Inhibitors of secreted phospholipase A2 suppress the release of PGE2 in renal mesangial cells.
Bioorg Med Chem
; 24(13): 3029-3034, 2016 07 01.
Article
em En
| MEDLINE
| ID: mdl-27234891
ABSTRACT
The upregulation of PGE2 by mesangial cells has been observed under chronic inflammation condition. In the present work, renal mesangial cells were stimulated to trigger a huge increase of PGE2 synthesis and were treated in the absence or presence of known PLA2 inhibitors. A variety of synthetic inhibitors, mainly developed in our labs, which are known to selectively inhibit each of GIVA cPLA2, GVIA iPLA2, and GIIA/GV sPLA2, were used as tools in this study. Synthetic sPLA2 inhibitors, such as GK115 (an amide derivative based on the non-natural amino acid (R)-γ-norleucine) as well as GK126 and GK241 (2-oxoamides based on the natural (S)-α-amino acid leucine and valine, respectively) presented an interesting effect on the suppression of PGE2 formation.
Palavras-chave
Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Dinoprostona
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Células Mesangiais
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Fosfolipases A2 Secretórias
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Inibidores de Fosfolipase A2
Limite:
Animals
Idioma:
En
Revista:
Bioorg Med Chem
Assunto da revista:
BIOQUIMICA
/
QUIMICA
Ano de publicação:
2016
Tipo de documento:
Article
País de afiliação:
Grécia