Inibidores seletivos de prostaglandina endoperóxido sintase-2 (PGHS-2): nova estratégia para o tratamento da inflamação

Química Nova

Adriana Dos Santos Lages²  Nelilma Correia Romeiro²  Carlos Alberto Manssour Fraga¹  Eliezer Jesus Barreiro¹ 

[1],Universidade Federal do Rio de Janeiro Instituto de Química Rio de Janeiro RJ

关键词: selective PGHS-2 inhibitors;    nonsteroidal anti-inflammatory drugs;    inflammation;   

DOI  :  10.1590/S0100-40421998000600017

来源: SciELO

【 摘 要 】

Prostaglandins (PG's), produced from arachidonic acid metabolism, are potent mediators of inflammation. Nonsteroidal anti-inflammatory (NSAIDs) exert their effects by inhibition of prostaglandin endoperoxide synthase (PGHS) enzyme, which catalyses the first committed step in arachidonic acid metabolism. Two isoforms of PGHS are known: PGHS-1, constitutively expressed in most tissues, and is responsible for physiological production of PG's. The second isoform, PGHS-2, is induced by cytokines, mitogens and endotoxins in inflammatory cells, and appears to be responsible for the elevated production of PG's during inflammation. With the recent discovery of the inducible PGHS (PGHS-2), the medicinal chemist now possesses a novel target for designing therapeutic agents that could provide suitable anti-inflammatory activity without the ulcerogenic and renal side effects associated with currently available NSAIDs, all of which inhibit both PGHS-1 and PGHS-2.

【 授权许可】

CC BY-NC   
 All the contents of this journal, except where otherwise noted, is licensed under a Creative Commons Attribution License