In vitro evaluation of leptin fragments activity on the ob receptor
In vitro evaluation of leptin fragments activity on the ob receptor
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DOI：
10.1002/pse.957
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发表时间：
2008-05-01
影响因子：
2.1
通讯作者：
Miranda, Antonio
中科院分区：
文献类型：
--
作者：
de Oliveira, Vani Xavier, Jr.;Fazio, Marcos Antonio;Miranda, Antonio
为了鉴定瘦素分子中负责其生物活性的区域，我们测试了六个相关的瘦素肽片段，表示为：Ac-hLEP（23-47）-NH2（I），Ac-hLEP（48-71）-NH2（II），Ac-hLEP（72-88）-NH2（III），Ac-hLEP（92-115）-NH2（IV），Ac-[Ser（117）]-hLEP（116-140）-NH2（V），Ac-hLEP（141-164）-NH 2（VI）及其相应的二硫键桥连二聚体形式。使用细胞传感器微生理计，通过与瘦素受体相互作用的能力，与瘦素相比评价片段的活性。我们的结果表明，片段IV和V以及[D-Leu（4）]-OB 3及其人序列类似物被存在于HP-75细胞中的瘦素受体识别，与其他工作者获得的结果一致，证实该分子的该区域含有瘦素分子的功能表位。版权所有（C）2007欧洲肽协会和约翰威利父子有限公司。
In an attempt to identify regions in the leptin molecule responsible for its bioactivity, we tested six related-leptin peptide fragments denoted: Ae-hLEP(23-47)-NH2 (I), Ac-hLEP(48-71)-NH2 (II), Ac-hLEP(72-88)-NH2 (III), Ac-hLEP(92-115)-NH2 (IV), Ac-[Ser(117)]-hLEP(116-140)-NH2 (V), Ac-hLEP(141-164)-NH2 (VI) and their correspondent disulfide bridged dimer forms. The activity of the fragments was evaluated in comparision to leptin, by their ability to interact with leptin receptor using a cytosensor microphysiometer. Our results indicated that the fragments IV and V and [D-Leu(4)]-OB3 and its human sequence analog were recognized by leptin receptor present in HP-75 cells, in agreement with the results obtained by other workers, validating that this region of the molecule contain the functional epitope of the leptin molecule. Copyright (C) 2007 European Peptide Society and John Wiley & Sons, Ltd.