• Screening a selection of analogues from this library against

  2024-09-28

  

  Screening a selection of analogues from this library against the panel of 26 kinases (16, 22, and 24 were screened at 30 μM due to poor solubility; 17 tested at 100 μM) generally demonstrated an increase in activity compared to sodium channel 3 (Fig. 3, Fig. 6). The benzamide analogue 16 demonstrat

• Fencilli et al reported derivatives of

  2024-09-28

  

  Fencilli et al. reported derivatives of PHA-680626 (15) which demonstrated strong anti-proliferative activity against large group of leukaemia cell lines including IM-resistant BAF3 cells expressing mutants like T315I, M351T and E255K. Decrease in Histone H3 phosphorylation led to induction of endo-

• With regard to the first question subcellular fractionation

  2024-09-28

  

  With regard to the first question, subcellular fractionation studies revealed that BDK and PPM1K are clearly detectable in both the mitochondrial and cytosolic subcellular fractions, thus making it possible for these enzymes to interact with both the BCKDH and ACL substrates. The preferential presen

• Secondly leptin has been shown to enhance aromatase

  2024-09-28

  

  Secondly, leptin has been shown to enhance aromatase mRNA expression, aromatase content and its enzymatic activity in epithelial breast cancer mecamylamine by inducing promoters II and I.3 via an enhanced binding of transcription activator protein 1 (AP-1) complex to specific DNA sites in the promo

• br Material and methods br Results br Discussion

  2024-09-28

  

  Material and methods Results Discussion Didox was originally created asa cytostatic drug to inhibit cancer cell proliferation by antagonizing RNR [11]. When used to target highly proliferative cells, Didox has extensive activity in vitro and in vivo. It has also been employed in clinical st

• The regulation of gene expression by glucocorticoids can be

  2024-09-28

  

  The regulation of gene expression by glucocorticoids can be mediated either by the canonical mechanism that involves the interaction of the glucocorticoid receptor (GR), a transcription factor activated by the hormone, with glucocorticoid response element (Ye et al., 2007), or by the non-canonical m

• Although the gene that encodes DHFR has been

  2024-09-28

  

  Although the gene that encodes DHFR has been strongly conserved during evolution, subtle differences in the active sites of bacterial, human and parasite N-Nonyldeoxynojirimycin have been exploited to develop DHFR inhibitors specific to particular pathogens 1, 3. For example, pyrimethamine and cyclo

• br Experimental procedures br Results br Discussion Our biop

  2024-09-28

  

  Experimental procedures Results Discussion Our biophysical and cellular analyses of mutant Aβ1–42 peptides support a role of the N-terminus of Aβ in peptide aggregation and toxicity. We demonstrate that double mutations constructed to humanize the rodent Aβ1–42 sequence result in a signific

• The decreased AR mediated response has been attributed to

  2024-09-28

  

  The decreased βAR-mediated response has been attributed to different mechanisms, including an attenuation of PKA activation, an impaired generation of cyclic AMP, a reduced receptor density, and a less efficient coupling to adenylyl-cyclase [10]. However, currently there is no single molecular or ce

• It is well known that the thymus plays an

  2024-09-27

  

  It is well known that the thymus plays an important function in the complex pathogenesis and perpetuation of MG. We compared resistin levels between patients with MG with or without thymoma and found that those with thymoma had higher levels than those without thymoma. It has been previously recogni

• Cy3 RNA mg Song et al reported series of triazolylsalicylami

  2024-09-27

  

  Song et al. reported series of 1,2,3-triazolylsalicylamide derivatives and screened over kinase panel and found compound 31 as most potent which inhibited Aurora-A, specifically with IC50 of 0.37 μM. Compound 31 was about 10-fold more active for Aurora-A than for Aurora-B (IC50 = 3.58 μM reported se

• br Genetic analysis of polarity complexes Model organisms

  2024-09-27

  

  Genetic analysis of polarity complexes Model organisms such as Caenorhabditis elegans and Drosophila melanogaster provide useful means of describing basic biological processes. They lend themselves particularly well to addressing some of the questions arising in this field because of their struct

• We have shown that an extensive region in SERBP

  2024-09-27

  

  We have shown that an extensive region in SERBP1 (amino acids 354 to 474, using co-ordinates based on the full-length isoform, Figs. 1a and 2) is necessary for it to interact with RACK1; since this region has substantial homology to the corresponding region of HABP1 (Fig. 3) it is a reasonable hypot

• Protein arrays provide a new approach

  2024-09-27

  

  Protein arrays provide a new approach for the identification of substrates for several protein-modifying enzymes. For example, protein kinase substrate identification, which constitutes an important aspect of pathway mapping because of the prevalence of these substrates in biological pathways. MacBe

• Pathological angiogenesis occurs when an imbalance of endoge

  2024-09-27

  

  Pathological angiogenesis occurs when an imbalance of endogenous proangiogenic and antiangiogenic factors occurs. Although the focus of angiogenesis-related drug development has been geared to the discovery of antiangiogenic compounds for use in pathologies where excessive angiogenesis occurs (cance

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