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Synthesis and biological evaluation of the 1,5-diarylpyrazole class of cyclooxygenase-2 inhibitors: identification of 4-[5-(4-methylphenyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl]benze nesulfonamide (SC-58635, celecoxib).

Journal of Medicinal Chemistry, 1997
A series of sulfonamide-containing 1,5-diarylpyrazole derivatives were prepared and evaluated for their ability to block cyclooxygenase-2 (COX-2) in vitro and in vivo.
T. Penning   +22 more
semanticscholar   +1 more source

Cloning and Expression of Cyclooxygenase-1 and Cyclooxygenase-2

2010
Cyclooxygenase (COX) enzymes play important roles in normal physiology and during inflammation of various cells and tissues. In order to help understand the functions of these enzymes, their genes can be cloned to facilitate the production of the proteins in recombinant form.
Beverly A. Reitz, Nicholas R. Staten
openaire   +3 more sources

Cyclooxygenase-2 and inflammation in atherosclerosis

Current Opinion in Pharmacology, 2004
By regulating the production of eicosanoids, cyclooxygenase (COX) modulates processes contributing to atherosclerosis and thrombosis, including platelet aggregation and the local inflammatory response. COX-2, a key mediator of inflammation, is upregulated in activated monocyte/macrophages, suggesting that COX-2 inhibition might reduce atherogenesis ...
MacRae F. Linton, Sergio Fazio
openaire   +2 more sources

Cyclooxygenase-2 Biology

Current Pharmaceutical Design, 2003
In mammalian cells, eicosanoid biosynthesis is usually initiated by the activation of phospholipase A(2) and the release of arachidonic acid from membrane phospholipids in response to the interaction of a stimulus with a receptor on the cell surface. Arachidonic acid is subsequently transformed by the enzyme cyclooxygenase (COX) to prostaglandins (PGs)
openaire   +3 more sources

Cyclooxygenase-2 and prostate carcinogenesis

Cancer Letters, 2003
In recent years a dramatic surge has occurred on studies defining to the role of cyclooxygenase (COX)-2 in causation and prevention of cancer. Prostaglandin (PG) endoperoxidase synthase also commonly referred to as COX is a key enzyme involved in the conversion of arachidonic acid to PGs and other eicosanoids.
T. Hussain, Hasan Mukhtar, Sanjay Gupta
openaire   +3 more sources

Lung cancer and cyclooxygenase-2

The Annals of Thoracic Surgery, 2003
Lung cancer is by far the leading cause of cancer-related death. Overall survival is poor and has not improved substantially over the last half century. It is clear that new approaches are needed and these should include prevention, screening for early detection, and novel treatments based on our understanding of the molecular biology of this disease ...
Ross M. Bremner   +4 more
openaire   +3 more sources

Perspectives on the Cyclooxygenase-2/ Cyclooxygenase-1 Hypothesis

JCR: Journal of Clinical Rheumatology, 1998
The introduction of the cyclooxygenase (COX) hypothesis to explain both the therapeutic effects and the toxicity of nonsteroidal anti-inflammatory drugs (NSAIDs) has provided direction for the development of preferential and highly selective COX-2 inhibitors, which retain efficacy against inflammation with reduced risk of toxicity. However, the complex
openaire   +2 more sources

THE ROLE OF CYCLOOXYGENASE-2 IN INFLAMMATION

American Journal of Therapeutics, 1995
Prostaglandins (PGs) can be synthetized via two isoforms of cyclooxygenase (COX). COX-1 is constitutively expressed in normal tissues, and its activity represent the normal physiological output of PGs. In inflammatory states, the newly discovered COX-2 is rapidly induced, and its activity accounts for the large amounts of PGs seen in inflammation.
Daniela Salvemini   +6 more
openaire   +3 more sources

Highly sensitive naphthalene-based two-photon fluorescent probe for in situ real-time bioimaging of ultratrace cyclooxygenase-2 in living biosystems.

Analytical Chemistry, 2014
Detecting and imaging of ultratrace cyclooxygenase-2 in living biosystems could provide much important valuable information for the diagnosis and intervention of cancer.
Hua Zhang   +9 more
semanticscholar   +1 more source

Cyclooxygenase-2 as a therapeutic target

Inflammation Research, 1998
Cyclooxygenase (COX)-2 is the predominant COX isoform present at sites of inflammation, and produces prostaglandins (PG) that cause swelling and pain. However, in situations where the release of protective PGs by COX-1 has been lost, the induction of COX-2 may compensate and reduce inflammatory responses.
T. W. Evans, J. A. Mitchell
openaire   +2 more sources

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