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粒细胞集落刺激因子受体肽激动剂的筛选。

A screen for peptide agonists of the G-CSF receptor.

作者信息

Conzelmann Nadine, Schneider Armin

机构信息

SYGNIS Bioscience, Im Neuenheimer Feld 515, 69120 Heidelberg, Germany.

出版信息

BMC Res Notes. 2011 Jun 15;4:194. doi: 10.1186/1756-0500-4-194.

Abstract

BACKGROUND

Granulocyte-colony stimulating factor (G-CSF) is one of the most important pharmacologically used proteins. Potential uses beyond the stimulation of neutrophilic granulocytes are the treatment of CNS disorders. Disadvantages of the G-CSF protein as a drug are its moderate plasma half-life time and considerable production costs. We therefore conducted a screen for peptide agonists derived from the sequence of human G-CSF.

FINDINGS

Despite of the high sensitivity of our screening system we could not detect any positive hits in a single peptide approach. In a multiplex approach using a permutation of any combination of 10 different peptides we could also not detect a positive block.

CONCLUSIONS

We conclude that larger coherent parts of the protein or dimerising peptides may be needed to achieve activation of the receptor.

摘要

背景

粒细胞集落刺激因子(G-CSF)是药理学上最重要的蛋白质之一。除了刺激嗜中性粒细胞外,其潜在用途还包括治疗中枢神经系统疾病。G-CSF蛋白作为药物的缺点是其血浆半衰期适中且生产成本高昂。因此,我们对源自人G-CSF序列的肽激动剂进行了筛选。

研究结果

尽管我们的筛选系统具有很高的灵敏度,但在单一肽方法中未检测到任何阳性结果。在使用10种不同肽的任意组合排列的多重方法中,我们也未检测到阳性阻断。

结论

我们得出结论,可能需要蛋白质的更大连贯部分或二聚化肽来实现受体的激活。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1bb4/3132715/4a1ca8032b1e/1756-0500-4-194-1.jpg

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