• To develop novel EPAC inhibitors Zhou and

  2020-03-06

  

  To develop novel EPAC inhibitors, Zhou and co-workers optimized the HTS hit as the chemical lead. After modifications of the substituents on the phenyl ring or C6-position of compound , compound () was identified to be the more potent compound in this series with an IC value of 4.0µM (EPAC2). Dock

• GSK2194069 Our observation that nuclear but not cytoplasmic

  2020-03-06

  

  Our observation that nuclear, but not cytoplasmic EP4 expression is associated with different outcomes is interesting. In breast cancer, using the same methods, we did not detect EP4 in the nucleus of malignant GSK2194069 whereas cytoplasmic EP4 was commonly observed [13]. While G protein-coupled

• The liposomes as a FDA approved drug delivery carrier have

  2020-03-06

  

  The liposomes, as a FDA-approved drug delivery carrier, have been widely utilized for drug delivery [32], [33], [34]. Liposomes are defined as self-assembled vesicles, which are composed of one or multiple concentric lipid bilayers and enclose an aqueous core. The advantages of utilizing liposomes a

• nop receptor To analyze EBI expression and its function in T

  2020-03-06

  

  To analyze EBI2 expression and its function in T cells in vivo, we created an EGFP reporter/knockout mouse strain, termed EBI2EGFP. This mouse strain in heterozygous configuration allows for a systematic analysis of the expression of EBI2 in distinct cell types in steady-state and under inflammatory

• These studies suggested that PV PVH might promote bone forma

  2020-03-06

  

  These studies suggested that PV/PVH might promote bone formation activities and/or inhibit bone resorption activities probably due to its anti-inflammation activity; however, the underlying mechanism remained unknown. Furthermore, it is unclear if PVH shows better activity than that of PV; this is i

• As for antiviral activity eight out of synthesized compounds

  2020-03-06

  

  As for antiviral activity, eight out of 23 synthesized compounds were active against influenza B virus with EC50 values in the range of 0.19–39 μM. Four of the eight influenza B hits were active against influenza A and two were also active against RSV (4 and 6, EC50 = 0.40 and 1.8 μM, respectively).

• br DDR role in kidney Thirty eight

  2020-03-06

  

  DDR1 role in kidney Thirty-eight papers are reported in PubMed upon the keyword search “DDR1 AND kidney”. Careful examination of those papers shows that only 31 are related to DDR1\'s role in glomerulosclerosis and renal fibrosis, 24 of those being research and the rest review articles. Since the

• The aim of this study was to

  2020-03-06

  

  The aim of this study was to evaluate the role of aberrant methylation of promoter regions of tumor suppressor genes in the clonal evolution from MGUS to MM. Thus, we analyzed in MGUS, SMM, and symptomatic MM patients, the methylation status of 4 genes—p15, p16, p53, and DAPK—whose promoter hypermet

• JLK 6 br Acknowledgements We thank Jeffrey D Konowalchuk and

  2020-03-06

  

  Acknowledgements We thank Jeffrey D. Konowalchuk and John Sony Robbins for their technical assistance. This work was supported by Natural Sciences and Engineering Research Council of Canada (NSERC) grants to DRB (RGPIN-2013-355303) and MB (RGPIN-2014-96395). AMR was supported by NSERC Vanier Doct

• Experiment Blunted fear potentiated startle due to

  2020-03-06

  

  Experiment 2: Blunted fear-potentiated startle due to deficient fear acquisition. SERT+/+ and SERT+/− showed significant acquisition of the cue-shock association, whereas SERT−/− did not (trial×genotype interaction: F2,50=3.3, p and F2,106=36.6, pEmpagliflozin of fear-potentiated startle. Acquisit

• The regression also revealed a significant

  2020-03-06

  

  The regression also revealed a significant association between admission selectivity (SELECT) and exam pass rate (PASS%) (p GSK461364 synthesis serve as an indicator of a student’s ability to learn and their aptitude for academic success. These same qualities likely enable more selective schools to

• The substitution of serine by

  2020-03-06

  

  The substitution of serine 185 by an alanine led to an increase of EGF-R stabilization along with a better binding of PRK1, a RhoB effector described to be involved in EGF-R intracellular traffic. Overall these data indicated that the phosphate group on serine 185 impaired its binding to the effecto

• As the primary model we selected LDL

  2020-03-06

  

  As the primary model we selected LDL-receptor knockout mice because these resemble the human plasma lipoprotein profile more closely. Currently, genetic models with reduced milk cholesterol content, which mimic cholesterol-free formula feeding, are unavailable. Thus, instead of modifying milk choles

• Fmoc-D-Phe(4-Cl)-OH receptor Overall we found that all hormo

  2020-03-06

  

  Overall, we found that all hormone treatment groups were able to learn spatial working and reference memory tasks, as shown by their performance across days on the WRAM (days 2–12, collapsed across the 4 trials) and the MWM (days 1–5, collapsed across the 4 trials). During the acquisition phase of

• PD 151746 In summary we have identified

  2020-03-06

  

  In summary, we have identified a series of amides as ERRγ agonists with suitable potency for further development. Our SAR studies of this chemotype identified SR19881 as the most potent full agonist of ERRγ with an EC=0.39 μM in a binding assay and an EC=4.7 μM in a cell-based assay. SR19881 was als

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