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首页> 外文期刊>Biochemistry >Extensive contact between Gi2 and N-formyl peptide receptor of human neutrophils: mapping of binding sites using receptor-mimetic peptides.
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Extensive contact between Gi2 and N-formyl peptide receptor of human neutrophils: mapping of binding sites using receptor-mimetic peptides.

机译：人类嗜中性粒细胞的Gi2和N-甲酰基肽受体之间的广泛接触：使用受体模拟肽映射结合位点。

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摘要

The N-formyl peptide receptor (FPR) of human neutrophils is a member of the G protein-coupled receptor (GPCR) superfamily. Sites on agonist-occupied FPR involved in binding the Gi2 protein were investigated by competition with synthetic receptor-mimetic peptides. Twenty-three synthetic FPR-mimetic and control peptides were tested for their ability to disrupt functionally active complexes of FPR and Gi2 in octyl glucoside, assayed by changes in sedimentation rates of FPR in detergent-containing sucrose gradients. GPCRs are thought to contain seven transmembrane segments with three cytoplasmic connecting loops and a cytoplasmic tail. Only certain peptides from regions in or adjoining each of the four predicted cytoplasmic domains of the 350 amino acid FPR, including the first cytoplasmic loop, were able to disrupt the reconstituted FPR-Gi2 complex. The IC50s of the peptides that were able to fully disrupt the FPR-Gi2 complex ranged from 20 microM (C2W 122-134) to 1.4 mM (C3A 230-246), a range similar to peptide inhibition of other G protein-coupled receptor-G protein interactions. Detergent concentrations above and below the critical micelle concentration had no effect on the activity of even the most hydrophobic peptide, C3B, and there was no apparent correlation of activity with hydrophobic moment, hydrophilic index, or net charge of the peptides. Control peptides from irrelevant proteins with similar physical properties and FPR extracellular domains did not dissociate the reconstituted FPR-Gi2 complex up to 5 mM, the highest concentration tested.(ABSTRACT TRUNCATED AT 250 WORDS)
机译：人类嗜中性粒细胞的N-甲酰基肽受体（FPR）是G蛋白偶联受体（GPCR）超家族的成员。通过与合成受体模拟肽竞争研究了激动剂占据的FPR上参与结合Gi2蛋白的位点。测试了23种合成FPR模拟肽和对照肽破坏辛基葡萄糖苷中FPR和Gi2的功能性活性复合物的能力，通过含洗涤剂的蔗糖梯度中FPR沉降速率的变化来测定。 GPCR被认为包含七个跨膜区段，具有三个胞质连接环和一个胞质尾巴。仅来自350个氨基酸的FPR的四个预测的胞质结构域中的区域或与之邻接的某些肽，包括第一个胞质环，能够破坏重构的FPR-Gi2复合物。能够完全破坏FPR-Gi2复合物的肽的IC50范围为20 microM（C2W 122-134）至1.4 mM（C3A 230-246），其范围类似于其他G蛋白偶联受体的肽抑制作用。 G蛋白相互作用。高于和低于临界胶束浓度的去污剂浓度甚至对最疏水的肽C3B的活性也没有影响，并且活性与肽的疏水性矩，亲水指数或净电荷之间没有明显的相关性。来自具有相似物理特性和FPR细胞外结构域的无关蛋白的对照肽未解离重构的FPR-Gi2复合体，最高检测浓度为5 mM（摘要截短为250字）

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