TY - JOUR
T1 - Inhibitors of secreted phospholipase A2 suppress the release of PGE2 in renal mesangial cells
JF - Bioorganic and Medicinal Chemistry
Y1 - 2016
A1 - Vasilakaki, S.
A1 - Barbayianni, E.
A1 - Magrioti, V.
A1 - Pastukhov, O.
A1 - Constantinou-Kokotou, V.
A1 - Huwiler, A.
A1 - Kokotos, G.
AB - 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.
VL - 24
N1 - Export Date: 18 January 2017
JO - Bioorg Med Chem
ER -