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br Methods br Results br
2019-08-08
Methods Results Discussion The lowest intra-CeA dose of R278995/CRA0450 that prevented the elevations in X-Gal formula reward thresholds associated with nicotine withdrawal was 0.05μg/side (0.1μg total bilateral dose). The total bilateral dose in the present study is 100 times lower than t
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It is not precisely known which
2019-08-08
It is not precisely known which of the intramolecular interactions created by the SH2 domain, the SH3–SH2 linker and the SH2–kinase linker are essential for the catalytic activity of Csk or how these interactions regulate Csk activity. Thus far it has been shown that site-directed mutagenesis of SH3
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Multiple sequence alignment of the proteins
2019-08-08
Multiple sequence alignment of the proteins in the DGAT1 sub-family shows that there are about 41 conserved amino INCB024360 analogue residues distributed over seven sequence motifs [74]. Unlike DGAT2, a large number of DGAT1 residues, including a majority of the conserved residues, are found in a
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The present review also summarizes the efforts that have
2019-08-08
The present review also summarizes the efforts that have been made to find new c-FMS inhibitors under clinical trial as given in the Table 1. These inhibitors may reduce the burdens of potency and side effects that have faced the scientists globally. ABT-869 41 was manufactured in Abbott laboratorie
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Protein kinase casein kinase CK comprises a family of highly
2019-08-08
Protein kinase casein kinase 1 (CK1) comprises a family of highly related, constitutively active serine/threonine protein kinases (reviewed by [15]). CK1 is involved in controlling a wide variety of different cellular events including protein turnover [16], [17], nuclear import [18] and the cellular
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atr inhibitor Nowadays it is possible to detect the AChE inh
2019-08-08
Nowadays it is possible to detect the AChE inhibitors by several methods such as gas chromatography-mass spectrometry [11], ion mobility spectrometry [12] and lab-on-chip devices [13,14]. However, almost all instrumental detection techniques that are able to conclusively determine the presence of th
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Another enzyme class that has emerged as a potential
2019-08-08
Another enzyme class that has emerged as a potential alternative to P450s are the so-called ‘unspecific peroxygenases’ (UPOs). They also contain a heme but are extracellularly expressed fungal enzymes that are often more stable than P450 monooxygenases. Importantly, UPOs use H2O2 instead of O2 as th
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The synthesis of compounds a and b are
2019-08-08
The synthesis of compounds 7a and 7b are outlined in Scheme 2. Compound 5 was obtained by di-tert-butyl pyrocarbonate protection of glycerol 4a. Then, compounds 6a and 6b were obtained by amination of the fluoride with a morpholino and dimethylamine, respectively. Target compounds 7a and 7b were obt
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br Conclusions and future perspectives It is now
2019-08-07
Conclusions and future perspectives It is now evident that selective ETA or nonselective endothelin receptor antagonism provides therapeutic potentials against a variety of cardiovascular diseases such as hypertension, PAH, and diabetic microvascular dysfunction (Fig. 1). However, PAH is currentl
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p and p which are downstream of pAkt and pERK
2019-08-07
p21 and p16, which are downstream of pAkt and pERK1/2, are tumor suppressors which induce cell senescence and EGTA arrest [[56], [57], [58]]. Inhibitors of pAkt or pERK1/2 can activate p21 and p16 and promote cell senescence and cell cycle arrest [11,12,[59], [60], [61]]. It is well known that p21
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As for the molecular mechanism Ferguson BD suggested that Ep
2019-08-07
As for the molecular mechanism, Ferguson BD suggested that EphB4/EphrinB2 stimulation induced topoisomerase I activity in small cell lung cancer cell lines. Treatment of Pertussis Toxin with EphrinB2/Fc induced topoisomerase activity as assessed by DNA relaxation in cells with high EphB4 expression
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Considering these reports and with the aim of further
2019-08-07
Considering these reports, and with the aim of further investigating the mechanism by which the cAMP-Epac/PKA pathway activates eNOS, we have performed imaging experiments evaluating the effect of drugs that increase cAMP or modify its signalling pathways (PKA or Epac activators and inhibitors) on b
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In conclusion our study has demonstrated that PGE stimulates
2019-08-07
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
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gsk-3 Introduction Collagen deposition is a common feature
2019-08-07
Introduction Collagen deposition is a common feature found in cancerous tissues and fibrotic organs/lesions. It is now well accepted that collagen deposition is not just a consequence of disease, but that it can also trigger a vicious cycle. Both chemical and physical signals elicited from collagen
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The positive correlation between ATG
2019-08-07
The positive correlation between ATG7 and DCTPP1 (TCGA data) suggested our hypothesis that DCTPP1 may affect the phenotype of prostate tumor, or maybe other types of tumors as well, through its role in autophagy. To test this hypothesis, we carried out western-blot experiments in which the ratios of
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