Assessing activation of the human neuropeptide FF2 receptor with a non-radioactive GTP binding assay

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• 作者：Engstr&ouml ; m ; Mia ; Nä ; rvä ; nen ; Ale ; Savola ; Juha-Matti ; Wurster ; Siegfried
• 关键词：Neuropeptide FF ; Eu-GTP binding assay ; [³⁵S]GTPγ ; S binding assay ; NPFF2 receptor ; Neuropeptides ; Structure&ndash ; activity relationship
• 刊名：Peptides
• 出版年：2004
• 期刊代码：59_01969781
• 类别：neu
• 出版时间：December, 2004
• 卷：25
• 期：12
• 页码：2099-2104
• 文件大小：141 K

摘要

We have evaluated a novel, time-resolved fluorometric GTP binding assay for its suitability for functional screening of neuropeptide FF (NPFF) receptor ligands. Our results suggest that this assay, which relies on the use of a europium-labeled GTP analogue, Eu-GTP, provides a powerful alternative to the [³⁵S]guanosine-5′-O-(3-thio)triphosphate binding assay for assessing the functional properties of NPFF analogs. Further, we demonstrate that the tetrapeptide PMRF-NH₂ exhibited high agonist potency at the NPFF2 receptor, and that the efficacies of this peptide and another shortened NPFF analog were greater than that of NPFF.