趋化因子fractalkine可通过直接结合不同于经典RGD结合位点的配体结合位点,在不依赖CX3CR1的情况下激活整合素。
The chemokine fractalkine can activate integrins without CX3CR1 through direct binding to a ligand-binding site distinct from the classical RGD-binding site.
作者信息
Fujita Masaaki, Takada Yoko K, Takada Yoshikazu
机构信息
Department of Dermatology, Biochemistry and Molecular Medicine, UC Davis School of Medicine, Sacramento, California, United States of America.
出版信息
PLoS One. 2014 May 2;9(5):e96372. doi: 10.1371/journal.pone.0096372. eCollection 2014.
The chemokine domain of fractalkine (FKN-CD) binds to the classical RGD-binding site of αvβ3 and that the resulting ternary complex formation (integrin-FKN-CX3CR1) is critical for CX3CR1 signaling and FKN-induced integrin activation. However, only certain cell types express CX3CR1. Here we studied if FKN-CD can activate integrins in the absence of CX3CR1. We describe that WT FKN-CD activated recombinant soluble αvβ3 in cell-free conditions, but the integrin-binding defective mutant of FKN-CD (K36E/R37E) did not. This suggests that FKN-CD can activate αvβ3 in the absence of CX3CR1 through the direct binding of FKN-CD to αvβ3. WT FKN-CD activated αvβ3 on CX3CR1-negative cells (K562 and CHO) but K36E/R37E did not, suggesting that FKN-CD can activate integrin at the cellular levels in a manner similar to that in cell-free conditions. We hypothesized that FKN-CD enhances ligand binding to the classical RGD-binding site (site 1) through binding to a second binding site (site 2) that is distinct from site 1 in αvβ3. To identify the possible second FKN-CD binding site we performed docking simulation of αvβ3-FKN-CD interaction using αvβ3 with a closed inactive conformation as a target. The simulation predicted a potential FKN-CD-binding site in inactive αvβ3 (site 2), which is located at a crevice between αv and β3 on the opposite side of site 1 in the αvβ3 headpiece. We studied if FKN-CD really binds to site 2 using a peptide that is predicted to interact with FKN-CD in site 2. Notably the peptide specifically bound to FKN-CD and effectively suppressed integrin activation by FKN-CD. This suggests that FKN-CD actually binds to site 2, and this leads to integrin activation. We obtained very similar results in α4β1 and α5β1. The FKN binding to site 2 and resulting integrin activation may be a novel mechanism of integrin activation and of FKN signaling.
趋化因子 fractalkine 的趋化因子结构域(FKN-CD)与 αvβ3 的经典 RGD 结合位点结合,并且由此形成的三元复合物(整合素 - FKN - CX3CR1)对于 CX3CR1 信号传导和 FKN 诱导的整合素激活至关重要。然而,只有某些细胞类型表达 CX3CR1。在此,我们研究了在缺乏 CX3CR1 的情况下 FKN-CD 是否能够激活整合素。我们发现野生型 FKN-CD 在无细胞条件下可激活重组可溶性 αvβ3,但 FKN-CD 的整合素结合缺陷突变体(K36E/R37E)则不能。这表明在缺乏 CX3CR1 的情况下,FKN-CD 可通过其与 αvβ3 的直接结合来激活 αvβ3。野生型 FKN-CD 可激活 CX3CR1 阴性细胞(K562 和 CHO)上的 αvβ3,但 K36E/R37E 则不能,这表明 FKN-CD 在细胞水平上能够以与无细胞条件下类似的方式激活整合素。我们推测 FKN-CD 通过与 αvβ3 中不同于经典 RGD 结合位点(位点 1)的第二个结合位点(位点 2)结合,增强配体与经典 RGD 结合位点(位点 1)的结合。为了确定可能的第二个 FKN-CD 结合位点,我们以处于封闭无活性构象的 αvβ3 为靶点,对 αvβ3 - FKN-CD 相互作用进行了对接模拟。模拟预测在无活性的 αvβ3 中存在一个潜在的 FKN-CD 结合位点(位点 2),其位于 αvβ3 头部结构中位点 1 相对一侧的 αv 和 β3 之间的缝隙处。我们使用一种预计在位点 2 与 FKN-CD 相互作用的肽,研究 FKN-CD 是否真的与位点 2 结合。值得注意的是,该肽特异性结合 FKN-CD,并有效抑制 FKN-CD 介导的整合素激活。这表明 FKN-CD 实际上与位点 2 结合,并由此导致整合素激活。我们在 α4β1 和 α5β1 中也获得了非常相似的结果。FKN 与位点 2 的结合以及由此导致的整合素激活可能是整合素激活和 FKN 信号传导的一种新机制。