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Titolo:
Cyclooxygenase inhibitors - current status and future prospects
Autore:
Dannhardt, G; Kiefer, W;
Indirizzi:
Univ Mainz, Inst Pharm, D-55099 Mainz, Germany Univ Mainz Mainz Germany D-55099 inz, Inst Pharm, D-55099 Mainz, Germany
Titolo Testata:
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
fascicolo: 2, volume: 36, anno: 2001,
pagine: 109 - 126
SICI:
0223-5234(200102)36:2<109:CI-CSA>2.0.ZU;2-6
Fonte:
ISI
Lingua:
ENG
Soggetto:
NONSTEROIDAL ANTIINFLAMMATORY DRUGS; PROSTAGLANDIN ENDOPEROXIDE SYNTHASE; SELECTIVE COX-2 INHIBITOR; INDUCIBLE CYCLOOXYGENASE; IN-VITRO; COLON-CANCER; POSTTRANSCRIPTIONAL REGULATION; GASTROINTESTINAL TOXICITY; DIFFERENTIAL INHIBITION; BIOLOGICAL EVALUATION;
Keywords:
cyclooxygenase (COX-1, COX-2); classic NSAIDs; selective COX-2 inhibitors; inflammation; angiogenesis; colon cancer; Alzheimer's disease;
Tipo documento:
Review
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
113
Recensione:
Indirizzi per estratti:
Indirizzo: Dannhardt, G Univ Mainz, Inst Pharm, Staudingerweg 5, D-55099 Mainz, Germany Univ Mainz Staudingerweg 5 Mainz Germany D-55099 nz, Germany
Citazione:
G. Dannhardt e W. Kiefer, "Cyclooxygenase inhibitors - current status and future prospects", EUR J MED C, 36(2), 2001, pp. 109-126

Abstract

Prostaglandins are formed from arachidonic acid by the action of cyclooxygenase and subsequent downstream synthetases. Two closely related forms of the cyclooxygenase have been identified which are now known as COX-1 and COX-2. Both isoenzymes transform arachidonic acid to prostaglandins, but differ in their distribution and their physiological roles. Meanwhile, the responsible genes and their regulation have been clarified. COX-I, the pre-dominantly constitutive form of the enzyme, is expressed throughout the body andperforms a number of homeostatic functions such as maintaining normal gastric mucosa and influencing renal blood flow and platelet aggregation. In contrast, the inducible form is expressed in response to inflammatory and other physiological stimuli and growth factors, and is involved in the production of the prostaglandins that mediate pain and support the inflammatory process. All the classic NSAIDs inhibit both COX-1 and COX-2 at standard anti-inflammatory doses. The beneficial anti-inflammatory and analgesic effectsare based on the inhibition of COX-2, but the gastrointestinal toxicity and the mild bleeding diathesis are a result of the concurrent inhibition of COX-1. Agents that inhibit COX-2 while sparing COX-I represent a new attractive therapeutic development and could represent a major advance in the treatment of rheumatoid arthritis and osteoarthritis. Apart from its involvement in inflammatory processes, COX-2 seems to play a role in angiogenesis, colon cancer and Alzheimer's disease, based on the fact that it is expressedduring these diseases. The benefits of specific and selective COX-2 inhibitors are currently under discussion and offer a new perspective for a further use of COX-2 inhibitors. (C) 2001 Editions scientifiques et medicales Elsevier SAS.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 03/04/20 alle ore 03:40:52