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We neither observed changes in midazolam eCLmet indicative
2021-01-28
We neither observed changes in midazolam eCLmet indicative of significant inhibition of CYP3A4/5 during both experiments, despite the in vitro evidence for CYP3A4/5 inhibition (Theile et al., 2017). The observed increase in CYP3A dependent midazolam clearance after chronic ingestion of clementines/c
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Compound was generated using a
2021-01-28
Compound was generated using a literature procedure and required two-step Dess–Martin-periodinane/Pinnick oxidation prior to the methylation of the sulfonamide. Compound () was obtained from the Suzuki coupling of the methyl ester intermediate (en route to BG45 ). Hydrolysis of all methyl ester
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glucokinase Application of the CPH model relies on the assum
2021-01-27
Application of the CPH model relies on the assumption that the hazard ratio of two observations is constant over time [2]. This enables us to infer the rate of risk of the treatment. For example, in the study of patients with pulmonary arterial hypertension (PAH) [5], the hazard ratio of a group of
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acamprosate calcium synthesis The use of recombinant ER and
2021-01-27
The use of recombinant ERα and ERβ binding assays offers a relatively inexpensive, rapid technique for screening compounds for potential direct acamprosate calcium synthesis receptor modulatory activity and understanding the mechanisms of existing herbal medicines. For background on the protein pro
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Several studies have shown that independently
2021-01-27
Several studies have shown that, independently of body-weight control, the central actions of leptin improve glycemic control in obese diabetic rat and mouse models [62]. For instance, restoration of OB-Rb expression in OB-Rb-deficient mice, and in particular in POMC neurons, was sufficient to norma
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br EBV BILF A Virus
2021-01-27
EBV-BILF1—A Virus-Encoded 7TM Receptor with Immune Evasive Functions The EBV-encoded BILF1 receptor (EBV-BILF1) is thought to be implicated in the immune evasion strategy of EBV.56, 61, 62 This orphan 7TM receptor is expressed at significant levels during the early lytic phase of the virus infect
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The synthesis of compounds a
2021-01-27
The synthesis of compounds 7a and 7b are outlined in Scheme 2. Compound 5 was obtained by di-tert-butyl pyrocarbonate protection of minocycline hydrochloride 4a. Then, compounds 6a and 6b were obtained by amination of the fluoride with a morpholino and dimethylamine, respectively. Target compounds 7
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The overall poor outcomes in ESCC are thought because
2021-01-27
The overall poor outcomes in ESCC are thought because of a combination of late diagnosis, aggressiveness of the disease, and a lack of effective treatment strategies for systemic disease. Several molecular pathways, such as epidermal growth factor receptor, vascular endothelial growth factor, and p5
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In order to gain further insights into the role of
2021-01-27
In order to gain further insights into the role of peptidases in B. xylophilus, four cysteine proteases highly secreted by B. xylophilus (Cardoso et al., 2016) were selected four further characterisation. Materials and methods Results and discussion Structural prediction and analysis The i
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br Material and methods br Results br Discussion In vitro
2021-01-27
Material and methods Results Discussion In vitro evidence indicates that LAS191859 is a potent CRTh2 antagonist as demonstrated in GTPγS binding studies with potency in the low nanomolar range and in addition it demonstrates a long receptor residence time. This potency is also maintained in
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Bradykinin acetate Numerous small molecule CRF receptor
2021-01-27
Numerous small molecule CRF receptor antagonists have been reported in the literature. Some representative examples are shown in . In preclinical studies (DMP696), , was found to be efficacious in preclinical behavioral models for anxiety and depression. In an open label clinical trial with (R121
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The observed increase in Bdnf
2021-01-27
The observed increase in Bdnf1 mRNA occurred 1 h after treatment indicates participation of BDNF in early plasticity and subsequently mnemonic processes. Most of the evidence regarding the importance of BDNF for memory formation derived from electrophysiological studies that utilized the molecular c
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Following mutagenesis of the glucarpidase gene
2021-01-27
Following mutagenesis of the glucarpidase gene of Pseudomonas sp. strain RS-16 [30], approximately 73% of the clones retained enzyme activity, as indicated by the clear zones and yellow precipitate surrounding their colonies. However, there were very few that had ‘halos’ around colonies that were da
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br Materials and methods br Results br
2021-01-27
Materials and methods Results Discussion In this study, we uncovered a female-specific haplotype-MDD vulnerability association, by which a two-marker haplotype TG of rs4633-rs4680 may link to enhanced MDD risk in females. Female haplotype TG carriers were estimated to have a 9.17-fold incre
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br Materials and methods br Results
2021-01-26
Materials and methods Results Discussion In addition, the responses of CYP450s induced by metalaxyl are species-specific in the four cells. For example, metalaxyl lead to induction of CYP1A1, CYP1A2, and CYP2B1 in HepG2 cells, CYP1A2 and CYP2B1 in H4IIE cells, CYP1A1 and CYP2B1 in LMH cells
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