小分子肽可抑制肾系膜细胞前列腺素 E₂ 的生成。
Small Peptides Able to Suppress Prostaglandin E₂ Generation in Renal Mesangial Cells.
机构信息
Laboratory of Organic Chemistry, Department of Chemistry, National and Kapodistrian University of Athens, Panepistimiopolis, Athens 15771, Greece.
Institute of Pharmacology, University of Bern, Bern 3010, Switzerland.
出版信息
Molecules. 2018 Jan 13;23(1):158. doi: 10.3390/molecules23010158.
Peptide drug discovery may play a key role in the identification of novel medicinal agents. Here, we present the development of novel small peptides able to suppress the production of PGE₂ in mesangial cells. The new compounds were generated by structural alterations applied on GK115, a novel inhibitor of secreted phospholipase A₂, which has been previously shown to reduce PGE₂ synthesis in rat renal mesangial cells. Among the synthesized compounds, the tripeptide derivative exhibited a nice dose-dependent suppression of PGE₂ production, similar to that observed for GK115.
肽类药物的发现可能在新型药物的鉴定中发挥关键作用。在此，我们介绍了新型小肽的开发，这些小肽能够抑制系膜细胞中 PGE₂的产生。新化合物是通过对 GK115 的结构改变生成的，GK115 是一种新型分泌型磷脂酶 A₂抑制剂，先前已被证明可减少大鼠肾系膜细胞中 PGE₂的合成。在所合成的化合物中，三肽衍生物 表现出与 GK115 相似的剂量依赖性 PGE₂产生抑制作用。
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