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Title 

Structural insight into the constitutive repression function of the nuclear receptor Rev-erbβ

Authors 

Eui-jeon WooDae Gwin JeongM Y LimSeung Jun KimK J KimSei Mee YoonByoung Chul ParkSeong Eon Ryu

Publisher 

Elsevier

Issue Date 

2007

Citation 

Journal of Molecular Biology, vol. 373, no. 3, pp. 735-744

Keywords 

constitutive repressioncrystal structureligand binding domainorphan receptorRev-erbβcell nucleus receptorcell nucleus receptor rev erb betaprotein functionreceptors, cytoplasmic and nuclear

Abstract 

The Rev-erb family is an orphan nuclear receptor acting as a negative regulator of transcription. Rev-erbα and Rev-erbβ are crucial components of the circadian clock and involved in various lipid homeostasis. They are unique nuclear receptors that lack the activation function 2 helix (AF2-helix) required for ligand-dependent activation by other members of nuclear receptors. Here, we report the crystal structure of Rev-erbβ (NR1D2) in a dimeric arrangement. The putative ligand-binding pocket (LBP) of Rev-erbβ is filled with bulky hydrophobic residues resulting in a residual cavity size that is too small to allow binding of any known ligand molecules. However, an alternative conformation of the putative LBP observed in another crystal form suggests the flexibility of this region. The kinked conformation of helix H11 allows helix H11 to bend toward helix H3 over the putative ligand binding pocket by filling and closing the cavity with its side-chains. In the absence of the AF2-helix and a cognate ligand, Rev-erbβ appears to stabilize the hydrophobic cluster in the putative ligand binding pocket and provide a structural platform for co-repressor binding by adopting the unique geometry of helix H11, a suitable conformation for the constitutive repression activity.

ISSN 

0022-2836

Link 

http://dx.doi.org/10.1016/j.jmb.2007.08.037

Appears in Collections

1. Journal Articles > Journal Articles

Registered Date

2019-05-02


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