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Apigenin Blocks Lipopolysaccharide-Induced Lethality In Vivo and Proinflammatory Cytokines Expression by Inactivating NF-κB through the Suppression of p65 Phosphorylation
TLDR
It is demonstrated that apigenin inhibits the production of proinflammatory cytokines IL-1β, IL-8, and TNF in LPS-stimulated human monocytes and mouse macrophages, and this findings suggest a molecular mechanism by which Apigenin suppresses inflammation and modulates the immune response in vivo. Expand
Apigenin-induced-apoptosis is mediated by the activation of PKCdelta and caspases in leukemia cells.
TLDR
Results indicate that this flavonoid provides selective activity to promote caspase-dependent-apoptosis of leukemia cells and uncover an essential role of PKCdelta during the induction of apoptosis by apigenin. Expand
The novel plant-derived agent silvestrol has B-cell selective activity in chronic lymphocytic leukemia and acute lymphoblastic leukemia in vitro and in vivo.
TLDR
Data indicate silvestrol has efficacy against B cells in vitro and in vivo and identify translational inhibition as a potential therapeutic target in B-cell leukemias. Expand
First three-dimensional structure of Toxoplasma gondii thymidylate synthase-dihydrofolate reductase: insights for catalysis, interdomain interactions, and substrate channeling.
TLDR
Structural and kinetic studies reveal unique, functional regions on the T. gondii TS-DHFR enzyme that may be targeted for inhibition, thus paving the way for designing species specific inhibitors. Expand
Subunit interface residues of glutathione S-transferase A1-1 that are important in the monomer-dimer equilibrium.
TLDR
Phe52 and Arg69 are the major determinants of dimer formation and a single mutation at either position substantially hinders dimerization, and the use of a mutant glutathione S-transferase which retains activity yet has a greatly weakened tendency to dimerize (such as R69E) may be advantageous for certain applications of GST fusion proteins. Expand
Enhanced HIV-1 replication in retinoid-treated monocytes. Retinoid effects mediated through mechanisms related to cell differentiation and to a direct transcriptional action on viral gene expression.
TLDR
It is shown that retinoic acid significantly increased HIV replication in monocytes through mechanisms related to cell differentiation and to a direct transcriptional effect on viral gene expression. Expand
Arsenic trioxide and ascorbic acid demonstrate promising activity against primary human CLL cells in vitro.
TLDR
Hu1D 10-mediated cell death was enhanced with ATO and ascorbic acid, thus justifying potential combination of ATO/arsenic trioxide therapy with antibodies such as Hu1D10 that also cause accumulation of ROS. Expand
Affinity Labeling of Rat Glutathione S-Transferase Isozyme 1-1 by 17β-Iodoacetoxy-estradiol-3-sulfate*
  • M. Vargo, R. Colman
  • Medicine, Chemistry
  • The Journal of Biological Chemistry
  • 19 January 2001
TLDR
Results indicate that 17β-iodoacetoxy-estradiol-3-sulfate reacts as an affinity label of the nonsubstrate steroid site rather than of the substrate sites occupied by Δ5-androstene-3,17-dione or glutathione, and suggest that Cys17 is the only enzymic amino acid modified. Expand
Nonconserved residues Ala287 and Ser290 of the Cryptosporidium hominis thymidylate synthase domain facilitate its rapid rate of catalysis.
TLDR
The crystal structure of ligand-bound S290G mutant enzyme is determined, which shows that the primary effect of the mutation is an increase in the distance between the TS ligands, the first evidence explaining the unusually fast TS rate in C. hominis. Expand
Novel non-active site inhibitor of Cryptosporidium hominis TS-DHFR identified by a virtual screen.
TLDR
A novel allosteric pocket amenable to inhibitor targeting is described, and a lead compound is identified with which to move towards potent, selective inhibitors of ChTS-DHFR. Expand
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