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Redirection of Eicosanoid Metabolism in mPGES-1-deficient Macrophages*
The data support the hypothesis that mPGES-1 induction in response to an inflammatory stimulus is essential for PGE2 synthesis and provide novel insights into how a cell processes the unstable endoperoxide PGH2 during the inactivation of a major metabolic outlet. Expand
Pyran-containing sulfonamide hydroxamic acids: potent MMP inhibitors that spare MMP-1.
The SAR of a series of sterically hindered sulfonamide hydroxamic acids with relatively large P1' groups is described, finding that fibrosis in rats and MSS in humans is still produced. Expand
Potent, selective pyrimidinetrione-based inhibitors of MMP-13.
Using SAR from two related series of pyrimidinetrione-based inhibitors, compounds with potent MMP-13 inhibition and >100-fold selectivity against other MMPs have been identified. Despite highExpand
Celecoxib Does Not Affect the Antiplatelet Activity of Aspirin in Healthy Volunteers
The data indicate that celecoxib does not alter the effects of aspirin on platelet function, and there was no significant difference in thromboxane inhibition between the two groups. Expand
Exercise protects against articular cartilage degeneration in the hamster.
A sedentary lifestyle in the hamster leads to a lower proteoglycan content in the cartilage and a lower synovial fluid volume, which is associated with cartilage fibrillation, pitting, and fissuring. Expand
The Phosphodiesterase Type 4 (PDE4) Inhibitor CP-80,633 Elevates Plasma Cyclic AMP Levels and Decreases Tumor Necrosis Factor-α (TNFα) Production in Mice: Effect of Adrenalectomy
Rolipram was previously reported to elevate plasma cyclic adenosine 3′,5′-monophosphate (cAMP) and inhibit serum tumor necrosis factor-α (TNFα) production in mice. CP-80,633, a new cyclic nucleotideExpand
Phosphinic acid-based MMP-13 inhibitors that spare MMP-1 and MMP-3.
Combining improved P(1)' and P(2) groups into a single molecule gave an inhibitor with a 4.5 nM IC(50) against M MP-13 and which is 270-fold selective over MMP-1. Expand
The phosphodiesterase type 4 (PDE4) inhibitor CP-80,633 elevates plasma cyclic AMP levels and decreases tumor necrosis factor-alpha (TNFalpha) production in mice: effect of adrenalectomy.
Results show that CP-80,633, when given p.o. to mice, is capable of elevating plasma cAMP and inhibiting TNFalpha production and that adrenal catecholamines contribute significantly to the effect of CP-70,000 on the cAMP response but only slightly to its effect on the systemic TNF alpha response. Expand
Solid-phase extraction and high-performance liquid chromatography analysis of lipoxygenase pathway products.
The addition of the mobile-phase additives, trifluoroacetic acid and triethylamine, enable the peptido-leukotrienes to be eluted with excellent peak shape and unique elution times. Expand
Inhibition of 5-lipoxygenase product formation and polymorphonuclear cell degranulation by tenidap sodium in patients with rheumatoid arthritis.
The unique 5-lipoxygenase inhibitory property of tenidap, as measured by LTB4 production and degranulation, suggests that it may have clinical activity which differentiates it from nonsteroidal antiinflammatory drugs. Expand