Background: Cancer is one of the most life-threatening diseases worldwide. Since inflammation is
considered to be one of the known characteristics of cancer, the activity of PGE2 has been paired with different
tumorigenic steps such as increased tumor cell proliferation, resistance to apoptosis, increased invasiveness,
angiogenesis and immunosuppression.
Objective: It has been successfully demonstrated that inhibition of mPGES-1 prevented inflammation in preclinical
studies. However, despite the crucial roles of mPGEs-1 and PGE2 in tumorigenesis, there is not much in vivo study
on mPGES-1 inhibition in cancer therapy. The specificity of mPGEs-1 enzyme and its low expression level under
normal conditions makes it a promising drug target with a low risk of side effects.
Methods: A comprehensive literature search was performed for writing this review. An updated view on PGE2
biosynthesis, PGES isoenzyme family and its pharmacology and the latest information about inhibitors of mPGES-1
have been discussed.
Results: In this study, it was aimed to highlight the importance of mPGES-1 and its inhibition in inflammationrelated
cancer and other inflammatory conditions. Information about PGE2 biosynthesis, its role in inflammationrelated
pathologies were also provided. We kept the noncancer-related inflammatory part short and tried to bring
together promising molecules or scaffolds.
Conclusion: The information provided in this review might be useful to researchers in designing novel and potent
mPGES-1 inhibitors for the treatment of cancer and inflammation.