Recent Patents on CNS Drug Discovery

Vincenzo Di Marzo
Istituto di Chimica Biomolecolare (I.C.B.)
Consiglio Nazionale delle Ricerche (C.N.R.)
Via Campi Flegrei 34
Pozzuoli, Napoli 80078


Towards the Management of Inflammation: Recent Developments of mPGES-1 Inhibitors

Author(s): Michel Dallaporta, Emilie Pecchi, Sylvie Thirion, Andre Jean and Jean-Denis Troadec

Affiliation: Centre de Recherche en Neurobiologie-Neurophysiologie de Marseille (CRN2M), Departement de Physiologie Neurovegetative, Faculte des Sciences et Techniques de St Jerome, Avenue Escadrille Normandie-Niemen, 13397 Marseille cedex 20, France.


For decades, the struggle against inflammation and related disorders has constituted an important field in medical practice, with strategies mainly aimed to inhibit the compounds produced through the arachidonic acid pathway. Thus, specific COX-2 inhibitors or “coxibs”, have been recently designed that play an important but controversial role in reducing inflammatory phenomenon. Lately, several patents have been generated which target the specific inhibition of microsomal Prostaglandin E synthase-1 (mPGES-1). This enzyme, which was cloned and characterized at the end of 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.

Keywords: mPGES-1, mPGES-1-inhibtors, PGE2, inflammation, anorexia, fever, pain, sickness behavior, cancer, cardiovascular diseases

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Article Details

Page: [70 - 80]
Pages: 11
DOI: 10.2174/157488910789753549