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Herein the interactions of etamicastat nepicastat and zamica
2019-09-19
Herein, the interactions of etamicastat, nepicastat and zamicastat with P-gp and BCRP were evaluated. Although recent investigations have been performed to assess the involvement of P-gp in the glutamate transporter exposure of nepicastat and etamicastat (Loureiro et al., 2015), the contribution of
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RLS is a genetically complex disorder in which genetic and
2019-09-19
RLS is a genetically complex disorder in which genetic and environmental factors contribute to the phenotype (Trenkwalder, Allen, Högl, Paulus, & Winkelmann, 2016). This disease is highly familial and six genetic variants with single nucleotide polymorphisms have been identified by genome-wide assoc
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Over the past decade targeting DNA repair proteins has
2019-09-19
Over the past decade, targeting DNA repair proteins has emerged as an effective tool to enhance chemosensitivity of malignant cells [9]. However, identification and selection of the proper target of DNA repair pathways is critical to increase cytotoxic activity of chemotherapeutic agents in cancer c
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br Introduction Although not fully understood the
2019-09-19
Introduction Although not fully understood, the molecular toxicology of sulfur mustard (bis(2-chloroethyl)sulfide, SM; CAS–Nr. 505-60-2), an alkylating warfare agent, has been attributed to DNA alkylation [1], [2], [3]. The same principle holds true for other alkylating compounds such as nitrogen
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Next we evaluated the therapeutic
2019-09-19
Next, we evaluated the therapeutic potential of compound () using the mouse model of collagen-induced arthritis (CIA model), which is the pathological model for RA. Consequently, oral once-daily dosing of 3 mg/kg reduced the overall progression of the clinical score, including inflammation and bone
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br Acknowledgements br Introduction Anxiety and depression a
2019-09-19
Acknowledgements Introduction Anxiety and depression are major components of maintaining the cycle of addiction, and are responsible for the negative reinforcement of drug seeking behaviors (Sarnyai et al., 1995, Koob and Le Moal, 2008). Both rats and humans exhibit increased anxiety states du
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We further examined our hypothesis that the
2019-09-19
We further examined our hypothesis that the activation of CRF and CCK systems is responsible for the enhanced anxiety-like behavior induced by immobilization stress using two antagonists to block the expression of CRF1 and CCK2 receptors. It was found that CCK2 receptor antagonist CR2945 or CRF1 ant
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br Materials and methods br Results and discussion
2019-09-18
Materials and methods Results and discussion Summary Acknowledgments We thank Muhammad Anwar for animal rearing and surgery. We also thank Michael M. Myers for editing. Finally, we thank David Hirschberg for his technical advice. Funding for this project was provided by the Einhorn Famil
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the full report As in our earlier observations the PTPN SNP
2019-09-18
As in our earlier observations, the PTPN22 SNP affected the appearance of β-cell autoimmunity, but in contrast to our earlier report, only a borderline effect of the PTPN22 SNP on the progression to clinical disease was observed in the current analysis [22], [27]. The finding of an effect of the PTP
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br A brief introduction to DUBs The
2019-09-18
A brief introduction to DUBs The reversal of ubiquitin conjugation of targeted proteins relies on deubiquitinating 5416 (DUBs), which catalytically cleave single Ub or poly-ubiquitin chains from proteins. The human genome encodes approximately 100 potential DUBs which can be classified into six
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UNC1215 In a study carried out by Aunis et
2019-09-18
In a study carried out by Aunis et al. the properties of soluble DBH and membrane bound were examined [23]. The membrane bound enzyme was shown in UNC1215 to the soluble form to have thermal denaturation at higher temperatures of 43.5–44°C. Similar discontinuities in the Arrhenius plots were obtain
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A second advance came with the discovery that conformational
2019-09-18
A second advance came with the discovery that conformationally-flexible benzamide analogs having an N-phenylpiperazine moiety possessed good affinity and modest selectivity for D3 versus D2 receptors [3,[14], [15], [16]]. This observation spawned a significant effort by medicinal chemists to develop
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hcv protease inhibitors br Biological roles of DGK
2019-09-18
Biological roles of DGKϵ Summary and future perspectives The most hcv protease inhibitors segment of DGKϵ, comprised of residues 20–42, appears to have no role in binding the lipid substrate DAG or in the acyl chain specificity of substrate phosphorylation. Nevertheless, the sequence in this
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br Materials and methods br Results br Discussion
2019-09-18
Materials and methods Results Discussion The present work demonstrates the functional role of DGAT2 in elevating the neutral lipid accumulation in engineered N. oceanica, which have aroused a great deal of interest in industrial scale biofuel production. Recently, there have been increasing
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The aberrant methylation of genes that
2019-09-18
The aberrant methylation of genes that suppress tumorigenesis appears to occur early in tumor development and increase progressively, eventually leading to the malignant phenotype [35]. Genes involved in every step of tumorigenesis can be silenced by this epigenetic mechanism. Hypermethylation of pr
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