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Inhibition by retinoic acid of collagenase production in rheumatoid synovial cells.
IN rheumatoid arthritis, synovial cells produce many mediators of inflammation in response to stimuli generated within the inflamed joint. Collagenase and prostaglandin E2 are two of these mediator...
Designing therapeutically effective 5-lipoxygenase inhibitors.
Metabolism of arachidonic acid by the enzyme 5-lipoxygenase leads to the formation of a group of biologically active lipids known as leukotrienes. Peptidoleukotrienes are powerful bronchoconstrictorExpand
Pre‐clinical pharmacology of ICI D2138, a potent orally‐active non‐redox inhibitor of 5‐lipoxygenase
1 This paper describes the pre‐clinical pharmacology of ICI D2138, a potent orally‐active non‐redox inhibitor of 5‐lipoxygenase which is undergoing clinical evaluation. 2 ICI D2138 potently inhibitedExpand
(Methoxyalkyl)thiazoles: a new series of potent, selective, and orally active 5-lipoxygenase inhibitors displaying high enantioselectivity.
(Methoxyalkyl)thiazoles are novel 5-lipoxygenase (5-LPO) inhibitors that are neither redox agents nor iron chelators. Consideration of a hypothetical model of the enzyme active site led to thisExpand
Structure and activity relationships leading to the discovery of ICI D2138, a selective, potent and orally active inhibitor of 5-lipoxygenase.
Structure and activity relationships of (methoxyalkyl)thiazole and 4-methoxytetrahydropyran series of 5-lipoxygenase inhibitors are reviewed. One member of the 4-methoxytetrahydropyran series,Expand
Collagenase production by synovial fibroblasts treated with phorbol myristate acetate.
A series of intracellular events occurring after treatment of rabbit synovial fibroblasts with 0.01 micrograms/ml phorbol myristate acetate (PMA) were measured. Ten minutes after addition of PMA,Expand
Malonaldehyde formation in intact platelets is catalysed by thromboxane synthase.
Imidazole and compound L8027 (selective inhibitors of thromboxane synthase) produced parallel inhibition of malonaldehyde and thromboxane B2 secretion induced by collagen or thrombin in gel-filteredExpand
Induction of collagenase and prostaglandin synthesis in synovial fibroblasts treated with monosodium urate crystals
The inflammation of acute gout has been studied extensively and is mediated by interaction of crystals of monosodium urate monohydrate (MSUM) with phagocytic cells (Phelps & McCarty 1966; Weissmann &Expand
Collagenase release from synovial fibroblasts: relationship to fatty acid release and prostaglandin synthesis
Rheumatoid synovium has proliferative and destructive characteristics in vivo. These capabilities are also evident in tissue culture studies in which cultured expiants of rheumatoid synovium haveExpand