• The authors identified inhibitors of SUMOylation using two a

  2019-07-15

  

  The authors identified inhibitors of SUMOylation using two assays to monitor the conjugation of SUMO1 to RanGAP1 by E1 and E2 enzymes: a fluorescence resonance energy transfer (FRET) primary screen that evaluated over 250,000 compounds and a chemiluminescence secondary screen. A counter screen was u

• br STAR Methods br Acknowledgments We are grateful to

  2019-07-13

  

  STAR★Methods Acknowledgments We are grateful to Amaia Lujambio, James Fagin, and Ramon Parsons for providing cell lines and Evripidis Gavathiotis for critical reading of the manuscript. We would like to thank Saboor Hekmaty for providing expertise with RNA-seq analysis. P.I.P. would like to ac

• br Experimental section br Acknowledgments This work was sup

  2019-07-13

  

  Experimental section Acknowledgments This work was supported by the National Natural Science Foundation of China (NSFC, Grant No. 81573285 and No. 81602965), the Natural Science Basic Research Plan in Shaanxi Province of China (Program No. 2018JM7071 and No. 2017JQ8002), and the Fundamental Re

• br Materials and methods br Result and discussion

  2019-07-13

  

  Materials and methods Result and discussion qRT-PCR was utilized to explore the effect of acetamizuril on the mRNA level of enolase. The results were analyzed according to the Livak 2−ΔΔCT method (Schmittgen and Livak, 2008): the mean CT of the enolase in treated and untreated samples was 29.8

• When six chemical inhibitors were incubated with TRB

  2019-07-13

  

  When six chemical inhibitors were incubated with TRB or TRC and human liver microsomal preparation, HLM2, the results showed that ketoconazole (a CYP3A4 inhibitor) was very effective in inhibiting 4β-C hydroxylation of TRB and TR, whereas sulfaphenazole (a CYP2C9 inhibitor) and quinidine (a CYP2D6 i

• All known vertebrate TRIMs are categorized in distinct

  2019-07-13

  

  All known vertebrate TRIMs are categorized in 11 distinct subclasses depending on the types of domains present at their carboxyl-terminals (Fig. 3) [29], [35]. Beyond conserved N-terminal domains, it is the C-terminal that provides specificity of interactions with other proteins. The subclass IV for

• br Conclusions In conclusion we identified

  2019-07-13

  

  Conclusions In conclusion, we identified and overexpressed DGAT2 in fast growing, oleaginous N. oceanica for the first time. The engineered N. oceanica overexpressing DGAT2 resulted in enhanced neutral lipid accumulation and altered fatty Sulbactam molecular composition. Altogether, our findings

• A number of immune relevant genes have

  2019-07-13

  

  A number of immune-relevant genes have been studied to explore the immunologic mechanisms in large yellow croakers; however, the chemokine receptor CXCR family has never been studied in this organism. Chemokines are a large superfamily of chemotactic cytokines that are utilized to direct the traffic

• br Materials and methods br Results Recombinant N

  2019-07-13

  

  Materials and methods Results Recombinant, N-terminally His6-tagged vCPH was purified to near homogeneity via a modification of the reported procedure and its identity confirmed by intact protein mass spectrometry (Supplementary Fig. 1). As reported, vCPH catalysed two hydroxylations of a PAPK

• br Progestogens and venous thromboembolism clinical data

  2019-07-13

  

  Progestogens and venous thromboembolism: clinical data Progestogens and haemostatis: biological studies For many years, the effect of HT on haemostatis has been largely investigated in observational studies as well as in high evidence level studies among users of oral and transdermal estrogens

• While previously reported optimizations on compound focused

  2019-07-13

  

  While previously reported optimizations on Pexidartinib focused on the phenyl ring A () and substituents on isoxazole ring, other alternatives to replace isoxazole ring were never explored. Herein, we propose to replace the isoxazole with its bioisosteric substituted phenyl ring B () to explore ne

• br Introduction Our understanding of how ligands

  2019-07-13

  

  Introduction Our understanding of how ligands interact with G protein coupled receptors is evolving, particularly the recognition that some have the ability to preferentially activate a subset of intracellular signalling cascades – so called pathway biased ligands [1]. Additionally, it is now acc

• Recent studies from the literature have identified new

  2019-07-12

  

  Recent studies from the literature have identified new pten inhibitor of antiviral agents able to target diverse host factors indispensable for efficient virus replication: as an example, the human DEAD-box polypeptide 3 (DDX3) inhibitor, 1-[4-(4-methyl-1H-1,2,3-triazol-1-yl)phenyl]-3-o-tolylurea (1

• nadph oxidase RDH belongs to C family of the short chain deh

  2019-07-12

  

  RDH10 belongs to 16C family of the short-chain dehydrogenase/reductase (SDRs) superfamily of proteins [12], [13]. Notably, in human genome adjacent to the gene encoding RDH10 on chromosome 8 are located two other genes encoding members of the SDR16C family: retinol dehydrogenase epidermal 2 (RDHE2,

• Next we evaluated the therapeutic potential of compound usin

  2019-07-12

  

  Next, we evaluated the therapeutic potential of compound () using the mouse model of collagen-induced arthritis (CIA model), which is the pathological model for RA. Consequently, oral once-daily dosing of 3 mg/kg reduced the overall progression of the clinical score, including inflammation and bone

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