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New alpha-substituted succinate-based hydroxamic acids as TNFalpha convertase inhibitors.
Tumor necrosis factor alpha convertase (TACE), the enzyme responsible for the processing of pro-TNFalpha to TNFalpha, has been reported to be a metalloproteinase closely related to matrixExpand
Daunorubicin Activates NFκB and Induces κB-dependent Gene Expression in HL-60 Promyelocytic and Jurkat T Lymphoma Cells*
The anthracycline antibiotic, daunorubicin, can induce programmed cell death (apoptosis) in cells. Recent work suggests that this event is mediated by ceramide via enhanced ceramide synthaseExpand
Leukotrienes do not regulate interleukin 1 production by activated macrophages.
The objective of this work was to investigate the role of leukotrienes in the production of IL-1 by activated human peripheral blood monocytes and mouse peritoneal macrophages. Using overnightExpand
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
Formation of dimethyl selenide and trimethylselenonium from selenobetaine in the rat.
The 24-h respiratory excretion of dimethyl selenide (DMSe) and urinary excretion of trimethylselenonium (TMSe) were studied in adult male rats injected with 2 mg Se/kg as selenobetaineExpand
(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
Production of TNFα by LPS-stimulated murine, rat and human blood and its pharmacological modulation
Tumour necrosis factorα (TNFα) has been reported to play a key role in the pathogenesis of sepsis and chronic inflammatory diseases, including rheumatoid arthritis and atherosclerosis, suggestingExpand
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
Hormone-induced desensitisation of hormonal control of cyclic AMP levels in human diploid fibroblasts.
THE elevation of cyclic AMP levels in response to hormonal stimulation in many cells and tissues is transient1–5. In the absence of an inhibitor of phosphodiesterase actiiity, much of the newlyExpand
Glucocorticoids increase the responsiveness of cells in culture to prostaglandin E1.
The influence of steroid hormones on the response of human astrocytoma cells (1321N1) to prostaglandin E(1) (PGE(1)) has been investigated. Responsiveness to PGE(1) was determined by measuring theExpand