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CYP A and CYP D are
2020-05-25
CYP3A4/5 and CYP2D6 are among the main drug-metabolizing enzymes in humans that are responsible for the metabolism of more than 50% of marketed drugs [19], [21]. Drugs metabolized by CYPs are prone to drug–drug interactions, thereby modifying their response [18], [32]. Metabolic inhibition is also i
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E is a classical initiator protein and as such plays
2020-05-25
E1 is a classical initiator protein and, as such, plays several roles in the initiation and catalysis of viral DNA synthesis. E1 must first recognize a specific segment of the viral Tianeptine sodium known as the “origin of DNA replication”, or “ori” for short. For most PV types examined to date, t
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We recently described the benzoxazin one analogue of
2020-05-25
We recently described the 1,3-benzoxazin-4-one analogue of LY294002 and showed it to have pan-PI3K and DNA-PK activity [2]. We have also reported on the activity of other family members, such as 3 which causes sensitization of lung cancer and colon cancer cells to radiation [11] and 4 (LTUSI122) as
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ATP dependent DNA ligases in
2020-05-25
ATP-dependent DNA ligases in vertebrates are divided in three families [7]. Family I DNA ligases are responsible for sealing the nicks during DNA replication and in long-patch base excision repair (BER). Family III DNA ligases are involved in short-patch BER. Lastly, family IV DNA ligases are involv
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The performance of the qCPA approaches
2020-05-22
The performance of the qCPA approaches is similar with regards to the derivative properties of CO2 and for mixtures of CO2+self-associating compounds. For CO2+n-alkanes the four-parameter versions of qCPA both perform somewhat better than the three-parameter version. Nevertheless this modest improve
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Though limited to a large cohort of self reported healthy
2020-05-22
Though limited to a large cohort of self-reported healthy individuals, associations between individual the site have been identified which may be clinically significant. Though slight, there is a relationship between the CYP2D6-inferred metabolizer phenotype and the diplotype-predicted activities o
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Peptides undergoing only a single hydroxylation i e PA
2020-05-22
Peptides undergoing only a single hydroxylation, i.e. PA-Hyp-KPAPK and PAPK-Hyp-APK, were then used to investigate the kinetics of vCPH co-factor and co-substrate dependences. The values for KMapp for Fe(II) and KM for 2OG for the two peptide substrates were within error (KMapp, Fe(II): 0.9 μM ± 0.1
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To date little is known about
2020-05-22
To date, little is known about mode of action or the underlying genetic basis of DEET repellency for human-biting ticks. To begin to unveil these mechanisms, we carried out behavioral assays to confirm the effectiveness of DEET as a deterrent for D. variabilis. RNA sequencing was then used to build
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Drug resistance to both pathogens and cancer has
2020-05-22
Drug resistance to both pathogens and cancer has been a big hindrance in healthcare. Integrated research undertakings are being pursued to find the exact causes of the lack of response towards drugs. Surprisingly, host pumps are the key factors in failure of most drugs. The pumps either do not allow
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Information on the mechanism by which
2020-05-22
Information on the mechanism by which parasite infections promote ECM degradation is limited (McKerrow et al., 1983; Andrade, 1994; Lu and Lai, 2013; Thibeaux et al., 2014). The interaction of plasminogen-plasmin with proteins of microorganisms, including bacteria, has been suggested to play a key r
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Immunomodulation effects of certain oxysterols were previous
2020-05-22
Immunomodulation effects of certain oxysterols were previously shown to depend on activation of oxysterol-binding liver X receptors (LXRs). Recent work from our labs as well as from others has shown additional receptors linking oxysterols and immunity. For example, we found that 7α,25-dihydroxychole
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Next the BE obtained for the different complexes
2020-05-22
Next, the BE obtained for the different complexes were evaluated. From the BE obtained from our MD simulations, a very good binder can be differentiated from a very weak binder (−11.85 kcal/mol for MTX vs. −6.74 and −3.61 kcal/mol for compounds 14b and 15c, respectively) but ligands with similar bin
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Presumably LBPs have health promoting activities
2020-05-22
Presumably, LBPs have health-promoting activities, such as antioxidant, immune regulation, anti-stress, anticancer, neuroprotective and antidiabetic activities [[7], [8], [9], [10], [11]]; LBPs can improve the whole-body health status of mice and stimulate the expressions of IL-2, IL-12 and TNF-α, w
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br Limitations There are some limitations to
2020-05-22
Limitations There are some limitations to take into account when interpreting these results. Firstly, direct causation cannot be established in this cross-sectional study, and it may be the downstream effects of TNFα, such as increased BIBR-1048 production, which are more proximally related to co
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The CysLT receptor antagonist BayCysLT RA significantly
2020-05-22
The CysLT2 receptor antagonist BayCysLT2RA significantly suppressed multiple antigen challenge-induced infiltration of eosinophils and mononuclear G-36 receptor into the lung, indicating that CysLT2 receptor activation is involved in leukocyte migration. In contrast to the present finding, Barret et
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