2nxx

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{{STRUCTURE_2nxx| PDB=2nxx | SCENE= }}
{{STRUCTURE_2nxx| PDB=2nxx | SCENE= }}
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'''Crystal Structure of the Ligand-Binding Domains of the T.castaneum (Coleoptera) Heterodimer EcrUSP Bound to Ponasterone A'''
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===Crystal Structure of the Ligand-Binding Domains of the T.castaneum (Coleoptera) Heterodimer EcrUSP Bound to Ponasterone A===
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==Overview==
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Retinoid X receptor (RXR) and Ultraspiracle (USP) play a central role as ubiquitous heterodimerization partners of many nuclear receptors. While it has long been accepted that a wide range of ligands can activate vertebrate/mollusc RXRs, the existence and necessity of specific endogenous ligands activating RXR-USP in vivo is still matter of intense debate. Here we report the existence of a novel type of RXR-USP with a ligand-independent functional conformation. Our studies involved Tribolium USP (TcUSP) as representative of most arthropod RXR-USPs, with high sequence homology to vertebrate/mollusc RXRs. The crystal structure of the ligand-binding domain of TcUSP was solved in the context of the functional heterodimer with the ecdysone receptor (EcR). While EcR exhibits a canonical ligand-bound conformation, USP adopts an original apo structure. Our functional data demonstrate that TcUSP is a constitutively silent partner of EcR, and that none of the RXR ligands can bind and activate TcUSP. These findings together with a phylogenetic analysis suggest that RXR-USPs have undergone remarkable functional shifts during evolution and give insight into receptor-ligand binding evolution and dynamics.
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(as it appears on PubMed at http://www.pubmed.gov), where 17673910 is the PubMed ID number.
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{{ABSTRACT_PUBMED_17673910}}
==About this Structure==
==About this Structure==
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[[Category: Hormone receptor]]
[[Category: Hormone receptor]]
[[Category: Hormone/growth factor complex]]
[[Category: Hormone/growth factor complex]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun May 4 10:03:11 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Jul 28 12:58:42 2008''

Revision as of 09:58, 28 July 2008

Template:STRUCTURE 2nxx

Crystal Structure of the Ligand-Binding Domains of the T.castaneum (Coleoptera) Heterodimer EcrUSP Bound to Ponasterone A

Template:ABSTRACT PUBMED 17673910

About this Structure

Full crystallographic information is available from OCA.

Reference

Structural and functional characterization of a novel type of ligand-independent RXR-USP receptor., Iwema T, Billas IM, Beck Y, Bonneton F, Nierengarten H, Chaumot A, Richards G, Laudet V, Moras D, EMBO J. 2007 Aug 22;26(16):3770-82. Epub 2007 Aug 2. PMID:17673910

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