1t65

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{{STRUCTURE_1t65| PDB=1t65 | SCENE= }}
{{STRUCTURE_1t65| PDB=1t65 | SCENE= }}
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'''Crystal structure of the androgen receptor ligand binding domain with DHT and a peptide derived form its physiological coactivator GRIP1 NR box 2 bound in a non-helical conformation'''
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===Crystal structure of the androgen receptor ligand binding domain with DHT and a peptide derived form its physiological coactivator GRIP1 NR box 2 bound in a non-helical conformation===
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==Overview==
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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.
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(as it appears on PubMed at http://www.pubmed.gov), where 15563469 is the PubMed ID number.
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{{ABSTRACT_PUBMED_15563469}}
==About this Structure==
==About this Structure==
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[[Category: Webb, P.]]
[[Category: Webb, P.]]
[[Category: Androgen receptor ligand binding domain grip1 nr box2 coactivators crystal structure non-helical]]
[[Category: Androgen receptor ligand binding domain grip1 nr box2 coactivators crystal structure non-helical]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May 3 09:34:36 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun Jul 27 17:12:19 2008''

Revision as of 14:12, 27 July 2008

Image:1t65.png

Template:STRUCTURE 1t65

Crystal structure of the androgen receptor ligand binding domain with DHT and a peptide derived form its physiological coactivator GRIP1 NR box 2 bound in a non-helical conformation

Template:ABSTRACT PUBMED 15563469

About this Structure

1T65 is a Protein complex structure of sequences from Homo sapiens. Full crystallographic information is available from OCA.

Reference

The molecular mechanisms of coactivator utilization in ligand-dependent transactivation by the androgen receptor., Estebanez-Perpina E, Moore JM, Mar E, Delgado-Rodrigues E, Nguyen P, Baxter JD, Buehrer BM, Webb P, Fletterick RJ, Guy RK, J Biol Chem. 2005 Mar 4;280(9):8060-8. Epub 2004 Nov 24. PMID:15563469

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