New indications for Prostaglandin E Synthase inhibitors, verification in human tissue
|Coordinator||Gesynta Pharma AB|
|Funding from Vinnova||SEK 300 000|
|Project duration||December 2017 - December 2018|
Purpose and goal
The aim of Gesynta´s project was to study the effects of mPGES-1 inhibitors on vascular physiology, specifically with regard to vasodilation in human tissue samples. The mechanism includes a shunting effect to vasodilatory prostacyclin. We could show that mPGES-1 inhibition has a positive effect through its vasodilatory properties and that this is linked to shunting.
Expected results and effects
mPGES-1 inhibitors display a vasodilatory effect that we now verified in two human systems. Both in intermediate arteries from breast tissue and small arteries taken close to fat biopsies. These results open the way for clinical studies of indications where the combination of an anti-inflammatory and vasodilatory effect of mPGES-1 inhibition is potentially beneficial.
Planned approach and implementation
Human tissue (vessels) from biopsies were incubated in organ baths and contractility was measured after addition of physiological stimulators. The Gesynta synthesised mPGES-1 inhibitors were added and effects on the contraction were analyzed. The mechanism for shunting could be verified using prostacyclin receptor antagonists.