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GSTP has an antiapoptotic activity that is mediated
2022-08-09

GSTP1 has an antiapoptotic activity that is mediated by the inhibitory interaction with JNK1. Our data suggest that GSTP1 treatment is associated with a significant down-regulation of caspase expression. This might explain the reduction in infarct-related cardiomyocyte death and saving the cardiomyo
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Having identified initial leads and further lead optimizatio
2022-08-09

Having identified initial leads and (), further lead optimization was initiated on B- and C-rings to afford compounds with improved potency. Initial set of substituted imidazole-biphenyl-carboxylic umbelliferone australia derivatives – and () were evaluated for GSNOR potency. Among this, fluoro, me
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All HFD fed groups in our study
2022-08-09

All HFD fed groups in our study, having significantly higher levels of EE (heat production) is consistent with previous studies [91], where a significant increase in EE was observed within just one week of HFD feeding [81]. It is hypothesized that this phenomenon is due to the increased body mass an
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Results from the current study are not
2022-08-09

Results from the current study are not consistent with those of a previous study (Poock et al., 2015) where there was no differences in ovulation induction response when there was administration of gonadorelin hydrochloride and gonadorelin diacetate salts. These differences in results are likely due
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In summary we have developed an
2022-08-09

In summary, we have developed an efficient synthetic route to the required urea-isostere containing hydroxamic acid-based inhibitor . The target molecule, , was found to retain the inhibitory potency of the corresponding carbo-analog against glyoxalase-I while possessing resistance to cleavage by γ-
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In the GLUT family glucose transporter
2022-08-09

In the GLUT family, glucose transporter 1(GLUT1) is primarily responsible for basal glucose uptake and maintenance of glucose basal metabolism in cells (Olson and Pessin, 1996). High GLUT1 expression occurred in various types of human cancers, like brain tumor, lung cancer and esophageal cancer (Nis
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The overall decrease in consummatory drive seen in rodents
2022-08-09

The overall decrease in consummatory drive seen in rodents treated with naltrexone in previous studies is in accordance with the effects seen with mice treated with SNAP 37889 in this study. While it may seem inappropriate to use a broad-acting drug like SNAP 37889 that suppresses overall consummato
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Reports described a range of
2022-08-08

Reports described a range of synthetic GPR40 agonists with desirable safety and efficacy profiles, compared with existing antidiabetic therapies such as insulin and sulfonylureas [[20], [21], [22], [23], [24], [25], [26], [27], [28]]. Among them, several small molecules were tested in the clinical t
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Neither E nor Z FPP synthase catalyzed the reaction
2022-08-08

Neither E- nor Z-FPP synthase catalyzed the reaction between 8-THPOGPP and IPP. However, a mutant E-FPP synthase (Y81S) produced 12-THPOFPP from the substrates 8-THPOGPP and IPP, and wild-type E-FPP synthase catalyzed the reaction betweeen 8-AcOGPP and IPP producing 12-AcOFPP. Mutant E-FPP synthase
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Potential platelet related mechanisms that might explain an
2022-08-08

Potential platelet-related mechanisms that might explain an augmented risk of MI in dabigatran treated patients have been investigated: Enhanced platelet reactivity is known to be associated with the risk of MI (Mangiacapra et al., 2018) and catalytically active thrombin is a potent stimulus to indu
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Our understanding of the genetic
2022-08-08

Our understanding of the genetic basis of myeloid malignancies has been profoundly improved in recent years. Studies have revealed new recurrent somatic mutations in myeloid malignancies, including myeloproliferative neoplasms (MPNs), myelodysplastic syndrome (MDS) and acute myeloid leukaemia (AML).
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br Drugs approved or in development To date
2022-08-08

Drugs approved or in development To date, three drugs: RAL (MK-0518), EVG (GS-9137) and DTG (GSK1349572) [104], have been approved by the FDA. Their structures are shown in Fig. 5. DTG is under development by GlaxoSmithKline (GSK), and studies have shown DTG to be effective in patients with resis
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In our previous study we designed and synthesized
2022-08-05

In our previous study, we designed and synthesized compounds of A series from the starting material 4-hydroxy-3-methoxycinnamic 9184 receptor (ferulic acid). These compounds with R group being amino acid residues, fatty acyl group and sulfuryl group showed moderate HDAC inhibition and in vitro anti
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miRNAs post transcriptionally regulate gene
2022-08-05

miRNAs post-transcriptionally regulate gene PRL-3 Inhibitor receptor by cleaving mRNA or inhibiting translation of target gene transcripts. Vita analysis of HBV genome sequence suggested that miR-185-5p may not directly act on HBV mRNAs, which suggested that miR-185-5p might suppress HBV gene expre
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It has been known for some time that an oral
2022-08-05

It has been known for some time that an oral salt load given to mammals induces a much greater natriuresis than the intravenous administration of an equivalent amount of saline (Carey et al., 1976, Singer et al., 1998). In addition, oral administration of salt to rats has been reported to augmented
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