Wu Xinle, Lemon Bryan, Li XiaoFan, Gupte Jamila, Weiszmann Jennifer, Stevens Jennitte, Hawkins Nessa, Shen Wenyan, Lindberg Richard, Chen Jin-Long, Tian Hui, Li Yang
Amgen Inc., South San Francisco, California 94080, USA.
J Biol Chem. 2008 Nov 28;283(48):33304-9. doi: 10.1074/jbc.M803319200. Epub 2008 Oct 1.
FGF19 subfamily proteins (FGF19, FGF21, and FGF23) are unique members of fibroblast growth factors (FGFs) that regulate energy, bile acid, glucose, lipid, phosphate, and vitamin D homeostasis in an endocrine fashion. Their activities require the presence of alpha or betaKlotho, two related single-pass transmembrane proteins, as co-receptors in relevant target tissues. We previously showed that FGF19 can bind to both alpha and betaKlotho, whereas FGF21 and FGF23 can bind only to either betaKlotho or alphaKlotho, respectively in vitro. To determine the mechanism regulating the binding and specificity among FGF19 subfamily members to Klotho family proteins, chimeric proteins between FGF19 subfamily members or chimeric proteins between Klotho family members were constructed to probe the interaction between those two families. Our results showed that a chimera of FGF19 with the FGF21 C-terminal tail interacts only with betaKlotho and a chimera with the FGF23 C-terminal tail interacts only with alphaKlotho. FGF signaling assays also reflected the change of specificity we observed for the chimeras. These results identified the C-terminal tail of FGF19 as a region necessary for its recognition of Klotho family proteins. In addition, chimeras between alpha and betaKlotho were also generated to probe the regions in Klotho proteins that are important for signaling by this FGF subfamily. Both FGF23 and FGF21 require intact alpha or betaKlotho for signaling, respectively, whereas FGF19 can signal through a Klotho chimera consisting of the N terminus of alphaKlotho and the C terminus of betaKlotho. Our results provide the first glimpse of the regions that regulate the binding specificity between this unique family of FGFs and their co-receptors.
成纤维细胞生长因子19亚家族蛋白(FGF19、FGF21和FGF23)是成纤维细胞生长因子(FGFs)中的独特成员,它们以内分泌方式调节能量、胆汁酸、葡萄糖、脂质、磷酸盐和维生素D的稳态。它们的活性需要α-或β-klotho这两种相关的单次跨膜蛋白作为相关靶组织中的共受体。我们之前表明,FGF19可以与α-和β-klotho结合,而FGF21和FGF23在体外分别只能与β-klotho或α-klotho结合。为了确定调节FGF19亚家族成员与klotho家族蛋白之间结合和特异性的机制,构建了FGF19亚家族成员之间的嵌合蛋白或klotho家族成员之间的嵌合蛋白,以探究这两个家族之间的相互作用。我们的结果表明,FGF19与FGF21 C末端尾巴的嵌合体仅与β-klotho相互作用,与FGF23 C末端尾巴的嵌合体仅与α-klotho相互作用。FGF信号测定也反映了我们观察到的嵌合体特异性的变化。这些结果确定FGF19的C末端尾巴是其识别klotho家族蛋白所必需的区域。此外,还生成了α-和β-klotho之间的嵌合体,以探究klotho蛋白中对该FGF亚家族信号传导重要的区域。FGF23和FGF21分别需要完整的α-或β-klotho进行信号传导,而FGF19可以通过由α-klotho的N末端和β-klotho的C末端组成的klotho嵌合体进行信号传导。我们的结果首次揭示了调节这一独特FGF家族与其共受体之间结合特异性的区域。