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ck1 inhibitor Hao et al evaluated the enantioselective MCL a
2020-07-28
Hao et al. evaluated the enantioselective MCL absorption, distribution, and metabolism in vivo following a single-dose in rats (Hao et al., 2018). Their results suggested preferential (−)-MCL enrichment in the liver, kidney, heart, lung, and testis (Hao et al., 2018). Besides that, (+)-MCL was conve
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Blood serum and plasma contain a range of
2020-07-28
Blood serum and plasma contain a range of enzymes that could potentially catalyze the hydrolysis of urea derivatives. Therefore it is possible for the prodrugs to be prematurely hydrolyzed by the plasma enzymes leading to the release of triazenes before reaching the pre-localized CPG2. Consequently,
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The varied functionality associated with sodium saccharin as
2020-07-28
The varied functionality associated with sodium saccharin, as a useful chiron, has promoted many attempts for synthesis of a wide range of benzenesulfonamides. Several studies have investigated the analgesic and anti-inflammatory activities of the benzenesulfonamides scaffold attached to a pyrazole
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br Clinical and therapeutical implications A direct link
2020-07-28
Clinical and therapeutical implications A direct link of CK2 to energy metabolism of the cell is provided by the fact that CK2 activity and protein level are elevated under hypoxic conditions. It regulates the hypoxia inducible transcription factor 1 alpha (HIF-1α) activity [54]. Due to the gener
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Recent studies have shown that nuclear localization and the
2020-07-28
Recent studies have shown that nuclear localization and the gene-regulatory function of SHP are enhanced by postprandial FGF19 signaling. In the liver, FGF19 mediates phosphorylation of SHP at Thr-55, which is critical for its interaction with RanBP2, a nuclear pore component and SUMO ligase that pr
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The number of leukocytes in the bronchoalveolar lavage and t
2020-07-27
The number of leukocytes in the bronchoalveolar lavage and the total number of macrophages and neutrophils in the alveolar space of the PPE 64d group was higher than that in the control group. Jiang et al. [29] investigated the role of the serotonin (5-HT or 5-HTT) transporter and the effect of simv
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br Experimental Procedures Further details and
2020-07-27
Experimental Procedures Further details and an outline of resources used in this work can be found in Supplemental Experimental Procedures. Introduction Oxysterols came to prominence in the late 1970\'s with the oxysterol hypothesis which proposed that the suppressive effect of cholesterol on
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Expression of MGMT in human cells can be switched off
2020-07-27
Expression of MGMT in human CI 976 can be switched off by enzymatic methylation of a cytosine residue in the MGMT promoter sequence. In this regard, both MGMT and the mismatch repair function MLH1 belong to a subset of DNA repair genes that are subjected to epigenetic control. In consequence, about
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The following experiment covers a bulk range
2020-07-27
The following experiment covers a bulk range of lipid from 0.2 to 20mM, with surface concentrations of DOG ranging from 0% to 10%. In this experiment eight master sets of 15-deoxy-Δ-12,14-Prostaglandin J2 receptor are made, each containing a different surface concentration of substrate, resulting i
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br Testicular HSD B isoforms br HSD B inhibitory
2020-07-27
Testicular HSD3B isoforms HSD3B-inhibitory endocrine disruptors Many endocrine disruptors could be anti-androgens. One of their mechanisms is direct inhibition of testicular HSD3B activity [2,24]. These environmental endocrine disruptors are derived from food, environment and other consumer pr
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br Acknowledgments We thank members
2020-07-27
Acknowledgments We thank members of the Kleer lab and Dr. Hernan Roca for discussions during the execution of this project, Dr. Gabriel Nunez for critical reading of the manuscript, and Dr. S. Takayama for guidance with the hanging drop spheroid assays. This work was supported by NIH grants (R01C
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The collagen binding membrane proteins discoidin domain rece
2020-07-27
The collagen-binding membrane proteins discoidin domain receptors (DDR1 and DDR2) are transmembrane receptors belonging to the family of receptor tyrosine kinases and have been studied for ECM remodeling in atherosclerosis,5, 6, 7 osteoarthritis,8, 9, 10 and several malignancies. It is well establis
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casein kinase The clinical consequences of variations in met
2020-07-27
The clinical consequences of variations in metabolism depend on whether the drug taken is pharmacologically active or is a prodrug that needs to be converted to an active metabolite. If the antipsychotic is pharmacologically active, the PM phenotype will result in increased plasma concentration. Man
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br Materials and methods br Results br Discussion This is
2020-07-27
Materials and methods Results Discussion This is the first report of a catalytic DNA or RNA cleaving DNA-enzyme that cleaved the CXCR-4 gene efficiently in a sequence specific manner. This is an important coreceptor for X4 viruses, the appearance of which usually coincides with the later st
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According to Graeff Graeff innate fear
2020-07-27
According to Graeff (Graeff, 1990), innate fear is mediated by neural circuitry that consists of at least the amygdala, medial hypothalamus and periaqueductal grey matter. In particular, the BLA has been considered to be a structure closely related to emotional responses to fear, stress and anxiety
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