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Herein we explored by docking
2021-04-30

Herein, we explored by docking studies the effectiveness of replacing the dimethyl substitution at C (6) of dihydrotriazine with a folded azaspiro-containing substituent, along with the introduction of differently substituted phenyl- and benzyl-rings or alkyl chains, linked at the position 1 of the
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Our data show a site
2021-04-30

Our data show a site-specific interaction of DDR2 with collagen II. This indicates that the DDRs recognise a particular sequence within collagen and not simply the collagenous triple helix per se. This common tertiary structure of all collagens is formed by three α chains, each with a repeating G-X-
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Oral antipsychotics are substrates of CYP enzymes which
2021-04-30

Oral antipsychotics are substrates of CYP450 enzymes, which are crucial to their metabolism and elimination (Fig. 1). The efficacy and toxicity of antipsychotic agents is affected by factors that induce or inhibit CYP450 expression and function, such as drug–drug interactions. Additionally, the mult
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br Materials and methods br Results
2021-04-30

Materials and methods Results Metabolic stability of compounds was studied by incubation with pooled human liver microsomes. Piperine was the metabolically most stable compound, with a t1/2 of 141min (Fig. 2, and Table 1). SCT-29 and LAU 397 showed t1/2 of approx. 45min, whereas a t1/2 of only
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It is worth mentioning that
2021-04-30

It is worth mentioning that, in this study we only observed the responses of CYP450 to the short-term exposure of DSP toxins (12 h). However, the toxic effects of DSP toxins to bivalves appeared to abate with longer exposure (Pinto-Silva et al., 2005; Flórez-Barrós et al., 2011; Prego-Faraldo et al.
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A variety of epidemiological and clinical
2021-04-29

A variety of epidemiological and clinical studies suggest that light alcohol consumption may exert a favorable effects on BP levels but chronic heavy alcohol consumtion causes sustained BP elevation [16], [17]. The hypertensive effect of heavy drinking occurs with all forms of alcohol (i.e. beer win
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br Activatable MRI probes MRI is commonly used in
2021-04-29

Activatable MRI probes MRI is commonly used in clinics around the world and has the advantages of outstanding tissue-penetration depth and extremely high spatial resolution for in vivo imaging [33]. MRI has relatively poor sensitivity and usually requires cp-690550 receptor agents to enhance the
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Taken together this study gives first insights into
2021-04-29

Taken together, this study gives first insights into the complex effect of DNMT inhibition on pattern separation. Acute administration of RG108 enhanced pattern separation performance measured with the OPS task and increased Bdnf1 expression. However, this effect was only acute, and was not present
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Molecular modelling studies were performed on the hDHFR inhi
2021-04-29

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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The secondary objective of the present
2021-04-29

The secondary objective of the present study was to evaluate the pharmacokinetics, safety, and tolerability of multiple oral doses of 450-mg delafloxacin to reach steady state in healthy male and female subjects. After multiple dosing of oral delafloxacin, steady state was reached after 4 days of do
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br The LSCP model and its properties In this section
2021-04-29

The LSCP model and its properties In this section, we first introduce the LSCP model in Section 2.1. Some examples of the model are presented in Section 2.2 and basic properties of the model are presented in Section 2.3. Finally, Section 2.4 introduces finite dimensional approximations necessary
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br Introduction The dopaminergic system and
2021-04-28

Introduction The dopaminergic system and its projections including both the prefrontal Pseudo-UTP mg (PFC) and striatum are known as being crucial to synaptic plasticity, skill acquisition and higher order functions (e.g., working memory and cognitive control; Matsumoto et al., 2003). Variations
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br Third trimester crossing the threshold to immunocompetenc
2021-04-28

Third trimester – crossing the threshold to immunocompetence Summary Regrettably, studies on the fetal immune system have yet to yield practical results. While it is becoming apparent that the fetal immune response plays a role in determining the outcome of congenital CMV infection, we still l
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br Acknowledgements br Introduction Protein
2021-04-28

Acknowledgements Introduction Protein–tyrosine phosphorylation, catalyzed by protein–tyrosine kinases and protein–tyrosine phosphatases, has a pivotal role in the regulation of a wide variety of cellular processes. Similar numbers of tyrosine kinases and tyrosine phosphatases are encoded by th
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br Benefits and risks of traditional combined oestrogen prog
2021-04-28

Benefits and risks of traditional combined oestrogen–progestogen HRT regimens Combined oestrogen–progestogen regimens were developed to reproduce the short- and long-term benefits of oestrogen replacement therapy (ERT) and to simultaneously provide appropriate protection against oestrogen-related
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