Toward the management of inflammation: recent developments of mPGES-1 inhibitors.
For decades, the struggle against inflammation and related disorders has constituted an important field in medical practice, with strategies mainly aimed at inhibiting compounds produced through the arachidonic acid pathway. Thus, specific COX-2 inhibitors or "coxibs", were recently designed, that play an increasing but controversial role in reducing inflammatory phenomenon. Lately, several patents have been generated which target the specific inhibition of the microsomal Prostanglandin E synthase-1 (mPGES-1). This enzyme, which was cloned and characterized at the end of the nineties, catalyzes under inflammatory stimuli the last step of PGE2 synthesis. A corpus of data is now available illustrating the pivotal role played by this enzyme in numerous symptoms linked to inflammation such as fever, anorexia or pain. The present review highlights the current state of knowledge of the involvement of mPGES-1 in sickness behaviour and in other inflammation-related disorders and summarizes the recent patents related to mPGES-1 and its specific inhibition.
Dallaporta
M
M
Centre de Recherche en Neurobiologie-Neurophysiologie de Marseille (CRN2M), UMR 6231 CNRS, USC INRA 2027, Université Paul Cézanne, Université de la Méditerranée, Marseille, France.
Pecchi
E
E
Thirion
S
S
Jean
A
A
Troadec
J-D
JD
D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000737:chemistry / Q000627:therapeutic use*; D016861:Cyclooxygenase Inhibitors / Q000627:therapeutic use; D004791:Enzyme Inhibitors / Q000737:chemistry / Q000627:therapeutic use*; D006801:Humans; D007249:Inflammation / Q000188:drug therapy* / Q000201:enzymology / Q000235:genetics; D019746:Intramolecular Oxidoreductases / Q000037:antagonists & inhibitors* / Q000378:metabolism; D000071876:Prostaglandin-E Synthases
D000894:Anti-Inflammatory Agents, Non-Steroidal; D016861:Cyclooxygenase Inhibitors; D004791:Enzyme Inhibitors; D019746:Intramolecular Oxidoreductases; C000605862:PTGES protein, human; D000071876:Prostaglandin-E Synthases