1t5z: Difference between revisions
New page: left|200px<br /> <applet load="1t5z" size="450" color="white" frame="true" align="right" spinBox="true" caption="1t5z, resolution 2.3Å" /> '''Crystal Structure of... |
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[[Image:1t5z.gif|left|200px]]<br /> | [[Image:1t5z.gif|left|200px]]<br /><applet load="1t5z" size="350" color="white" frame="true" align="right" spinBox="true" | ||
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caption="1t5z, resolution 2.3Å" /> | caption="1t5z, resolution 2.3Å" /> | ||
'''Crystal Structure of the Androgen Receptor Ligand Binding Domain (LBD) with DHT and a peptide derived from its physiological coactivator ARA70'''<br /> | '''Crystal Structure of the Androgen Receptor Ligand Binding Domain (LBD) with DHT and a peptide derived from its physiological coactivator ARA70'''<br /> | ||
==Overview== | ==Overview== | ||
Androgens drive sex differentiation, bone and muscle development, and | Androgens drive sex differentiation, bone and muscle development, and promote growth of hormone-dependent cancers by binding the nuclear androgen receptor (AR), which recruits coactivators to responsive genes. Most nuclear receptors recruit steroid receptor coactivators (SRCs) to their ligand binding domain (LBD) using a leucine-rich motif (LXXLL). AR is believed to recruit unique coactivators to its LBD using an aromatic-rich motif (FXXLF) while recruiting SRCs to its N-terminal domain (NTD) through an alternate mechanism. Here, we report that the AR-LBD interacts with both FXXLF motifs and a subset of LXXLL motifs and that contacts with these LXXLL motifs are both necessary and sufficient for SRC-mediated AR regulation of transcription. Crystal structures of the activated AR in complex with both recruitment motifs reveal that side chains unique to the AR-LBD rearrange to bind either the bulky FXXLF motifs or the more compact LXXLL motifs and that AR utilizes subsidiary contacts with LXXLL flanking sequences to discriminate between LXXLL motifs. | ||
==Disease== | ==Disease== | ||
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==About this Structure== | ==About this Structure== | ||
1T5Z is a [http://en.wikipedia.org/wiki/Protein_complex Protein complex] structure of sequences from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] with DHT as [http://en.wikipedia.org/wiki/ligand ligand]. Full crystallographic information is available from [http:// | 1T5Z is a [http://en.wikipedia.org/wiki/Protein_complex Protein complex] structure of sequences from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] with <scene name='pdbligand=DHT:'>DHT</scene> as [http://en.wikipedia.org/wiki/ligand ligand]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1T5Z OCA]. | ||
==Reference== | ==Reference== | ||
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[[Category: Homo sapiens]] | [[Category: Homo sapiens]] | ||
[[Category: Protein complex]] | [[Category: Protein complex]] | ||
[[Category: Baxter, J | [[Category: Baxter, J D.]] | ||
[[Category: Delgado-Rodrigues, E.]] | [[Category: Delgado-Rodrigues, E.]] | ||
[[Category: Estebanez-Perpina, E.]] | [[Category: Estebanez-Perpina, E.]] | ||
[[Category: Fletterick, R | [[Category: Fletterick, R J.]] | ||
[[Category: Guy, R | [[Category: Guy, R K.]] | ||
[[Category: Mar, E.]] | [[Category: Mar, E.]] | ||
[[Category: Moore, J | [[Category: Moore, J M.R.]] | ||
[[Category: Nguyen, P.]] | [[Category: Nguyen, P.]] | ||
[[Category: Webb, P.]] | [[Category: Webb, P.]] | ||
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[[Category: androgen receptor ligand binding domain ara70 crystal structure coactivators]] | [[Category: androgen receptor ligand binding domain ara70 crystal structure coactivators]] | ||
''Page seeded by [http:// | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 15:10:12 2008'' | ||
