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Our previous high throughput screening HTS campaign using au
2021-07-02
Our previous high-throughput screening (HTS) campaign using automated, robust, and sensitive fluorescence based NAD/NADH Quantitation Colorimetric Kit synthesis assay [10], [11] led to the identification of several EPAC specific inhibitors (ESIs), and was subsequently followed by extensive hit-to-le
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The endothelin receptor type B EDNRB belongs to
2021-07-02
The endothelin receptor type B (EDNRB) belongs to the family of G protein-coupled receptors, which functions as a vital regulatory factor in signal transduction in cells, locating on human chromosome 13q22.3 (Ayala-Valdovinos et al., 2016; Bregar et al., 2018; Morimoto et al., 2018; Widowati et al.,
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In terms of its protease activity
2021-07-02
In terms of its protease activity, MME has a broad range of substrates being able to target glucagon, bradykinin, GLP1, and several other BG45 of circulating small molecules [25]. MME has been shown to target free insulin B-chain [32], although whether MME could target and degrade the insulin recep
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Molecular modelling studies were performed on
2021-06-29
Molecular modelling studies were performed on the hDHFR inhibitors identified (1, 11, 13, 14, 16, 25 and 32) to explore the structural basis of the interaction between the mentioned compounds and the human enzyme. The docking studies were performed using the X-ray crystallographic structure of the h
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Industrial fermentation aims to produce valuable products fr
2021-06-29
Industrial fermentation aims to produce valuable products from cheap feedstocks by utilizing diverse microbial functions through aerobic or anaerobic fermentation [[8], [9], [10]]. During anaerobic fermentation, the reducing power is mostly directed to product synthesis rather than being oxidized, r
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The goal of this paper is to
2021-06-29
The goal of this Dihydroartemisinin paper is to investigate the penalized empirical likelihood method for the Cox model, as a competitor to the penalized partial likelihood. Since empirical likelihood (EL) was proposed by Owen, 1988, Owen, 2001, empirical likelihood methods have been investigated w
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An Emerging Role for the EphrinB
2021-06-28
An Emerging Role for the EphrinB2-EphB4-RASA1 Signaling Axis in Human Congenital Cerebrovascular Disorders Normal vascular development includes de novo blood vessel formation from endothelial cells (ECs) (vasculogenesis) 1, 2, expansion of the network through vessel sprouting, splitting, and remode
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We continued to investigate the contribution
2021-06-28
We continued to investigate the contribution of the EP1 Sertraline HCl to nociceptive sensitization by utilizing its natural ligand PGE and tested the effect of local subcutaneous injection of PGE (5nmol in 5μl) into one hindpaw on mechanical and heat pain thresholds. Wild-type mice displayed maximu
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br Methods br Results br Discussion Here we
2021-06-28
Methods Results Discussion Here we have shown that two GPCR subtypes thought to trigger similar signalling events by coupling to Gαq in fact regulate different signalling networks via coupling to distinct G proteins. Thus global effects regulated by both receptors in events such as cardiac
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The hepatic cytochrome P CYP superfamily is essential for
2021-06-28
The hepatic cytochrome P450 (CYP450) superfamily is essential for metabolising foreign chemicals, fatty acids, vitamins, hormones and other compounds and consists of 18 subfamilies (Uno et al., 2012). The number of discovered CYP genes is increasing as a result of intense work with CYP450 gene struc
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br Discussion Although DNA has a
2021-06-28
Discussion Although DNA has a limited chemical stability it has long been known that DNA in blood stains may remain relative stable for weeks, months, or even years at ambient temperature,1, 2, 3, 4, 5, 6 and samples (e.g., reference samples) that have been transferred to a matrix, e.g., FTA® pap
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For reductive amination by L
2021-06-28
For reductive amination by L-AmDH, the term related to the enzyme-ammonia complex is excluded rather than the enzyme-pentanone term (Table 1). If this were an ordered mechanism, this would imply ammonia binds second, after NADH and before 2-pentanone. However, a large KM,NH4 value renders ammonia bi
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The results described in the present study confirm
2021-06-28
The results described in the present study confirm key restrictions on reaction conditions which must considered to maximize reactor productivity. Increased viscosity should be avoided for the amination of ketones by L-AmDH, as a 4-fold increase in viscosity can lower the reaction rate by as much as
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Finally the identification of predictive biomarkers
2021-06-28
Finally, the identification of predictive biomarkers of response will also allow the more recently discovered CDK inhibitors to be explored in particular genetically-defined contexts, for example by building on recent observations that KRAS mutant tumors are highly sensitive to CDK1 inhibition, and
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br Theory br Method To test our hypotheses as shown
2021-06-28
Theory Method To test our hypotheses as shown in Fig. 1, we conducted a survey at an international media company (hereafter referred to as ‘MediaCo’) headquartered in the UK. Its 5500 employees are dispersed throughout the world, partly due to massive acquisitions within the past decade. In ex
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