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image/svg+xml Jakob Voss, based on art designer at PLoS, modified by Wikipedia users Nina and Beao Closed Access logo, derived from PLoS Open Access logo. This version with transparent background. http://commons.wikimedia.org/wiki/File:Closed_Access_logo_transparent.svg Jakob Voss, based on art designer at PLoS, modified by Wikipedia users Nina and Beao Nature Structural & ...arrow_drop_down
image/svg+xml Jakob Voss, based on art designer at PLoS, modified by Wikipedia users Nina and Beao Closed Access logo, derived from PLoS Open Access logo. This version with transparent background. http://commons.wikimedia.org/wiki/File:Closed_Access_logo_transparent.svg Jakob Voss, based on art designer at PLoS, modified by Wikipedia users Nina and Beao
Nature Structural & Molecular Biology
Article . 2005 . Peer-reviewed
License: Springer TDM
Data sources: Crossref
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Modulation of human nuclear receptor LRH-1 activity by phospholipids and SHP

Authors: Eric A, Ortlund; Yoonkwang, Lee; Isaac H, Solomon; Janet M, Hager; Rachid, Safi; Yunhee, Choi; Ziqiang, Guan; +5 Authors

Modulation of human nuclear receptor LRH-1 activity by phospholipids and SHP

Abstract

The human nuclear receptor liver receptor homolog 1 (hLRH-1) plays an important role in the development of breast carcinomas. This orphan receptor is efficiently downregulated by the unusual co-repressor SHP and has been thought to be ligand-independent. We present the crystal structure at a resolution of 1.9 A of the ligand-binding domain of hLRH-1 in complex with the NR box 1 motif of human SHP, which we find contacts the AF-2 region of hLRH-1 using selective structural motifs. Electron density indicates phospholipid bound within the ligand-binding pocket, which we confirm using mass spectrometry of solvent-extracted samples. We further show that pocket mutations reduce phospholipid binding and receptor activity in vivo. Our results indicate that hLRH-1's control of gene expression is mediated by phospholipid binding, and establish hLRH-1 as a novel target for compounds designed to slow breast cancer development.

Keywords

Models, Molecular, Spectrometry, Mass, Electrospray Ionization, Binding Sites, Molecular Sequence Data, Receptors, Cytoplasmic and Nuclear, Crystallography, X-Ray, Protein Structure, Tertiary, DNA-Binding Proteins, Gene Expression Regulation, Humans, Amino Acid Sequence, Sequence Alignment, Phospholipids, HeLa Cells, Protein Binding, Transcription Factors

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    193
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Powered by OpenAIRE graph
citations
This is an alternative to the "Influence" indicator, which also reflects the overall/total impact of an article in the research community at large, based on the underlying citation network (diachronically).
BIP!Citations provided by BIP!
popularity
This indicator reflects the "current" impact/attention (the "hype") of an article in the research community at large, based on the underlying citation network.
BIP!Popularity provided by BIP!
influence
This indicator reflects the overall/total impact of an article in the research community at large, based on the underlying citation network (diachronically).
BIP!Influence provided by BIP!
impulse
This indicator reflects the initial momentum of an article directly after its publication, based on the underlying citation network.
BIP!Impulse provided by BIP!
193
Top 10%
Top 10%
Top 1%