In 2011, AstraZeneca embarked on a major revision of its research and development (R&D)
strategy with the aim of improving R&D productivity, which was below industry averages in …

Malate dehydrogenases are widely distributed and alignment of the amino acid sequences
show that the enzyme has diverged into 2 main phylogenetic groups. Multiple amino acid …

Nitric oxide synthase (NOS) enzymes synthesize nitric oxide, a signal for vasodilatation and
neurotransmission at low concentrations and a defensive cytotoxin at higher concentrations. …

In normal physiologic responses to injury and infection, inflammatory cells enter tissue and
sites of inflammation through a chemotactic process regulated by several families of proteins, …

The discovery of a novel class of nitric oxide synthase (NOS) inhibitors, 2-substituted 1,2-dihydro-4-quinazolinamines,
and the related 4‘-aminospiro[piperidine-4,2‘(1‘H)-quinazolin]-4‘-…

The chemokine receptors CXCR1 and CXCR2 are G-protein-coupled receptors (GPCRs)
implicated in mediating cellular functions associated with the inflammatory response. Potent …

The malate dehydrogenase from Escherichia coli has been specifically altered at a single
amino acid residue by using site-directed mutagenesis. The conserved Arg residue at amino …

4-Methylaminopyridine (4-MAP) (5) is a potent but nonselective nitric oxide synthase (NOS)
inhibitor. While simple N-methylation in this series results in poor activity, more elaborate N-…

… Author links open overlay panel David R. Cheshire a , Anders Åberg d , Gunilla MK
Andersson d , Glen Andrews b , Haydn G. Beaton a , Timothy N. … Cooper a , David Cox a …

3-Phenyl-3, 4-dihydro-1-isoquinolinamine is a weak inhibitor of iNOS and nNOS. Structural
variation of 5a results in inhibitors with a range of potency and selectivity for the NOS …