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The aniline R group was extensively explored and a large
2020-04-17
The aniline R2 group was extensively explored and a large variety of substitution was tolerated at several positions on the aryl ring (). Notably, substitution at the 3-position often gave increased potency. Increasing lipophilic bulk at this position gave increasing potency within an ether series (
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br Enzymes involved in microbial
2020-04-17
Enzymes involved in microbial steroid degradation are generally not expressed constitutively, but they are upregulated depending on which steroid substrates are present [17,81]. Thus, a cell-free extract prepared from testosterone-adapted C. testosteroni ATCC 11996 cells displayed a 1(2)-dehydroge
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The presence of external NAD P H dehydrogenases
2020-04-17
The presence of external NAD(P)H dehydrogenases (NDE) on the outer surface of the inner mitochondrial membrane enables the mitochondria to oxidize cytosolic NAD(P)H (Moller 2001). A porin (a voltage-dependent anion-selective channel, VDAC) that is abundant in the outer mitochondrial membrane permits
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The role of DDR in glomerular injury has
2020-04-17
The role of DDR1 in glomerular injury has been then further studied by the Chatziantoniou group in experimentally-induced crescentic glomerulonephritis, by injection of alloimmune sheep nephrotoxic serum (NTS) [54]. Glomerulonephritis produced a 17-fold increase of DDR1 expression, predominantly in
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The aberrant methylation of genes that suppress
2020-04-17
The aberrant methylation of genes that suppress tumorigenesis appears to occur early in tumor development and increase progressively, eventually leading to the malignant phenotype [35]. Genes involved in every step of tumorigenesis can be silenced by this epigenetic mechanism. Hypermethylation of pr
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Next we evaluated the therapeutic potential of compound usin
2020-04-17
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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In a cell based functional assay
2020-04-17
In a cell-based functional assay, the antagonist properties of were assessed by measuring inhibition of CRF-stimulated cyclic adenosine monophosphate (cAMP) production in human Y-79 retinoblastoma cells. produced a concentration-dependent inhibition of CRF (1nM)-induced cAMP production with an IC
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Regarding the effects of CRF on anxiety
2020-04-17
Regarding the effects of CRF on anxiety, Sahuque et al. (2006) have demonstrated that this neuropeptide also enhances anxiety when injected into the bed nucleus of the stria terminalis (BNST), a streptozotocin structure that has also been related to defensive behavior (Casada and Dafny, 1991, Chen
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br Experimental methods br Results and
2020-04-17
Experimental methods Results and discussion Conclusions Here we describe the first reported method for high-yield KC7F2 mg of active and soluble mature CPG2 (in the absence of the leader peptide) and its individual catalytic and dimerization domains in E. coli. Such a method is of key impor
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br Tests and measurements We used a set
2020-04-17
Tests and measurements We used a set of FPGA cores for all tests and measurements. Firstly, the control circuit for the Controlled Current Limiter illustrates the proposed TMR method. The circuit contains a D-Register to enable or disable the power to the protected device, a counter, which is use
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Several extragenic cot ts suppressors have been identified
2020-04-17
Several extragenic cot-1 (ts) suppressors have been identified. Among them, cytoplasmic dynein, dynactin, and nuclear distribution mutants of N. crassa, as well as an additional gene gul-1 (NCU01197), have been shown to have genetic interactions with cot-1 (Bruno et al., 1996, Seiler et al., 2006, T
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br Results and discussion br Conclusions We
2020-04-17
Results and discussion Conclusions We have developed a method to produce wildtype and mutant Ric-8A proteins from E. coli that can be phosphorylated at the regulatory protein kinase CK2 phosphosites to near homogeneity. The phosphorylation status and activity of the purified Ric-8A proteins wa
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Therefore the SPH algorithm in AUTODYN
2020-04-17
Therefore, the SPH algorithm in AUTODYN-3D™ was used to simulate the experiment in Ref. [5] to verify the credibility of the numerical simulation method by results that could be measured accurately. Then the verified numerical simulation method was used to simulate BAD generated by RHA subjected to
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Several studies have indicated that ICT induces activation
2020-04-16
Several studies have indicated that ICT induces activation of ERK and p38 kinase in a variety of cells. The ERK pathway was involved in and partly contributed to the neuroprotective effects in rat neuronal Fenoprofen Calcium australia [14] and anticancer effects in several cancer cells [5], [7], [8]
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Recent studies from the literature have identified
2020-04-16
Recent studies from the literature have identified new hydralazine hcl 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
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