A novel fluorescent cross-reactive formylpeptide receptor/formylpeptide receptor-like 1 hexapeptide ligand.
A novel fluorescent cross-reactive formylpeptide receptor/formylpeptide receptor-like 1 hexapeptide ligand.
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DOI：
10.1002/cyto.a.20670
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发表时间：
2009-03
期刊：
影响因子：
3.7
通讯作者：
Edwards, Bruce S.
中科院分区：
文献类型：
--
作者：
Strouse, J. Jacob;Young, Susan M.;Mitchell, Hugh D.;Ye, Richard D.;Prossnitz, Eric R.;Sklar, Larry A.;Edwards, Bruce S.
关键词：
甲酰肽受体参与多种免疫和炎症反应级联。进一步了解FPR家族配体相互作用可以在生物学和治疗发现中发挥不可或缺的作用。该家族的荧光报告配体是增加对配体/受体相互作用的理解的理想实验工具。通过使用高通量HyperCyt®流式细胞仪平台探索肽WK（FL）YMVm的配体结合亲和力和荧光报告活性。在双重测定形式中比较几种已知FPR和FPRL 1肽配体的相对结合亲和力。荧光W-肽配体WK（FL）YMVm被证明是FPR/FPRL 1双链体测定的高亲和力、交叉反应性报告配体。配体特异性证明了每个受体与已知的，选择性的肽配体。通过荧光共聚焦显微镜内化实验进一步验证了报告配体的结合位点特异性。荧光肽配体WK（FL）YMVm以高亲和力结合FPR和FPRL 1。在HTS流式细胞术中使用该荧光探针观察已知肽配体的差异亲和力。
Formylpeptide receptors are implicated in a variety of immunological and inflammatory response cascades. Further understanding FPR-family ligand interactions could play an integral role in biological and therapeutic discovery. Fluorescent reporter ligands for the family are desirable experimental tools for increased understanding of ligand/receptor interactions. The ligand binding affinity and fluorescent reporting activity of the peptide WK(FL)YMVm was explored though use of the high throughput HyperCyt® flow cytometric platform. Relative binding affinities of several known FPR and FPRL1 peptide ligands were compared in a duplex assay format. The fluorescent W-peptide ligand, WK(FL)YMVm, proved to be a high affinity, cross-reactive reporter ligand for the FPR/FPRL1 duplex assay. Ligand specificity was demonstrated for each receptor with known, selective peptide ligands. The binding site specificity of the reporter ligand was further verified by a fluorescent confocal microscopy internalization experiment. The fluorescent peptide ligand WK(FL)YMVm bound with high affinity to both FPR and FPRL1. The differential affinities of known peptide ligands were observed with the use of this fluorescent probe in HTS flow cytometry.
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