• Our previous high throughput screening HTS campaign using au

  2019-10-19

  

  Our previous high-throughput screening (HTS) campaign using automated, robust, and sensitive fluorescence based iMDK assay [10], [11] led to the identification of several EPAC specific inhibitors (ESIs), and was subsequently followed by extensive hit-to-lead optimizations [20], [21], [22], [23], [24

• In conclusion our study has

  2019-10-19

  

  In conclusion, our study has demonstrated that PGE2 stimulates expression of survivin in hepatocellular carcinoma cells. Although there are 4 subtypes of EP receptors, the EP1 receptor appears to be the predominant receptor that regulates PGE2-induced expression of survivin, mainly through trans-act

• Potential break through technology poised

  2019-10-19

  

  Potential break-through technology poised to overcome these above-mentioned limitations is that of the “substrate mediated enzyme prodrug therapy”, SMEPT (Fig. 1). Learning from the previously established enzyme prodrug therapies (EPT) and specifically the antibody-directed EPT (ADEPT) [12], develop

• We had earlier reported that collagen fibers

  2019-10-19

  

  We had earlier reported that collagen fibers with intact native banded structure were occasionally observed in the kinase-deficient, membrane-anchored DDR2 ECD (DDR2/-KD) samples; however, in our DDR1/ECD and DDR2/ECD samples, observation of native banded structure of collagen was far more infrequen

• br Phenotypic responses alkylation induced cell death

  2019-10-18

  

  Phenotypic responses: alkylation-induced cell death and mutagenesis E. coli alkB mutants were isolated in a screen for strains specifically sensitive to the cytotoxicity of MMS but not UV-irradiation. This was the first indication that the AlkB protein is a primary cellular defence against alkyla

• Although DGK is a lipid modulating enzyme the

  2019-10-18

  

  Although DGKγ is a lipid-modulating enzyme, the role of DGKγ in integral cell metabolism has not been reported. We found that DGKγ made a difference on cell metabolism profile in HCC cells, which may be caused partially by the downregulation of GLUT1. Glucose is a major source of energy, and decreas

• Our results suggest that formation of DDR b

  2019-10-18

  

  Our results suggest that formation of DDR1b clusters may be important for and precede receptor phosphorylation. Indeed, while DDR1b clustering was readily detected (by YFP signal) 30 min after collagen administration, phosphorylated DDR1 species at Y513 (present in the IJXM) were evident after 4 h o

• Altogether we have shown the presence of fully methylated

  2019-10-18

  

  Altogether we have shown the presence of fully methylated DAPK fragments in serum of ovarian cancer patients but also of women with uterine leiomyoma. This indicates the prerequisite for the analysis of not only healthy controls but also of women with other frequent non-cancer disease for the valida

• N fowleri enters the host through

  2019-10-18

  

  N. fowleri enters the host through the nasal cavity and travels via the olfactory nerve into the CVT 10216 pathway where it causes PAM (Visvesvara and Stehr-Green, 1990). The ameba most commonly infects healthy young adults and children and is able to evade the immune system but also elicits extensi

• During the course of our research on mGlu

  2019-10-18

  

  During the course of our research on mGlu PAMs,, the hydroxyacetophenone scaffold was found to possess dual mGlu PAM and CysLT1 antagonism activity, presumably as orthosteric antagonist (). There is currently an increasing interest in drug discovery to explore multitarget drugs or polypharmacology

• In the present study it was

  2019-10-18

  

  In the present study, it was found that HepG2, H4IIE and LMH cells were inclined to remove S-metalaxyl and lead to decrease of ERs of metalaxyl, while L8824 cells were inclined to attenuate R-metalaxyl and resulted in an inverse shift of ER. These findings indicate the enantioselective accumulation

• Our structures also provide new insights into

  2019-10-18

  

  Our structures also provide new insights into CRTH2 drug development. The ligand binding pocket revealed by our structures comprises many aromatic residues and a few polar residues at the distal end. Correspondingly, most CRTH2 antagonists share a similar structural feature characterized by an aceta

• Our results indicate that C CoA is formed

  2019-10-18

  

  Our results indicate that C75-CoA is formed in the hypothalamus following stereotaxic injection of C75. Inhibition of hypothalamic CPT1 by C75-CoA in vivo, as seen in our experiments, is independent of the putative inhibition by malonyl-CoA, which may be formed after the action of C75 either on FAS

• These cognitive deficits may suggest that cognitive therapy

  2019-10-18

  

  These cognitive deficits may suggest that cognitive therapy and pharmacotherapy for gambling behavior may ultimately wish to consider genotyping as a means of better targeting treatment approaches. If core cognitive deficits are shown consistently in certain subgroups of gamblers based on genotype,

• In the current study we monitored

  2019-10-18

  

  In the current study, we monitored different groups at risk for CMV reactivation. Similar to the findings from other groups, we observed CMV-reactivations with high-level viremia mostly during the first three months after alloHSCT only in the (D−/R+) and (D+/R+) group [[23], [24]]. Increasing IFN‐γ

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