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Although many of the hepatic responses observed on the
2019-07-04

Although many of the hepatic responses observed on the first day of recovery attenuated over the course of the recovery period, minimal-to-mild centrilobular hepatocellular hypertrophy tended to persist. Mean absolute and relative liver weights had returned to control levels after 28 days of recover
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luteolin Mouse Cyp a is a homologous isoform of the
2019-07-04

Mouse Cyp3a11 is a homologous isoform of the human CYP3A4 gene, and both are highly expressed in the liver (Hart, Cui, Klaassen, & Zhong, 2009). CYP3A4 is the most abundant CYP450 in hepatic microsomes responsible for drug and xenobiotic metabolism (Zanger & Schwab, 2013), and it is the most active
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Here we examine the associations between
2019-07-04

Here, we examine the associations between serum pro and anti-inflammatory cytokines and cognitive functioning in early-stage bipolar I disorder (BDI) patients. As per previous studies, ‘early-stage’ was defined as being within three years of the first manic episode (Kauer-Sant\'Anna et al., 2009). W
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Taking a pragmatic approach with
2019-07-04

Taking a pragmatic approach with a view to complete the study and because chemotherapy regimens in NETs are not standardized, we do not impose a specific regimen in both arms. However, one regimen in each arm is recommended in order to reduce heterogeneity: the ALKY-based chemotherapy arm will recei
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AMG-900 br Introduction In mammals there are
2019-07-04

Introduction In mammals there are ten known isoforms of the enzyme diacylglycerol kinase (DGK), as well as gene splice variants. Enzymes of this family all have a homologous active site but differ widely in their molecular mass, mechanisms of activation and biological function (Shulga et al., 201
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Cysteine protease inhibitors representing several chemical s
2019-07-04

Cysteine protease inhibitors representing several chemical scaffold types are effective in halting parasite replication without toxicity to the host (Renslo and McKerrow, 2006). A vinyl sulfone cysteine protease inhibitor, K11777, is completing final Good Laboratory Practice (GLP) preclinical tests
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Alvocidib flavopiridol is a piperidine chromenone http www
2019-07-04

Alvocidib (flavopiridol) is a piperidine-chromenone derivative (Fig. 6D) that is not FDA approved, but is in clinical trials for breast, endometrial, and several other cancers and hematological malignancies (Table 4) [[100], [101], [102], [103], [104]]. This drug targets CDK9 (IC50 = 3.2 nM) and CDK
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Apart from its high affinity the selection of
2019-07-04

Apart from its high affinity, the selection of GW2580 as ptc124 lead in our radiotracer development program was motivated by its exceptional selectivity. The observed profound impact of small structural modifications on the selected panel of four kinases tested prompted us to conduct comprehensive k
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In this study we observed alterations in mRNA
2019-07-04

In this study, we observed alterations in mRNA levels of CRF receptors in the PFCx and Hip during the development of sensitization. In particular, in the Hip both CRF receptors showed significantly increased UM171 when the sensitization condition was established. Similarly, CRF2 receptor increase wa
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Recently experimentally exposed common carp took up
2019-07-03

Recently, experimentally-exposed common carp took up CLO from water and maintained a consistent concentration in the liver and blood plasma (Corcoran et al., 2014). Clotrimazole may influence other aquatic organisms. Survival and development of marine shrimp larvae (Palaemon serratus) were affected
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DNA replication checkpoint kinases in both yeast and human c
2019-07-03

DNA replication checkpoint kinases in both yeast and human ABT-199 upregulate dNTP levels under replication stress to mediate their essential function at replication forks (Yeeles et al., 2013). It is possible that upregulation of dNTP levels under replication stress helps fork restart once replica
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In conclusion we have discovered two
2019-07-03

In conclusion, we have discovered two new derivatives ( and ) that are potent inhibitors of DHODH. H and C NMR spectroscopic data revealed that these compounds undergo ready isomerisation at room temperature in -DMSO, but the docking studies indicate that there is neither conformation nor configurat
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The present study found a significant
2019-07-03

The present study found a significant negative correlation between miR-152-3p and CDK8 expression in human HCC tissues. We also validated that CDK8 was a direct target of miR-152-3p, and overexpression of miR-152-3p inhibited proliferation and induced apoptosis in HCC NAD/NADH Quantitation Colorimet
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Preparation of the pyridyl ether analogs was accomplished by
2019-07-03

Preparation of the 2-pyridyl ether analogs (–) was accomplished by alkylation of alcohol with 2-bromopyridines in the presence of NaH to afford the desired pyridyl ether analogs in low to moderate yield. Preparation of the 3-pyridyl analog was carried out by conversion of alcohol to the tosylate,
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The in vitro cytotoxicity of the prodrugs was assessed
2019-07-03

The in vitro cytotoxicity of the prodrugs was assessed in the LS174T human colon cell line (). The results were found to reflect the stability of the prodrugs, with the unstable urea compounds ( and ) giving relatively poor cytotoxicity differentials between prodrugs and parents (i.e., approximately
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