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To study systemic potential of the selected compounds as EP
2021-05-22

To study systemic potential of the selected compounds as EP1 receptor antagonist, they were evaluated with regard to the sulprostane-induced increase of intravesical bladder pressure in rats. Some of the analogs, 13 and 15–17, which were selected on the basis of their in vitro EP1 receptor affinity,
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Enhanced responses to varying concentrations
2021-05-22

Enhanced responses to varying concentrations of bronchoconstrictors, such as MCh, and airway obstruction are characteristic of CGP 57380 and common to other clinical states, including chronic obstructive pulmonary disease, lung transplantation, and infection- or chemical agent-induced airway inflamm
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In principle in vitro techniques
2021-05-22

In principle, in vitro techniques for assessing enzyme induction might include the use of cultured hepatocytes, precision-cut liver slices, immortalized Physcion lines (such as those derived from hepatomas) and reporter gene constructs (where appropriate cells are transfected with recombinant DNA e
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L-Carnitine inner salt The hepatic cytochrome P CYP superfam
2021-05-22

The hepatic cytochrome P450 (CYP450) superfamily is essential for metabolising foreign chemicals, fatty acids, vitamins, hormones and other compounds and consists of 18 subfamilies (Uno et al., 2012). The number of discovered CYP genes is increasing as a result of intense work with CYP450 gene struc
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Despite robust translation of GA only
2021-05-22

Despite robust translation of GA, only small amounts of GR and GP were translated in cultured Gossypol synthesis and chick embryo spinal cord neural cells from the 75 copies of G4C2 in monocistronic constructs. Interestingly, GA is also the most common dipeptide found in autopsy tissue in FALS pati
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br Experimental Procedures Further details and
2021-05-22

Experimental Procedures Further details and an outline of resources used in this work can be found in Supplemental Experimental Procedures. Introduction In response to T cell-dependent (TD) antigen stimulation, antigen-specific Shikonin receptor migrate to the periphery of B cell follicles a
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Downregulation of tumor suppressors is a major factor
2021-05-22

Downregulation of tumor suppressors is a major factor that leads to tumorigenesis. Phosphatase and tensin homolog deleted on chromosome 10 (PTEN), a common tumor suppressor, the topoisomerase inhibitors of which is often downregulated or even absent in the majority of human cancers, functions as a p
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Likewise the conserved cysteine in the E
2021-05-22

Likewise, the conserved cysteine in the E2 protein is the only residue shown to be essential for the transfer of Ub/Ubl from E2 to the HECT ligases (Dye and Schulman, 2007, Wu et al., 2003). However, all other terminal Ub/Ubl transfer reactions involving E2 enzymes suggest a critical role for the ta
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br Results br Discussion Previous studies have
2021-05-22

Results Discussion Previous studies have mapped ABCF1 as a risk factor gene for rheumatoid arthritis and autoimmune pancreatitis (Ota et al., 2007, Richard et al., 1998). Additionally, recent genome-wide association studies have also associated ABCF1 with the risk of gout (Dong et al., 2017) a
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br Results and discussion br Conclusion In the current
2021-05-22

Results and discussion Conclusion In the current study, a series of novel ‘open-chain’ classes of E. coli PDHc E1 inhibitors, N-acylhydrazone pyrimidine derivatives A, B, and C were designed and synthesized. As novel ThDP analogs, all A displayed moderate to powerful inhibitory activity with I
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br Enzymes repairing alkylated DNA br
2021-05-22

Enzymes repairing alkylated DNA Induction of the Ada regulon Methylated Ada is a strong activator for ada and alkA promoters. Although much weaker than the methylated form, unmethylated Ada acts alone as an activator for ada and alkA promoters. In contrast, the unmethylated protein present in
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A An optimized BEI SEIscore based
2021-05-22

(A) An “optimized BEI-SEIscore” based on the trends, emerged from the statistical analysis of several optimization studies in pharmaceutical industry (Abad-Zapatero, 2007, Abad-Zapatero and Blasi, 2011). This type of optimized scores has been used in many previous studies. Ki=1nM at 300° K, compare
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In humans CYP A major isoforms of CYP As in
2021-05-22

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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The consistent anti anxiety effects
2021-05-22

The consistent anti-anxiety effects obtained with intra-mPFC injections of CP 376395 strongly suggest a tonic role of CRF at CRF1 receptors located within this limbic DiscoveryProbe™ Inhibitor Library receptor area in the modulation of anxiety in the mouse on the EPM. Intra-mPFC injection of CP 3763
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The crystal structure of LiCoO is presented in Fig
2021-05-22

The crystal structure of LiCoO2 is presented in Fig. 1. We can notice that the Li and Co atoms occupy the centers of two different edge-sharing [CoO6]-octahedra, which results in formation of separate Li and Co layers. Hence, the layered structure of LiMO2 is able to intercalate lithium into transit
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