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.
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。
