampa</settlement><region type="state">Floride</region></placeName><orgName type="university">Université de Floride du Sud</orgName></affiliation></author><author><name sortKey="Poirot, Marc" sort="Poirot, Marc" uniqKey="Poirot M" first="Marc" last="Poirot">Marc Poirot</name><affiliation wicri:level="3"><inist:fA14 i1="01"><s1>Département "Innovation Thérapeutique et Oncologie Moléculaire", Centre de Physiopathologie de Toulouse Purpan, Institut National de la Santé et de la Recherche Médicale U563, and Institut Claudius Regaud</s1><s2>31052 Toulouse</s2><s3>FRA</s3><sZ>1 aut.</sZ><sZ>2 aut.</sZ><sZ>3 aut.</sZ><sZ>4 aut.</sZ><sZ>7 aut.</sZ><sZ>9 aut.</sZ><sZ>11 aut.</sZ></inist:fA14><country>France</country><placeName><region type="region" nuts="2">Occitanie (région administrative)</region><region type="old region" nuts="2">Midi-Pyrénées</region><settlement type="city">Toulouse</settlement></placeName></affiliation></author><author><name sortKey="Balaguer, Patrick" sort="Balaguer, Patrick" uniqKey="Balaguer P" first="Patrick" last="Balaguer">Patrick Balaguer</name><affiliation wicri:level="3"><inist:fA14 i1="05"><s1>Institut National de la Santé et de la Recherche Médicale 439, Pathologie Moléculaire des Récepteurs Nucléaires</s1><s2>34090 Montpellier</s2><s3>FRA</s3><sZ>8 aut.</sZ></inist:fA14><country>France</country><placeName><region type="region" nuts="2">Occitanie (région administrative)</region><region type="old region" nuts="2">Languedoc-Roussillon</region><settlement type="city">Montpellier</settlement></placeName></affiliation></author><author><name sortKey="Faye, Jean Charles" sort="Faye, Jean Charles" uniqKey="Faye J" first="Jean-Charles" last="Faye">Jean-Charles Faye</name><affiliation wicri:level="3"><inist:fA14 i1="01"><s1>Département "Innovation Thérapeutique et Oncologie Moléculaire", Centre de Physiopathologie de Toulouse Purpan, Institut National de la Santé et de la Recherche Médicale U563, and Institut Claudius Regaud</s1><s2>31052 Toulouse</s2><s3>FRA</s3><sZ>1 aut.</sZ><sZ>2 aut.</sZ><sZ>3 aut.</sZ><sZ>4 aut.</sZ><sZ>7 aut.</sZ><sZ>9 aut.</sZ><sZ>11 aut.</sZ></inist:fA14><country>France</country><placeName><region type="region" nuts="2">Occitanie (région administrative)</region><region type="old region" nuts="2">Midi-Pyrénées</region><settlement type="city">Toulouse</settlement></placeName></affiliation></author><author><name sortKey="Sutherland, Robert L" sort="Sutherland, Robert L" uniqKey="Sutherland R" first="Robert L." last="Sutherland">Robert L. 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Doisneau-Sixou</name><affiliation wicri:level="3"><inist:fA14 i1="01"><s1>Département "Innovation Thérapeutique et Oncologie Moléculaire", Centre de Physiopathologie de Toulouse Purpan, Institut National de la Santé et de la Recherche Médicale U563, and Institut Claudius Regaud</s1><s2>31052 Toulouse</s2><s3>FRA</s3><sZ>1 aut.</sZ><sZ>2 aut.</sZ><sZ>3 aut.</sZ><sZ>4 aut.</sZ><sZ>7 aut.</sZ><sZ>9 aut.</sZ><sZ>11 aut.</sZ></inist:fA14><country>France</country><placeName><region type="region" nuts="2">Occitanie (région administrative)</region><region type="old region" nuts="2">Midi-Pyrénées</region><settlement type="city">Toulouse</settlement></placeName></affiliation><affiliation wicri:level="1"><inist:fA14 i1="02"><s1>Cancer Research Program, Garvan Institute of Medical Research, St. Vincent's Hospital, Darlinghurst</s1><s2>Sydney, New South Wales 2010</s2><s3>AUS</s3><sZ>1 aut.</sZ><sZ>4 aut.</sZ><sZ>10 aut.</sZ></inist:fA14><country>Australie</country><wicri:noRegion>Sydney, New South Wales 2010</wicri:noRegion></affiliation></author><author><name sortKey="Cestac, Philippe" sort="Cestac, Philippe" uniqKey="Cestac P" first="Philippe" last="Cestac">Philippe Cestac</name><affiliation wicri:level="1"><inist:fA14 i1="01"><s1>Département "Innovation Thérapeutique et Oncologie Moléculaire", Centre de Physiopathologie de Toulouse Purpan, Institut National de la Santé et de la Recherche Médicale U563, and Institut Claudius Regaud</s1><s2>31052 Toulouse</s2><s3>FRA</s3><sZ>1 aut.</sZ><sZ>2 aut.</sZ><sZ>3 aut.</sZ><sZ>4 aut.</sZ><sZ>7 aut.</sZ><sZ>9 aut.</sZ><sZ>11 aut.</sZ></inist:fA14><country>France</country><wicri:noRegion>31052 Toulouse</wicri:noRegion><placeName><settlement type="city">Toulouse</settlement><region type="region" nuts="2">Occitanie (région administrative)</region><region type="old region" nuts="2">Midi-Pyrénées</region></placeName></affiliation></author><author><name sortKey="Chouini, Sarah" sort="Chouini, Sarah" uniqKey="Chouini S" first="Sarah" last="Chouini">Sarah Chouini</name><affiliation wicri:level="1"><inist:fA14 i1="01"><s1>Département "Innovation Thérapeutique et Oncologie Moléculaire", Centre de Physiopathologie de Toulouse Purpan, Institut National de la Santé et de la Recherche Médicale U563, and Institut Claudius Regaud</s1><s2>31052 Toulouse</s2><s3>FRA</s3><sZ>1 aut.</sZ><sZ>2 aut.</sZ><sZ>3 aut.</sZ><sZ>4 aut.</sZ><sZ>7 aut.</sZ><sZ>9 aut.</sZ><sZ>11 aut.</sZ></inist:fA14><country>France</country><wicri:noRegion>31052 Toulouse</wicri:noRegion><placeName><settlement type="city">Toulouse</settlement><region type="region" nuts="2">Occitanie (région administrative)</region><region type="old region" nuts="2">Midi-Pyrénées</region></placeName></affiliation></author><author><name sortKey="Carroll, Jason S" sort="Carroll, Jason S" uniqKey="Carroll J" first="Jason S." last="Carroll">Jason S. Carroll</name><affiliation wicri:level="1"><inist:fA14 i1="01"><s1>Département "Innovation Thérapeutique et Oncologie Moléculaire", Centre de Physiopathologie de Toulouse Purpan, Institut National de la Santé et de la Recherche Médicale U563, and Institut Claudius Regaud</s1><s2>31052 Toulouse</s2><s3>FRA</s3><sZ>1 aut.</sZ><sZ>2 aut.</sZ><sZ>3 aut.</sZ><sZ>4 aut.</sZ><sZ>7 aut.</sZ><sZ>9 aut.</sZ><sZ>11 aut.</sZ></inist:fA14><country>France</country><wicri:noRegion>31052 Toulouse</wicri:noRegion><placeName><settlement type="city">Toulouse</settlement><region type="region" nuts="2">Occitanie (région administrative)</region><region type="old region" nuts="2">Midi-Pyrénées</region></placeName></affiliation><affiliation wicri:level="1"><inist:fA14 i1="02"><s1>Cancer Research Program, Garvan Institute of Medical Research, St. Vincent's Hospital, Darlinghurst</s1><s2>Sydney, New South Wales 2010</s2><s3>AUS</s3><sZ>1 aut.</sZ><sZ>4 aut.</sZ><sZ>10 aut.</sZ></inist:fA14><country>Australie</country><wicri:noRegion>Sydney, New South Wales 2010</wicri:noRegion></affiliation></author><author><name sortKey="Hamilton, Andrew D" sort="Hamilton, Andrew D" uniqKey="Hamilton A" first="Andrew D." last="Hamilton">Andrew D. Hamilton</name><affiliation wicri:level="1"><inist:fA14 i1="03"><s1>Department of Chemistry, Yale University</s1><s2>New Haven, Connecticut 06511</s2><s3>USA</s3><sZ>5 aut.</sZ></inist:fA14><country>États-Unis</country><wicri:noRegion>New Haven, Connecticut 06511</wicri:noRegion></affiliation></author><author><name sortKey="Sebti, Said M" sort="Sebti, Said M" uniqKey="Sebti S" first="Said M." last="Sebti">Said M. Sebti</name><affiliation wicri:level="4"><inist:fA14 i1="04"><s1>Drug Discovery Program, H. Lee Moffitt Cancer Center and Research Institute and Department of Biochemistry and Molecular Biology, University of South Florida</s1><s2>Tampa, Florida 33612</s2><s3>USA</s3><sZ>6 aut.</sZ></inist:fA14><country>États-Unis</country><placeName><settlement type="city">Tampa</settlement><region type="state">Floride</region></placeName><orgName type="university">Université de Floride du Sud</orgName></affiliation></author><author><name sortKey="Poirot, Marc" sort="Poirot, Marc" uniqKey="Poirot M" first="Marc" last="Poirot">Marc Poirot</name><affiliation wicri:level="3"><inist:fA14 i1="01"><s1>Département "Innovation Thérapeutique et Oncologie Moléculaire", Centre de Physiopathologie de Toulouse Purpan, Institut National de la Santé et de la Recherche Médicale U563, and Institut Claudius Regaud</s1><s2>31052 Toulouse</s2><s3>FRA</s3><sZ>1 aut.</sZ><sZ>2 aut.</sZ><sZ>3 aut.</sZ><sZ>4 aut.</sZ><sZ>7 aut.</sZ><sZ>9 aut.</sZ><sZ>11 aut.</sZ></inist:fA14><country>France</country><placeName><region type="region" nuts="2">Occitanie (région administrative)</region><region type="old region" nuts="2">Midi-Pyrénées</region><settlement type="city">Toulouse</settlement></placeName></affiliation></author><author><name sortKey="Balaguer, Patrick" sort="Balaguer, Patrick" uniqKey="Balaguer P" first="Patrick" last="Balaguer">Patrick Balaguer</name><affiliation wicri:level="3"><inist:fA14 i1="05"><s1>Institut National de la Santé et de la Recherche Médicale 439, Pathologie Moléculaire des Récepteurs Nucléaires</s1><s2>34090 Montpellier</s2><s3>FRA</s3><sZ>8 aut.</sZ></inist:fA14><country>France</country><placeName><region type="region" nuts="2">Occitanie (région administrative)</region><region type="old region" nuts="2">Languedoc-Roussillon</region><settlement type="city">Montpellier</settlement></placeName></affiliation></author><author><name sortKey="Faye, Jean Charles" sort="Faye, Jean Charles" uniqKey="Faye J" first="Jean-Charles" last="Faye">Jean-Charles Faye</name><affiliation wicri:level="3"><inist:fA14 i1="01"><s1>Département "Innovation Thérapeutique et Oncologie Moléculaire", Centre de Physiopathologie de Toulouse Purpan, Institut National de la Santé et de la Recherche Médicale U563, and Institut Claudius Regaud</s1><s2>31052 Toulouse</s2><s3>FRA</s3><sZ>1 aut.</sZ><sZ>2 aut.</sZ><sZ>3 aut.</sZ><sZ>4 aut.</sZ><sZ>7 aut.</sZ><sZ>9 aut.</sZ><sZ>11 aut.</sZ></inist:fA14><country>France</country><placeName><region type="region" nuts="2">Occitanie (région administrative)</region><region type="old region" nuts="2">Midi-Pyrénées</region><settlement type="city">Toulouse</settlement></placeName></affiliation></author><author><name sortKey="Sutherland, Robert L" sort="Sutherland, Robert L" uniqKey="Sutherland R" first="Robert L." last="Sutherland">Robert L. Sutherland</name><affiliation wicri:level="1"><inist:fA14 i1="02"><s1>Cancer Research Program, Garvan Institute of Medical Research, St. Vincent's Hospital, Darlinghurst</s1><s2>Sydney, New South Wales 2010</s2><s3>AUS</s3><sZ>1 aut.</sZ><sZ>4 aut.</sZ><sZ>10 aut.</sZ></inist:fA14><country>Australie</country><wicri:noRegion>Sydney, New South Wales 2010</wicri:noRegion></affiliation></author><author><name sortKey="Favre, Gilles" sort="Favre, Gilles" uniqKey="Favre G" first="Gilles" last="Favre">Gilles Favre</name><affiliation wicri:level="1"><inist:fA14 i1="01"><s1>Département "Innovation Thérapeutique et Oncologie Moléculaire", Centre de Physiopathologie de Toulouse Purpan, Institut National de la Santé et de la Recherche Médicale U563, and Institut Claudius Regaud</s1><s2>31052 Toulouse</s2><s3>FRA</s3><sZ>1 aut.</sZ><sZ>2 aut.</sZ><sZ>3 aut.</sZ><sZ>4 aut.</sZ><sZ>7 aut.</sZ><sZ>9 aut.</sZ><sZ>11 aut.</sZ></inist:fA14><country>France</country><wicri:noRegion>31052 Toulouse</wicri:noRegion><placeName><settlement type="city">Toulouse</settlement><region type="region" nuts="2">Occitanie (région administrative)</region><region type="old region" nuts="2">Midi-Pyrénées</region></placeName></affiliation></author></analytic><series><title level="j" type="main">Endocrinology : (Philadelphia)</title><title level="j" type="abbreviated">Endocrinology : (Phila.)</title><idno type="ISSN">0013-7227</idno><imprint><date when="2003">2003</date></imprint></series></biblStruct></sourceDesc><seriesStmt><title level="j" type="main">Endocrinology : (Philadelphia)</title><title level="j" type="abbreviated">Endocrinology : (Phila.)</title><idno type="ISSN">0013-7227</idno></seriesStmt></fileDesc><profileDesc><textClass></textClass></profileDesc></teiHeader><front><div type="abstract" xml:lang="en">Activation of estrogen receptors (ERs) by estrogens triggers both ER nuclear transcriptional activity and Src/Ras/Erks pathway-dependent mitogenic activity. The present study implicates prenylated proteins in both estrogenic actions. The farnesyltransferase and geranylgeranyltransferase I inhibitors (FTI-277 and GGTI-298, respectively) antagonize estradiol-stimulated cell cycle progression, progesterone receptor, cyclin D1, and c-Myc expression. In contrast, the inhibitors markedly stimulate transcription from two genes containing estrogen response elements, both in the absence and presence of estradiol. The pure antiestrogen ICI 182,780 inhibits by more than 85% these effects on transcription. We demonstrate that both FTI-277 and GGTI-298 increase the association of steroid receptor coactivator-1 with ERa and FTI-277 decreases the association of ERa with the histone deacetylase 1, a known transcriptional repressor. In addition, FTI-277 has no marked effect on the association of the two corepressors, nuclear receptor corepressor and silencing mediator of retinoid and thyroid receptor with ERa, whereas GGTI-298, similar to tamoxifen, clearly increased these associations. Together, these results demonstrate that prenylated proteins play a role in estradiol stimulation of proliferation and progesterone receptor expression. However, they antagonize the ability of ERa to stimulate estrogen response element-dependent transcriptional activity, acting presumably through coregulator complex formation.</div></front></TEI><affiliations><list><country><li>Australie</li><li>France</li><li>États-Unis</li></country><region><li>Floride</li><li>Languedoc-Roussillon</li><li>Midi-Pyrénées</li><li>Occitanie (région administrative)</li></region><settlement><li>Montpellier</li><li>Tampa</li><li>Toulouse</li></settlement><orgName><li>Université de Floride du Sud</li></orgName></list><tree><country name="France"><region name="Occitanie (région administrative)"><name sortKey="Doisneau Sixou, Sophie F" sort="Doisneau Sixou, Sophie F" uniqKey="Doisneau Sixou S" first="Sophie F." last="Doisneau-Sixou">Sophie F. Doisneau-Sixou</name></region><name sortKey="Balaguer, Patrick" sort="Balaguer, Patrick" uniqKey="Balaguer P" first="Patrick" last="Balaguer">Patrick Balaguer</name><name sortKey="Carroll, Jason S" sort="Carroll, Jason S" uniqKey="Carroll J" first="Jason S." last="Carroll">Jason S. Carroll</name><name sortKey="Cestac, Philippe" sort="Cestac, Philippe" uniqKey="Cestac P" first="Philippe" last="Cestac">Philippe Cestac</name><name sortKey="Chouini, Sarah" sort="Chouini, Sarah" uniqKey="Chouini S" first="Sarah" last="Chouini">Sarah Chouini</name><name sortKey="Favre, Gilles" sort="Favre, Gilles" uniqKey="Favre G" first="Gilles" last="Favre">Gilles Favre</name><name sortKey="Faye, Jean Charles" sort="Faye, Jean Charles" uniqKey="Faye J" first="Jean-Charles" last="Faye">Jean-Charles Faye</name><name sortKey="Poirot, Marc" sort="Poirot, Marc" uniqKey="Poirot M" first="Marc" last="Poirot">Marc Poirot</name></country><country name="Australie"><noRegion><name sortKey="Doisneau Sixou, Sophie F" sort="Doisneau Sixou, Sophie F" uniqKey="Doisneau Sixou S" first="Sophie F." last="Doisneau-Sixou">Sophie F. Doisneau-Sixou</name></noRegion><name sortKey="Carroll, Jason S" sort="Carroll, Jason S" uniqKey="Carroll J" first="Jason S." last="Carroll">Jason S. Carroll</name><name sortKey="Sutherland, Robert L" sort="Sutherland, Robert L" uniqKey="Sutherland R" first="Robert L." last="Sutherland">Robert L. Sutherland</name></country><country name="États-Unis"><noRegion><name sortKey="Hamilton, Andrew D" sort="Hamilton, Andrew D" uniqKey="Hamilton A" first="Andrew D." last="Hamilton">Andrew D. Hamilton</name></noRegion><name sortKey="Sebti, Said M" sort="Sebti, Said M" uniqKey="Sebti S" first="Said M." last="Sebti">Said M. Sebti</name></country></tree></affiliations></record>Pour manipuler ce document sous Unix (Dilib)
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|texte= Contrasting effects of prenyltransferase inhibitors on estrogen-dependent cell cycle progression and estrogen receptor-mediated transcriptional activity in MCF-7 cells
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