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LRP6 细胞外结构域及其与 DKK1 复合物的晶体结构。

Crystal structures of the extracellular domain of LRP6 and its complex with DKK1.

机构信息

Department of Biological Structure, University of Washington School of Medicine, Seattle, Washington, USA.

出版信息

Nat Struct Mol Biol. 2011 Oct 9;18(11):1204-10. doi: 10.1038/nsmb.2139.


DOI:10.1038/nsmb.2139
PMID:21984209
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC3249237/
Abstract

Low-density-lipoprotein (LDL) receptor-related proteins 5 and 6 (LRP5/6) are Wnt co-receptors essential for Wnt/β-catenin signaling. Dickkopf 1 (DKK1) inhibits Wnt signaling by interacting with the extracellular domains of LRP5/6 and is a drug target for multiple diseases. Here we present the crystal structures of a human LRP6-E3E4-DKK1 complex and the first and second halves of human LRP6's four propeller-epidermal growth factor (EGF) pairs (LRP6-E1E2 and LRP6-E3E4). Combined with EM analysis, these data demonstrate that LRP6-E1E2 and LRP6-E3E4 form two rigid structural blocks, with a short intervening hinge that restrains their relative orientation. The C-terminal domain of DKK1 (DKK1c) interacts with the top surface of the LRP6-E3 YWTD propeller and given their structural similarity, probably also that of the LRP6-E1 propeller, through conserved hydrophobic patches buttressed by a network of salt bridges and hydrogen bonds. Our work provides key insights for understanding LRP5/6 structure and the interaction of LRP5/6 with DKK, as well as for drug discovery.

摘要

低密度脂蛋白(LDL)受体相关蛋白 5 和 6(LRP5/6)是 Wnt 共受体,对于 Wnt/β-连环蛋白信号通路至关重要。Dickkopf 1(DKK1)通过与 LRP5/6 的细胞外结构域相互作用抑制 Wnt 信号通路,是多种疾病的药物靶点。在这里,我们展示了人 LRP6-E3E4-DKK1 复合物的晶体结构,以及人 LRP6 的四个螺旋桨表皮生长因子(EGF)对的前半部分和后半部分(LRP6-E1E2 和 LRP6-E3E4)的晶体结构。结合 EM 分析,这些数据表明 LRP6-E1E2 和 LRP6-E3E4 形成两个刚性结构块,中间有一个短的铰链,限制了它们的相对取向。DKK1 的 C 端结构域(DKK1c)与 LRP6-E3 YWTD 螺旋桨的顶面相互作用,并且由于它们的结构相似性,可能还与 LRP6-E1 螺旋桨相互作用,通过由盐桥和氢键网络支撑的保守疏水性斑块。我们的工作为理解 LRP5/6 的结构以及 LRP5/6 与 DKK 的相互作用提供了关键的见解,也为药物发现提供了关键的见解。

相似文献

[1]
Crystal structures of the extracellular domain of LRP6 and its complex with DKK1.

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[2]
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[3]
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[6]
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[10]
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本文引用的文献

[1]
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[2]
Wnt isoform-specific interactions with coreceptor specify inhibition or potentiation of signaling by LRP6 antibodies.

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Reconstitution of a frizzled8.Wnt3a.LRP6 signaling complex reveals multiple Wnt and Dkk1 binding sites on LRP6.

J Biol Chem. 2010-1-21

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