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SB 203580 is a specific inhibitor of a MAP kinase homologue which is stimulated by cellular stresses and interleukin‐1
TLDR
It is established that MAPKAP kinase‐2 is a physiological RK substrate, and that HSP27 is phosphorylated by MAPK AP kinase-2 in vivo. Expand
A protein kinase involved in the regulation of inflammatory cytokine biosynthesis
TLDR
Production of interleukin-1 and tumour necrosis factor from stimulated human monocytes is inhibited by a new series of pyridinyl-imidazole compounds, suggesting that the CSBPs are critical for cytokine production. Expand
Pyridinyl Imidazole Inhibitors of p38 Mitogen-activated Protein Kinase Bind in the ATP Site*
TLDR
Findings indicate that the pyridinyl imidazoles act in vivo by inhibiting p38 kinase activity through competition with ATP and that their selectivity is probably determined by differences in nonconserved regions within or near the ATP binding pocket. Expand
Regulation of stress-induced cytokine production by pyridinylimidazoles; inhibition of CSBP kinase.
TLDR
Members of three classes of pyridinylimidazoles bind with varying affinities to CSBP (p38) kinase which is a member of a stress-induced signal transduction pathway, and binding is shown to correlate with inhibition of CSBP kinase activity. Expand
2,4,5- triarylimidazole inhibitors of IL-1 biosynthesis
Abstract As part of an effort to define the pharmacophore and discover the mechanism by which the antiinflammatory dual cyclooxygenase / 5-lipoxygenase inhibitors SK&F 86002 and SK&F 105809 inhibitExpand
Pyrimidinylimidazole inhibitors of CSBP/p38 kinase demonstrating decreased inhibition of hepatic cytochrome P450 enzymes.
Pyrimidine analogs of the pyrimidinylimidazole class of CSBP/p38 kinase inhibitors were prepared in an effort to reduce the potent inhibition of hepatic cytochrome P450 observed for the pyridinylExpand
1-substituted 4-aryl-5-pyridinylimidazoles: a new class of cytokine suppressive drugs with low 5-lipoxygenase and cyclooxygenase inhibitory potency.
A series of 1-alkyl- or -aryl-4-aryl-5-pyridinylimidazoles (A) were prepared and tested for their ability to bind to a recently discovered protein kinase termed CSBP and to inhibit lipopolysaccharideExpand
Nonpeptidic urotensin‐II receptor antagonists I: in vitro pharmacological characterization of SB‐706375
TLDR
SB‐706375 is a high‐affinity, surmountable, reversible and selective nonpeptide UT receptor antagonist with cross‐species activity that will assist in delineating the pathophysiological actions of U‐II in mammals. Expand
Iron-Catalyzed Borylation of Alkyl, Allyl, and Aryl Halides: Isolation of an Iron(I) Boryl Complex
Activation of B2pin2 with tBuLi facilitates the Fe-catalyzed borylation of alkyl, allyl, benzyl, and aryl halides via the formation of Li[B2pin2(tBu)] (1). The reaction of 1 with a representativeExpand
ENANTIOSELECTIVE SYNTHESIS OF PUMILIOTOXIN 251D. A STRATEGY EMPLOYING AN ALLENE-BASED ELECTROPHILE-MEDIATED CYCLIZATION
The enantioselective synthesis of pumiliotoxin 251D (1) (nine steps, 6.3% overall yield) is described in which the Pd II -mediated cyclization of the optically pure allenic amine 6 to giveExpand
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