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In anticipation of an approach
2019-10-25
In anticipation of an approach based on modification of the cyclohexylacetic AP1903 mg subunit of 1 as a means of improving permeability, a set of analogs were prepared to map out the optimum display of the acidic functionality. Homologated acids 25 and 26 were found to be equipotent to 1, although
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Given the excellent in vitro pharmacology profiles of methyl
2019-10-25
Given the excellent in vitro pharmacology profiles of methyl ester 28 and primary amide 29 efforts were reengaged on neutral analogs of these leads, with a focus on non-amide replacements for the carboxylic leonurine functionality of 1. Acetonitrile 49 was found to have a good balance of DGAT-1 inhi
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In this study cell migration in response to
2019-10-25
In this study, cell migration in response to LTD4 exhibited a typical bell-shaped dose-response curve with optimal activity at 10 nM. However, the effect of inhaled CysLTs on airway inflammatory cells in vivo has not been widely reported to date, therefore, the role of CysLTs in the development of a
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Midazolam oral clearance is used for
2019-10-25
Midazolam oral clearance is used for characterization of both intestinal and hepatic CYP3A activity. However, the identification and subsequent use of metabolic markers of CYP3A activity can eliminate the need for unnecessary administration of probe drugs such as midazolam. Such metabolic markers wo
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We continued to investigate the
2019-10-24
We continued to investigate the contribution of the EP1 Melphalan to nociceptive sensitization by utilizing its natural ligand PGE and tested the effect of local subcutaneous injection of PGE (5nmol in 5μl) into one hindpaw on mechanical and heat pain thresholds. Wild-type mice displayed maximum se
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br Introduction Schistosomiasis one of the major parasitic d
2019-10-24
Introduction Schistosomiasis, one of the major parasitic diseases that affect humans in tropical and subtropical countries, is an acute and chronic condition caused by blood flukes (trematode worms) of the genus Schistosoma (World Health Organization, 2014). Schistosomiasis infects over 240 milli
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Additionally of outmost important is the location of the dif
2019-10-24
Additionally, of outmost important is the location of the different CpG islands in relation to the transcription starting site (TSS) of the promoter as well as their interaction with transcription activators or repressors. It has been shown that methylation at the downstream region of the TSS in the
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Though limited to a large
2019-10-24
Though limited to a large cohort of self-reported healthy individuals, associations between individual Misoprostol have been identified which may be clinically significant. Though slight, there is a relationship between the CYP2D6-inferred metabolizer phenotype and the diplotype-predicted activities
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br Conclusions br Source of financial support or funding
2019-10-24
Conclusions Source of financial support or funding This investigation was supported by the University of Utah Study Design and Biostatistics Center, with funding in part from the National Center for Research Resources and the National Center for Advancing Translational Sciences, National Insti
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br Casein Kinase II CK Casein
2019-10-24
Casein Kinase II (CK2) Casein Kinase II (CK2) is a ubiquitous serine/threonine-selective pro-oncogenic protein kinase that has become a more prominent target for research due to its effects and key role in tumorigenesis (Gowda et al., 2017a, Pinna, 2002). CK2, a well-conserved, pleiotropic kinase
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br Acknowledgements This work was
2019-10-24
Acknowledgements This work was supported by National Natural Science Foundation of China (31701807, 31572000) and Jiangsu Province Science Foundation for Youths (BK20170491). Introduction Two Cl− channels of the ClC family, ClC-K1 and ClC-K2 (or their human orthologs ClC-Ka and ClC-Kb, respec
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br Introduction Al Awqati and his colleagues using
2019-10-24
Introduction Al Awqati and his colleagues using R(+)-methylindazone, R(+)-[(6,7-dichloro-2-cyclopentyl-2,3-dihydro-2-methyl-1-oxo-1H-inden-5-yl)-oxy] acetic GW311616 hydrochloride (IAA-94) (Landry et al., 1987) isolated the first chloride intracellular ion channel (CLIC) proteins (p64) from bovi
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The compounds listed in Table Table
2019-10-24
The compounds listed in Table 1, Table 2, Table 3, Table 4, Table 5 were biologically evaluated for their inhibition of the specific binding of a radiolabeled ligand [3H]PGE2 to membrane fractions prepared from cells stably expressing each mouse prostanoid receptor. The EP1 antagonist activity of th
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Social interaction is known to be the main source
2019-10-23
Social interaction is known to be the main source of stress in human beings (Dickerson and Kemeny, 2004, Tamashiro et al., 2005). An animal model of social stress should closely mimic real-life situations in human life (Neisewander et al., 2012); in this context, social defeat in an agonistic encoun
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Assessment of the activity of native and denatured
2019-10-23
Assessment of the activity of native and denatured TAT-CPG2 after penetration suggests that TAT-CPG2 has been successfully delivered into the cells, and the transduced enzyme is functional inside the cells. The enzyme activity of both native and denatured TAT-fusion proteins in the cultured HepG2 Lo
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