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As previously stated the most unexpected finding from
2020-08-26

As previously stated, the most unexpected finding from this series of compounds was the identification of a dimethyl isoxazole side chain that gave dramatically improved binding over the parent compounds. Holding this piece of the molecule constant, a series of analogs were made to further understan
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We next examined the effects of substituents around
2020-08-26

We next examined the effects of substituents around the carboxylic dna-pk pathway moiety on CRTH2 binding (Table 4). The carboxylic acid moiety shared by the representative CRTH2 antagonists and is essential for the CRTH2 activity. Germinal dimethylation of the methylene moiety next to the carboxyl
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Finally unilateral microinjection of CP Astressin B CP CRF o
2020-08-26

Finally, unilateral microinjection of CP-376395, Astressin 2B, CP-376395 + CRF or ASTR 2B + CRF into the BLA (Fig. 3A) or CeA (Fig. 3B) did not significantly alter spontaneous motor activity in the open field test (F4,24 = 0.148, P > 0.05; F4,29 = 0.290, P > 0.05 in the BLA and CeA, respectively, AN
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In summary we have identified a series of amides as
2020-08-26

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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Because of the lack of sequence current knowledge on the
2020-08-26

Because of the lack of sequence, current knowledge on the cellular regulation of CoA-IT is scarce. However, recent work has suggested an interesting new role for CoA-IT in regulating the extent of the AA mobilization response in primed macrophages. Bacterial lipopolysaccharide (LPS) is a poor trigge
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This pre GC B cell differentiation deficiency caused
2020-08-26

This pre-GC B cell differentiation deficiency caused by RD2 loss of function was explained at least in part by the finding that the BCL6 RD2 domain is required to repress expression of the key migration factors GRP183 and S1PR1. Downregulation of GRP183 is critically important for B cell migration i
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With respect to the muscle compartment only low
2020-08-26

With respect to the muscle compartment, only low protein expression of ASB9 has been detected in healthy human skeletal muscle [as reported in the Human Protein Atlas (HPA)], whereas high levels of Asb5 protein expression are detected in mammalian skeletal muscle, which appears to be important in th
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br Acknowledgments This work was
2020-08-26

Acknowledgments This work was supported by a grant from the National Center for GM Crops (PJ008152) of the Next Generation BioGreen 21 Program funded by the Rural Development Administration, Republic of Korea, to W.T.K. Introduction Ubiquitin (Ub) has been considered as one of the most import
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br General mechanism of NHEJ NHEJ is an
2020-08-26

General mechanism of NHEJ NHEJ is an amazingly versatile pathway that can select specific enzymes which bind to, process, and finally mediate the direct re-ligation of a wide range of DSBs including those that are complex, have incompatible ends, and contain TUG 891 synthesis damages [7], [8], [9
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AMPHs facilitate dopamine release which further triggers dop
2020-08-26

AMPHs facilitate dopamine release, which further triggers dopamine depletion [72]. Indeed, we observed that repeated treatment of MPA significantly inhibited TH-, DAT-, and VMAT-2 levels. Since DAT and VMAT-2 are important for dopaminergic terminal markers [10], their decreases suggest that MPA-indu
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The present results are potentially relevant for understandi
2020-08-24

The present results are potentially relevant for understanding anxiety disorders and their treatment. Both COMT Val158Met (Lonsdorf and Kalisch, 2011, Montag et al., 2012) and neuroticism/anxiety (Clark et al., 1994, Mineka et al., 1998, Weinstock and Whisman, 2006) have been linked to the prevalenc
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This study focused on NPC L because it is
2020-08-24

This study focused on NPC1L1 because it is critical for intestinal alpha-Endorphin receptor of both dietary and biliary cholesterol.1, 7, 8 Overall, regulation in the intestine of cholesterol, BAs, and lipids by FGF19 and SHP may involve the combined actions of regulation of other genes that were i
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The underlying assumption of consolidation re consolidation
2020-08-24

The underlying assumption of consolidation/re-consolidation is that the WAY-262611 activity initiated during the acquisition trial/re-consolidation trial continues to persist briefly after completion of the trial and it is during this post-trial period that immediate post-trial treatments can influ
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Although high concentrations of SCR
2020-08-24

Although high concentrations of SCR7-G and SCR7-R inhibited LigIV as reported [11], the SCR7 derivatives were more effective inhibitors of LigIIIα and, in particular, LigI. Although it is possible that differences in the DNA substrate underlie this discrepancy, it appears more likely that this refle
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Another notable finding in this study is
2020-08-24

Another notable finding in this study is that Cbl-b-mediated ubiquitination accelerates the degradation of phosphorylated DDR2. Cbl family has been documented to facilitate RTK degradation either in proteasome through K48-linked poly-ubiquitination or in lysosome through mono-, multiple mono- and K6
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