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Present malarial chemotherapies mainly rely
2020-04-27
Present malarial chemotherapies mainly rely on a very few chemotypes or their allied structures such as quinolines, anti-folates and some cyclic endo-peroxides (Nayyar et al., 2012). Over the last few decades, the extensive and repetitive deployment of these drugs has stimulated resistance in the pa
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In normal chow fed mice EP
2020-04-27
In normal chow fed mice, EP4 deficiency also decreased the expression of CYP8B1, the downstream target of CYP7A1. Similarly, knockdown of EP4 with small interfering RNA reduced the expression of CYP8B1 in HepG2 cells. Therefore, it was anticipated that there would be an increased expression of CYP8B
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Meanwhile high levels of extraversion
2020-04-27
Meanwhile, high levels of extraversion have been associated with weaker conditioning and faster melatonin receptor agonist learning (Eysenck, 1970). Similar to neuroticism/anxiety, the role of extraversion for fear conditioning and extinction has found only limited empirical support (Rauch et al., 2
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This approach is similar to that suggested
2020-04-27
This approach is similar to that suggested by the previous edition of the GL [6]. Not surprisingly, the questions to be answered are the same (i.e., was the event TLOC? In cases of TLOC, is this mdm2 inhibitor of syncopal or non-syncopal origin? In cases of suspected syncope, is there a clear aetio
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Our previous high throughput screening
2020-04-27
Our previous high-throughput screening (HTS) campaign using automated, robust, and sensitive fluorescence based beta-lactamase 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],
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adrenergic antagonist More and more studies are
2020-04-27
More and more studies are focused on the function role of EPAC1 in cancer proliferation, apoptosis and migration. Recently, it was reported that the EPAC-ERK and AKT signaling pathways promote the B cell antigen receptor (BCR) mediated growth arrest and apoptosis in the B lymphoma cell line WEHI-231
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Phenolic compounds generated during biomass pretreatment inh
2020-04-27
Phenolic compounds generated during d-biotin pretreatment inhibit and/or deactivate cellulolytic/hemicellulolytic enzymes as well as the viability and fermentative capacity of yeast and bacteria [4], [5], [6], [7], [8], [9], [10], [11], [12], [13]. Phenolic compounds cause changes in protein conform
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The most significant finding was the
2020-04-27
The most significant finding was the inhibition of EROD and BFCOD activity by CLO. Inhibition of EROD and BFCOD were reversible, as pre-incubation did not enhance CLO inhibitory potency, and no reductions in IC50 values were observed. We further characterized the kinetic pattern of inhibition using
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br DDR receptor and MMP expression Type II collagen
2020-04-26
DDR2 receptor and MMP-13 expression Type II collagen protein in articular cartilage is highly stable structure as its half-life is 117 years [43]. The chondrocytes have limited ability to synthesis type II collagen protein in the matrix of mature articular cartilage once the collagen gets disrupt
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Compared to ET all agonists tested showed a
2020-04-26
Compared to ET-1, all agonists tested showed a 2–4 fold bias for the G protein constrictor assay compared to the β-arrestin assay (Table 1). This preliminary analysis indicated that at least modest pathway bias for endogenous ET peptides is possible, however the physiological significance of this, i
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From the general synthetic route we first
2020-04-26
From the general synthetic route, we first synthesized a directed set of analogues of general formula , keeping the synthesis simple by using a symmetrical pyrazole (R=R=Me). The SAR of a set of 30 compounds in the GTPγS binding assay turned out to be quite tight: only 4 (13%) compounds showed moder
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Introduction Enzymes have higher selectivity specificity and
2020-04-26
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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br Acknowledgment This work was supported by the Estonian
2020-04-26
Acknowledgment This work was supported by the Estonian Science Foundation (Grant ETF8862). Introduction In higher eukaryotes ionizing-radiation (IR) induced DNA double-strand breaks (DSB) are primarily repaired by the non-homologous end joining (NHEJ) pathway [1]. Ku, a heterodimeric protein
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xanthine oxidase inhibitor br Conclusion br Conflict of inte
2020-04-26
Conclusion Conflict of interest Author contributions Acknowledgements Piyamas Kanokwongnuwut was supported by the Development and Promotion of Science and Technology Talent Project (DPST), Royal Thai Government Scholarship. Funding for the work was provided by the Attorney General’s Depa
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The Rev protein is a
2020-04-26
The Rev1 protein is a crucial regulator of TLS activity because of its structural function [10]; therefore, we focused on Rev1 to investigate how Dot1/Rad53 function impinges on TLS-dependent mutagenic bypass of MMS-induced lesions. In particular, we examined Rev1 localization to chromatin by immuno
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