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Substitutions on the benzene ring of the
2020-08-12
Substitutions on the benzene ring of the phenyl acetic ω-Agatoxin TK moiety were evaluated to study their effect on DP and CRTH2 selectivity (). Compound has strong affinity for CRTH2, but it only has moderate affinity for DP. Small substitutions such as methoxy () and fluorine () next to the arylox
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The Lysine mutant is located in the tail region of
2020-08-11
The Lysine429 mutant is located in the tail region of 5-HT2A, which is predicted to be unstructured. This region has been shown to interact, in vitro, with PSD95 and leads to differences in signaling (Xia et al., 2003). The ASK motif, a component of the tail region, is also important for regulation
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br Conclusion New series of thiazolo d pyridazine
2020-08-11
Conclusion New series of thiazolo[4,5-d]pyridazine and imidazo[2′,1′:2,3]thiazolo[4,5-d]pyridazine were designed and synthesized using thiazole as scaffold based on its previously observed activity as DHFR inhibitor. Compounds 13 and 43 (Fig. 9) proved to be the most active DHFR inhibitors with I
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protein kinase Six substrate recognition sites SRS SRS have
2020-08-11
Six substrate recognition sites (SRS1-SRS6) have been identified at positions 102-123, 204-209, 238-244, 301-319, 374-382 and 483-492 (Table 2, underlined residues) based on Gotoh\'s proposal [30]. CYP3A163 displays the similar characteristic long sequences between helices F and G presenting two add
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Several in vivo human studies have produced
2020-08-11
Several in vivo human studies have produced conflicting results for evaluating the inhibition of OCs on the metabolism of CYP3A substrates. Balogh et al. [12] demonstrated an approximately 25% inhibition of CYP3A activities in vivo after the administration of an OC containing 30μg of ethinylestradio
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Another novel finding of our
2020-08-11
Another novel finding of our study was that the global 5 hmC was down-regulated and was associated with a substantial reduction of TET expression in the PE placentas compared with the controls. The decreased global 5 hmC level was consistent with the increased global 5 mC level in the preeclamptic p
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daminozide synthesis Allele specific methylation has been ob
2020-08-11
Allele-specific methylation has been observed in CpG islands of imprinted genes.27, 32 In the present study, however, methylation of CpG1 was specific to ALL daminozide synthesis and occurred in the leukemia cells of 28% of children with ALL, but it was not found in normal leukocytes from the same p
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In general accurate results for
2020-08-11
In general, accurate results for the prediction of the solubility in scCO2 + cosolvents using the CPA-EoS were verified. ALD values for each solute (Table 1) varied from 0.04 to 1.5. Few solutes, such as lauric acid, myristic acid, hydroquinone and salicylic acid, presented the highest ALD values. A
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Retigabine dihydrochloride Neuropsychological studies of adu
2020-08-11
Neuropsychological studies of adults with problem gambling indicate impairments in many cognitive areas including inhibition, working memory, decision-making, cognitive flexibility, and executive planning (Ledgerwood et al., 2012, Goudriaan et al., 2006). Dopamine is a neurotransmitter that regulate
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The major concern of PDE I
2020-08-11
The major concern of PDE-5-I use in liver cirrhosis is the potentially harmful effect on systemic blood pressure. Data of clinical studies are conflicting [27], [30], [31], [32], but available patient details suggest that in advanced liver cirrhosis, PDE-5-Is lower systemic blood pressure to a great
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The objective of the present work is
2020-08-11
The objective of the present work is to search for the optimum blend when 12.5–50% metakaolin is substituted by RHA and reacted with 10 M sodium hydroxide solution to produce geopolymers. It was hypothesized that the amorphous 1478 from RHA will increase the Si/Al ratio of the mix and in situ react
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Fusion genes are formed as the
2020-08-11
Fusion genes are formed as the result of either structural chromosomal rearrangement including, primarily, translocation, inversion, amplification and deletion, or non-structural aberrations caused by cis- and trans-splicing or transcriptional read-through. Such events are known to play important ro
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ERK and p MAPK signaling pathways
2020-08-11
ERK and p38 MAPK signaling pathways play critical role in genesis and metastasis of melanoma (Tang et al., 2018). >50% of melanoma APO866 (Abildgaard and Guldberg, 2015) show abnormal activity of BRAF-RAS-RAF to activate MEK signal that drives the growth-promoting extracellular signal-regulated kin
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Introduction Enzymes have higher selectivity specificity and
2020-08-11
Introduction Enzymes have higher selectivity, specificity and efficiency than chemical catalysts. Due to their properties and their green chemistry, biocatalysts are widely used in food, textile and pharmaceutical industry [1], [2]. A high efficient biocatalyst for industrial applications must be s
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In Fig results of this experiment are shown as the
2020-08-11
In Fig. 1 results of this experiment are shown as the contour plots of endopeptidase activity. Optimal for the enzyme production by this strain concentrations of peptone and inorganic phosphate were found to be 24 and 0.3g/l, respectively. For specific activity, the optima close to those for glutamy
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