The study published in the journal ChemMedChem is a result of cooperation between teams guided by Zlatek Janeba from the Institute of Organic Chemistry and Biochemistry of the Czech Academy of Sciences (CAS) and Zdeněk Zídek from the Institute of Experimental Medicine, CAS.
18. 8. 2020
It concerns the development of new inhibitors of prostaglandin E2 (PGE2) which is an important mediator of inflammatory diseases.
PGE2 is one of many metabolites of arachidonic acid (AA). Its production mainly depends on the enzymes cyclooxygenase (COX-1 / COX-2) and prostaglandin E synthesis (PGES-1). As adverse reactions to drugs based on COX inhibition have been surveyed in clinics, PGES-1 inhibitors are considered more suitable for the development of new anti-inflammatory drugs. Some of the polysubstituted pyrimidine derivatives presented in the study are strong inhibitors of PGE2, whereas the mechanism of action consist in the selective inhibition of PGES-1 activity. The activities of other enzymes and the formation of other physiologically important metabolites of AA remain unaffected.
This process is simply illustrated by the image used on the cover of the magazine.
You can find more information in the published article:
F. Kalčic, V. Kolman, H. Ajani, Z. Zídek, Z. Janeba. Polysubstituted Pyrimidines as mPGES‐1 Inhibitors: Discovery of Potent Inhibitors of PGE2 Production with Strong Anti‐inflammatory Effects in Carrageenan‐Induced Rat Paw Edema. ChemMedChem 2020, 15, 1398.
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