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Small Peptides Able to Suppress Prostaglandin E(2) Generation in Renal Mesangial Cells

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 PGE(2) in mesangial cells. The new compounds were generated by structural alterations applied on GK115, a novel inhi...

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Detalles Bibliográficos
Autores principales: Vasilakaki, Sofia, Pastukhov, Oleksandr, Mavromoustakos, Thomas, Huwiler, Andrea, Kokotos, George
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2018
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6017359/
https://www.ncbi.nlm.nih.gov/pubmed/29342835
http://dx.doi.org/10.3390/molecules23010158
Descripción
Sumario: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 PGE(2) in mesangial cells. The new compounds were generated by structural alterations applied on GK115, a novel inhibitor of secreted phospholipase A(2), which has been previously shown to reduce PGE(2) synthesis in rat renal mesangial cells. Among the synthesized compounds, the tripeptide derivative 11 exhibited a nice dose-dependent suppression of PGE(2) production, similar to that observed for GK115.