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Ligand-specific allosteric regulation of coactivator functions of androgen receptor in prostate cancer cells
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| Zeitschriftentitel: | Proceedings of the National Academy of Sciences |
|---|---|
| Personen und Körperschaften: | , , , , , , , |
| In: | Proceedings of the National Academy of Sciences, 103, 2006, 9, S. 3100-3105 |
| Format: | E-Article |
| Sprache: | Englisch |
| veröffentlicht: |
Proceedings of the National Academy of Sciences
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| Schlagwörter: |
| author_facet |
Baek, Sung Hee Ohgi, Kenneth A. Nelson, Charles A. Welsbie, Derek Chen, Charlie Sawyers, Charles L. Rose, David W. Rosenfeld, Michael G. Baek, Sung Hee Ohgi, Kenneth A. Nelson, Charles A. Welsbie, Derek Chen, Charlie Sawyers, Charles L. Rose, David W. Rosenfeld, Michael G. |
|---|---|
| author |
Baek, Sung Hee Ohgi, Kenneth A. Nelson, Charles A. Welsbie, Derek Chen, Charlie Sawyers, Charles L. Rose, David W. Rosenfeld, Michael G. |
| spellingShingle |
Baek, Sung Hee Ohgi, Kenneth A. Nelson, Charles A. Welsbie, Derek Chen, Charlie Sawyers, Charles L. Rose, David W. Rosenfeld, Michael G. Proceedings of the National Academy of Sciences Ligand-specific allosteric regulation of coactivator functions of androgen receptor in prostate cancer cells Multidisciplinary |
| author_sort |
baek, sung hee |
| spelling |
Baek, Sung Hee Ohgi, Kenneth A. Nelson, Charles A. Welsbie, Derek Chen, Charlie Sawyers, Charles L. Rose, David W. Rosenfeld, Michael G. 0027-8424 1091-6490 Proceedings of the National Academy of Sciences Multidisciplinary http://dx.doi.org/10.1073/pnas.0510842103 <jats:p>The androgen receptor not only mediates prostate development but also serves as a key regulator of primary prostatic cancer growth. Although initially responsive to selective androgen receptor modulators (SARMs), which cause recruitment of the nuclear receptor–corepressor (N-CoR) complex, resistance invariably occurs, perhaps in response to inflammatory signals. Here we report that dismissal of nuclear receptor–corepressor complexes by specific signals or androgen receptor overexpression results in recruitment of many of the cohorts of coactivator complexes that permits SARMs and natural ligands to function as agonists. SARM-bound androgen receptors appear to exhibit failure to recruit specific components of the coactivators generally bound by liganded nuclear receptors, including cAMP response element-binding protein (CBP)/p300 or coactivator-associated arginine methyltransferase 1 (CARM1) to the SARM-bound androgen receptor, although still causing transcriptional activation of androgen receptor target genes. SARM-bound androgen receptors use distinct LXXLL (L, leucine; X, any amino acid) helices in the p160 nuclear receptor interaction domains that may impose selective allosteric effects, providing a component of the molecular basis of differential responses to different classes of ligands by androgen receptor.</jats:p> Ligand-specific allosteric regulation of coactivator functions of androgen receptor in prostate cancer cells Proceedings of the National Academy of Sciences |
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| title |
Ligand-specific allosteric regulation of coactivator functions of androgen receptor in prostate cancer cells |
| title_unstemmed |
Ligand-specific allosteric regulation of coactivator functions of androgen receptor in prostate cancer cells |
| title_full |
Ligand-specific allosteric regulation of coactivator functions of androgen receptor in prostate cancer cells |
| title_fullStr |
Ligand-specific allosteric regulation of coactivator functions of androgen receptor in prostate cancer cells |
| title_full_unstemmed |
Ligand-specific allosteric regulation of coactivator functions of androgen receptor in prostate cancer cells |
| title_short |
Ligand-specific allosteric regulation of coactivator functions of androgen receptor in prostate cancer cells |
| title_sort |
ligand-specific allosteric regulation of coactivator functions of androgen receptor in prostate cancer cells |
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Multidisciplinary |
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http://dx.doi.org/10.1073/pnas.0510842103 |
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2006 |
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3100-3105 |
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<jats:p>The androgen receptor not only mediates prostate development but also serves as a key regulator of primary prostatic cancer growth. Although initially responsive to selective androgen receptor modulators (SARMs), which cause recruitment of the nuclear receptor–corepressor (N-CoR) complex, resistance invariably occurs, perhaps in response to inflammatory signals. Here we report that dismissal of nuclear receptor–corepressor complexes by specific signals or androgen receptor overexpression results in recruitment of many of the cohorts of coactivator complexes that permits SARMs and natural ligands to function as agonists. SARM-bound androgen receptors appear to exhibit failure to recruit specific components of the coactivators generally bound by liganded nuclear receptors, including cAMP response element-binding protein (CBP)/p300 or coactivator-associated arginine methyltransferase 1 (CARM1) to the SARM-bound androgen receptor, although still causing transcriptional activation of androgen receptor target genes. SARM-bound androgen receptors use distinct LXXLL (L, leucine; X, any amino acid) helices in the p160 nuclear receptor interaction domains that may impose selective allosteric effects, providing a component of the molecular basis of differential responses to different classes of ligands by androgen receptor.</jats:p> |
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| author | Baek, Sung Hee, Ohgi, Kenneth A., Nelson, Charles A., Welsbie, Derek, Chen, Charlie, Sawyers, Charles L., Rose, David W., Rosenfeld, Michael G. |
| author_facet | Baek, Sung Hee, Ohgi, Kenneth A., Nelson, Charles A., Welsbie, Derek, Chen, Charlie, Sawyers, Charles L., Rose, David W., Rosenfeld, Michael G., Baek, Sung Hee, Ohgi, Kenneth A., Nelson, Charles A., Welsbie, Derek, Chen, Charlie, Sawyers, Charles L., Rose, David W., Rosenfeld, Michael G. |
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| description | <jats:p>The androgen receptor not only mediates prostate development but also serves as a key regulator of primary prostatic cancer growth. Although initially responsive to selective androgen receptor modulators (SARMs), which cause recruitment of the nuclear receptor–corepressor (N-CoR) complex, resistance invariably occurs, perhaps in response to inflammatory signals. Here we report that dismissal of nuclear receptor–corepressor complexes by specific signals or androgen receptor overexpression results in recruitment of many of the cohorts of coactivator complexes that permits SARMs and natural ligands to function as agonists. SARM-bound androgen receptors appear to exhibit failure to recruit specific components of the coactivators generally bound by liganded nuclear receptors, including cAMP response element-binding protein (CBP)/p300 or coactivator-associated arginine methyltransferase 1 (CARM1) to the SARM-bound androgen receptor, although still causing transcriptional activation of androgen receptor target genes. SARM-bound androgen receptors use distinct LXXLL (L, leucine; X, any amino acid) helices in the p160 nuclear receptor interaction domains that may impose selective allosteric effects, providing a component of the molecular basis of differential responses to different classes of ligands by androgen receptor.</jats:p> |
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| spelling | Baek, Sung Hee Ohgi, Kenneth A. Nelson, Charles A. Welsbie, Derek Chen, Charlie Sawyers, Charles L. Rose, David W. Rosenfeld, Michael G. 0027-8424 1091-6490 Proceedings of the National Academy of Sciences Multidisciplinary http://dx.doi.org/10.1073/pnas.0510842103 <jats:p>The androgen receptor not only mediates prostate development but also serves as a key regulator of primary prostatic cancer growth. Although initially responsive to selective androgen receptor modulators (SARMs), which cause recruitment of the nuclear receptor–corepressor (N-CoR) complex, resistance invariably occurs, perhaps in response to inflammatory signals. Here we report that dismissal of nuclear receptor–corepressor complexes by specific signals or androgen receptor overexpression results in recruitment of many of the cohorts of coactivator complexes that permits SARMs and natural ligands to function as agonists. SARM-bound androgen receptors appear to exhibit failure to recruit specific components of the coactivators generally bound by liganded nuclear receptors, including cAMP response element-binding protein (CBP)/p300 or coactivator-associated arginine methyltransferase 1 (CARM1) to the SARM-bound androgen receptor, although still causing transcriptional activation of androgen receptor target genes. SARM-bound androgen receptors use distinct LXXLL (L, leucine; X, any amino acid) helices in the p160 nuclear receptor interaction domains that may impose selective allosteric effects, providing a component of the molecular basis of differential responses to different classes of ligands by androgen receptor.</jats:p> Ligand-specific allosteric regulation of coactivator functions of androgen receptor in prostate cancer cells Proceedings of the National Academy of Sciences |
| spellingShingle | Baek, Sung Hee, Ohgi, Kenneth A., Nelson, Charles A., Welsbie, Derek, Chen, Charlie, Sawyers, Charles L., Rose, David W., Rosenfeld, Michael G., Proceedings of the National Academy of Sciences, Ligand-specific allosteric regulation of coactivator functions of androgen receptor in prostate cancer cells, Multidisciplinary |
| title | Ligand-specific allosteric regulation of coactivator functions of androgen receptor in prostate cancer cells |
| title_full | Ligand-specific allosteric regulation of coactivator functions of androgen receptor in prostate cancer cells |
| title_fullStr | Ligand-specific allosteric regulation of coactivator functions of androgen receptor in prostate cancer cells |
| title_full_unstemmed | Ligand-specific allosteric regulation of coactivator functions of androgen receptor in prostate cancer cells |
| title_short | Ligand-specific allosteric regulation of coactivator functions of androgen receptor in prostate cancer cells |
| title_sort | ligand-specific allosteric regulation of coactivator functions of androgen receptor in prostate cancer cells |
| title_unstemmed | Ligand-specific allosteric regulation of coactivator functions of androgen receptor in prostate cancer cells |
| topic | Multidisciplinary |
| url | http://dx.doi.org/10.1073/pnas.0510842103 |