Department of Biological Structure, University of Washington School of Medicine, Seattle, Washington, USA.
Nat Struct Mol Biol. 2011 Oct 9;18(11):1204-10. doi: 10.1038/nsmb.2139.
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.
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。
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