Targeting inflammation: multiple innovative ways to reduce prostaglandin E₂.
The PGE2 pathway is important in inflammation-driven diseases and specific targeting of the inducible mPGES-1 is warranted due to the cardiovascular problems associated with the long-term use of COX-2 inhibitors. This review focuses on patents issued on methods of measuring mPGES-1 activity, on drugs targeting mPGES-1 and on other modulators of free extracellular PGE2 concentration. Perspectives and conclusions regarding the status of these drugs are also presented. Importantly, no selective inhibitors targeting mPGES-1 have been identified and, despite the high number of published patents, none of these drugs have yet made it to clinical trials.
The University of Arizona Cancer Center, Tucson, AZ 85724, USA.
Jessica K
JK
Norberg
Earlphia
E
Sells
Hui-Hua
HH
Chang
Srinivas R
SR
Alla
Shuxing
S
Zhang
Emmanuelle J
EJ
Meuillet
D000818:Animals; D015232:Dinoprostone / Q000378:metabolism*; D006801:Humans; D007249:Inflammation / Q000378:metabolism*; D019746:Intramolecular Oxidoreductases / Q000037:antagonists & inhibitors* / Q000378:metabolism; D000071876:Prostaglandin-E Synthases
D019746:Intramolecular Oxidoreductases; C000605862:PTGES protein, human; D000071876:Prostaglandin-E Synthases; D015232:Dinoprostone