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Results are expressed as mean s
2021-05-18

Results are expressed as mean±s.e.m. Paired or unpaired Student's t test was used for comparisons between 2 groups and one-way ANOVA followed by Bonferroni's post-test for more groups. Statistical significance was assigned if p Results and discussion Variations in [Ca2+]i in cardiomyocytes loaded
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CPI-203 br Rationale and hypothesis To discover
2021-05-17

Rationale and hypothesis To discover an allosteric inhibitor of EGFR, Jia et al. (2016) screened a library of 2.5 million compounds at 1 μM ATP concentration in opposition the purified EGFR L858R/T790M mutant enzyme. 1322 best hits were found from this round of screening. The pinnacle hits had be
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br Funding This work was supported by the
2021-05-17

Funding This work was supported by the grants from MSD, Terumo Life Science Foundation, Takeda Science Foundation, and Japan Diabetes Foundation. Disclosures Acknowledgments The authors thank C. Morimoto (Juntendo University, Tokyo, Japan) and K. Takeda (Immunology Frontier Research Center
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We have reported previously that aminoacrylate derivatives o
2021-05-17

We have reported previously that β-aminoacrylate derivatives of the general structure () are inhibitors of DHODH. In particular, tricyclic derivatives and displayed sub-micromolar IC values against DHODH, and in the case of there was a 1000-fold greater potency compared to the human enzyme (DHOD
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Air trapping at the small airways is related to severe
2021-05-17

Air-trapping at the small airways is related to severe Naproxen Sodium receptor (Bjermer, 2014), and acute exacerbation (Mahut et al., 2010). Although asthma patients are generally treated with inhaled corticosteroid (ICS) or with ICS and long-acting β2 agonist (LABA), the efficacy of such treatmen
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CYP s are heme containing monooxygenases constituting a
2021-05-17

CYP450s are heme-containing monooxygenases constituting a conserved gene superfamily of heme-thiolate proteins, and are found in prokaryotes and eukaryotes (Martignoni et al., 2006). They play a key role in detoxification of endogenous (e.g., steroids) and exogenous compounds (e.g., drug, insecticid
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4-ethylphenyl sulfate In humans CYP A major isoforms of CYP
2021-05-17

In humans, CYP3A4/5, major isoforms of CYP3As in the liver, have variants that reduce the enzyme activities [33], [34]. In addition, Werk et al. recently reported the first case of a complete failure of CYP3A enzyme activity due to homozygous loss-of-function mutation of CYP3A4 combined with nonfunc
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Compounds and were synthesized according to Reductive aminat
2021-05-17

Compounds and () were synthesized according to . Reductive amination of ethyl acetoacetate with aniline afforded ester . Saponification of followed by intramolecular Friedel–Crafts acylation afforded ketone . Amide formation with benzoyl chloride followed by a reductive amination yielded compound .
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The V V process of
2021-05-17

The V&V process of the FPGA development includes equivalence checking (Huang and Cheng, 1998, Huang et al., 2000, Kuehlmann and Krohm, 1997, Kuehlmann et al., 1995, Burch et al., 1994) as well as the simulation techniques. The equivalence checking can prove that two given designs have the same funct
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SPR was used to measure biomolecular kinetic interactions
2021-05-17

SPR was used to measure biomolecular kinetic interactions between TERRA G-quadruplex and ligand in the present study. SPR is a widely used method, but cannot tell which specific type of interaction happened. Compounds with similar structures probably have similar mechanism of interaction, while comp
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In Murray Darling rainbowfish confirming the expected
2021-05-17

In Murray–Darling rainbowfish, confirming the expected in vivo effects of androgenic progestins could be achieved using short-term exposures and determining expression profiles for androgen-responsive genes, or in longer term exposures by monitoring fecundity or the development of male secondary sex
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Similarly to other investigations the present
2021-05-17

Similarly to other investigations, the present study found that ZEA in high concentrations decreases viability of both normal (Liu et al., 2018, Zheng et al., 2018a, Zheng et al., 2018b) and cancer 5-ht receptors (Khosrokhavar et al., 2009, Kowalska et al., 2017). The toxic effect of ZEA observed b
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The need for dedicated DAPT updates is
2021-05-17

The need for dedicated DAPT updates is well justified by the large amount of data and new information generated in the field over the past few years. As expected, the ACC/AHA and ESC updates contain large areas of overlap as well as some differences. Differences were largely explained by the differe
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br Structure and function of EPAC isoforms
2021-05-17

Structure and function of EPAC isoforms EPACs are guanine nucleotide exchange factors (GEFs) for the Ras-like GTPases Rap1 and Rap2 [9]. There are two mammalian EPAC isoforms, EPAC1 and EPAC2 1, 2 (Figure 1). Whereas EPAC1 displays a wide tissue distribution, the expression of EPAC2 is more restr
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In the previous study glutamyl endopeptidase of B
2021-05-17

In the previous study glutamyl endopeptidase of B. intermedius has been reported to be distributed in the GM 6001 of B. intermedius as follows: 90% of synthesized enzyme has been detected in the culture liquid, 9.3% of glutamyl endopeptidase—in the fraction of membrane proteins [20]. The distributio
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