Inhibitors of secreted phospholipase A2 suppress the release of PGE2 in renal mesangial cells

Vasilakaki, Sofia; Barbayianni, Efrosini; Magrioti, Victoria; Pastukhov, Oleksandr; Constantinou-Kokotou, Violetta; Huwiler, Andrea; Kokotos, George (2016). Inhibitors of secreted phospholipase A2 suppress the release of PGE2 in renal mesangial cells. Bioorganic & medicinal chemistry, 24(13), pp. 3029-3034. Elsevier 10.1016/j.bmc.2016.05.017

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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.

Item Type:

Journal Article (Original Article)

Division/Institute:

04 Faculty of Medicine > Pre-clinic Human Medicine > Institute of Pharmacology

UniBE Contributor:

Pastukhov, Oleksandr and Huwiler, Andrea

Subjects:

600 Technology > 610 Medicine & health

ISSN:

0968-0896

Publisher:

Elsevier

Language:

English

Submitter:

Jana Berger

Date Deposited:

13 Sep 2016 14:20

Last Modified:

13 Sep 2016 14:20

Publisher DOI:

10.1016/j.bmc.2016.05.017

PubMed ID:

27234891

Uncontrolled Keywords:

Inhibitors; Mesangial cells; Phospholipase A(2); Prostaglandin E(2); Secreted phospholipase A(2)

BORIS DOI:

10.7892/boris.87524

URI:

https://boris.unibe.ch/id/eprint/87524

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