• Jesus et al discovered a new series

  2024-02-29

  

  Jesus et al. discovered a new series of azaindole as Aurora inhibitors through various modification of GSK1070916 (47). They synthesized series from modification of the GSK1070916 and evaluated for in-vitro Aurora-B/INCENP and Aurora-A/TPX2 inhibition assays. Modified s6 kinase 48 and 49 showed IC5

• In this study significant reduction

  2024-02-29

  

  In this study, significant reduction in the HCO3− content in sham-operated and testosterone-treated rats following bafilomycin A1 administration suggested that V-ATPase could be involved in mediating the decrease in vas deferens fluid HCO3− content, most probably due to the increase in H+ secretion

• Regulators of the DDR have therefore become attractive

  2024-02-29

  

  Regulators of the DDR have therefore become attractive targets for cancer therapy primarily through two potential approaches. First, to be used as chemo- or radiosensitisers to increase the effectiveness of standard genotoxic treatments and to help prevent or overcome the development of resistance.

• Although the LB domains of mGlu receptors

  2024-02-29

  

  Although the LB2 domains of mGlu receptors have not been shown to form an extensive interface during activation, they do draw closer to each other, as demonstrated in crystal structures (Kunishima et al., 2000, Muto et al., 2007, Tsuchiya et al., 2002) and by FRET analysis (Doumazane et al., 2013, V

• The enzyme Arginase ARG plays a

  2024-02-29

  

  The enzyme Arginase 1 (ARG1) plays a role in the hepatic urea cycle by hydrolyzing L-arginine to L-ornithine and urea [13]. In the context of macrophages and MDSCs, ARG1 expression redirects L-arginine metabolism to abolish cytotoxic nitric oxide production [14], suppress T-cell function [15], [16],

• Recently competitive inhibitors of arginase have

  2024-02-29

  

  Recently, competitive inhibitors of arginase have been developed which have greater specificity for the enzyme. Initial development of these compounds involved determination of the crystal structure of arginase. Christianson and colleagues found that a binuclear manganese cluster was required for ca

• Arginase deficiency is a rare

  2024-02-29

  

  Arginase deficiency is a rare urea cycle disorder with hyperargininemia and profound neurological impairment as hallmark features. Arginase-1-deficient mouse models have been created, and they exhibit a profound lethal phenotype approximately 2 weeks after birth in the global knockout (KO) mice or a

• NO is an important mediator for maintaining

  2024-02-29

  

  NO is an important mediator for maintaining bone integrity since it plays a role in the bone remodeling process. It was shown that mechanical strain and shear stress induce NO synthesis in osteoblasts and osteocytes (van't Hof & Stuart, 2001). It was reported that mechanical loading influences its a

• br Experimental section br Abbreviations PSA

  2024-02-29

  

  Experimental section Abbreviations PSA, puromycin–sensitive aminopeptidase; APN, aminopeptidase N; AML, acute myeloid Leukemia; ALL, acute lymphoblastic leukemia; AADR, amino Atglistatin deprivation response; PAN, puromycin aminonucleoside; DCC, dicyclohexyl carbodiimide; NHS, N–hydroxy succi

• br Discussion Missense mutations transversions of the first

  2024-02-29

  

  Discussion Missense mutations (transversions) of the first nucleotide of the phenylalanine NG25 at position 1174 (F1174) of the anaplastic lymphoma kinase gene can result in substitutions to leucine or valine (F1174L/V) while missense mutation (transversion) of the second nucleotide of the pheny

• Alectinib is a second generation ALK antagonist that

  2024-02-29

  

  Alectinib is a second generation ALK antagonist that is built upon a 9-ethyl-6, 6-dimethyl-11-oxo benzo[b]carbazole scaffold (Fig. 5C) [58]. This drug is effective against the ALK L1196M gatekeeper mutation along with C1156Y and F1174L mutations [7]. The 11-oxo group of the drug forms a Xylazine HCl

• We found evidence of the interaction between AR and hemiacet

  2024-02-29

  

  We found evidence of the interaction between AR and hemiacetals by evaluating the effect of glucose on l-idose reduction. l-idose was recently proposed as the best AR substrate able to mimic glucose [38]. This aldose is structurally very closely related to d-glucose, from which it differs only in th

• We next considered the effect of

  2024-02-29

  

  We next considered the effect of alkyl chain length on the inhibitory activity. As can be seen from , it is obvious that there is no proportional relationship between the methylene chain length and activity. The activity decreased when the chain length increased from 1 to 3 and increased with elonga

• br Translational Considerations Targeting the AHR Pathway

  2024-02-29

  

  Translational Considerations Targeting the AHR Pathway Modulating AHR function offers exciting therapeutic potential in host immunity and inflammation. However, the emerging concept of AHR function in a cell type-specific manner, combined with differences between AHR activation in cell culture in

• br Translational Considerations Targeting the AHR Pathway

  2024-02-29

  

  Translational Considerations Targeting the AHR Pathway Modulating AHR function offers exciting therapeutic potential in host immunity and inflammation. However, the emerging concept of AHR function in a cell type-specific manner, combined with differences between AHR activation in cell culture in

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