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The lack of biological activity
2021-12-27
The lack of biological activity of this family of compounds against T. cruzi is quite unexpected and cannot be attributable simply to the presence of a hydroxyl group at C-1. In fact, either compound 6 or risedronate (5), both bearing a hydroxyl group at C-1, are effective inhibitors of TcFPPS.21, 2
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In tumor cells HK II induction
2021-12-27
In tumor cells HK-II induction is mediated by Akt/mTOR pathway [6], [11]. HK-II dynamically shuttles between the mitochondria and cytoplasm under different metabolic conditions. In cardiomyocytes, Akt enhances HK-II binding to mitochondria, setting the heart at a state resistant to ischemic injury [
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In this investigation the NlVg relative transcript level
2021-12-27
In this investigation, the NlVg relative transcript level was also prompted by 1.3-fold compared to the untreated control in the TZP treatment, while there was a slight increase of 13.6% for NlVgR (Fig. 7A and B). One underlying molecular mechanism for the TZP-induced fecundity is the significant up
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There has been some debate about which types of
2021-12-27
There has been some debate about which types of liver cells might be able to activate canonical Hh signalling during liver injury. These uncertainties reflect technical challenges imposed by imperfect and inconsistent reagent specificity and the nature of the signalling process itself, which is quit
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br Acknowledgments This research was funded by generous gran
2021-12-27
Acknowledgments This research was funded by generous grants from the Singapore National Medical Research Council (NMRC CBRG grant NMRC/CBRG12Nov114 (BD)). WJC is supported by NMRC Clinician Scientist Investigator award and partly supported by a Singapore Cancer Syndicate Grant, the National Resea
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Considering that TGF plays a pivotal role in inflammation
2021-12-27
Considering that TGF-β1 plays a pivotal role in inflammation, renal fibrosis, cell growth, differentiation, and apoptosis, it has been viewed as a vital mediator in kidney disease [49,50]. Studies have demonstrated that TGF-β1 is upregulated in both human and experimental kidney diseases [51,52]. TG
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Glutathione S transferases constitute a family of enzymes
2021-12-27
Glutathione-S-transferases constitute a family of enzymes involved in the detoxification of xenobiotics, signalling cascades and serving as ligandins or/and catalyzing the conjugation of various chemicals and drugs [53]. The present finding indicates significant increase in GST activity in the brain
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In the Toc Regulator Mode Fig recognition of the
2021-12-27
In the “Toc34 Regulator Mode” (Fig. 6), recognition of the transit peptide by Toc159 monomer (step 4) leads to heterodimer-formation [18]. Subsequently, preprotein interaction with the Toc34G homodimer (step 1) regulates the Toc34G homodimer (step 2, 3). However, this mode requires a parallel induct
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The diversity of biological properties
2021-12-27
The choline fenofibrate sale of biological properties and interactions of GSK-3 have been reviewed recently (, , , , ). The interactions of GSK-3 in the signaling pathways induced by nutraceuticals is covered in the review by ) in this special issue of . GSK-3 is a frequent target of many nutraceut
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Much of the understanding of this system has
2021-12-27
Much of the understanding of this system has come from several studies focussed on CB1. A significant amount of research has demonstrated that activation of the CB1 receptor by cannabinoid ligands stimulates food intake [10], reduces gastrointestinal motility [11], and increases lipogenesis [12] and
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br Conflicts of interest br
2021-12-27
Conflicts of interest Introduction Antiretroviral therapy (ART) is effective in reducing mortality (Detels et al., 1998), and preventing mother-to-child transmission (MTCT) (CDC, 1994, Connor et al., 1994) and sexual transmission of HIV (Cohen et al., 2011). However, the optimal time to start
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In the present study recipient oestradiol serum levels on th
2021-12-27
In the present study, recipient oestradiol serum levels on the day of donor oocyte retrieval or warming were found to be significantly higher in the antagonist group and higher than 100 pg/ml in all cases. Serum oestradiol level has been reported to have no effect on endometrial receptiveness in ooc
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A high throughput screening campaign of the Lilly
2021-12-27
A high-throughput screening campaign of the Lilly corporate compound collection led to the discovery of as potent and selective inhibitor of GlyT1 (IC=45nM, GlyT2 IC>30,000nM). In addition to the characteristic -methyl glycine moiety as acidic head group and the novel ethanolamine linker, also cont
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In summary we discovered azaindole
2021-12-27
In summary, we discovered 7-azaindole substituted -hydroxypyridone as a potent zinc-binding GLO1 inhibitor (IC=11nM) through lead generation from HTS and structure-based inhibitor design. The X-ray cocrystal structure and the comparison of binding energies with the indole counterpart revealed that
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We recently reported the first cyclopropene analog of the
2021-12-27
We recently reported the first cyclopropene-analog of the amino caged compounds neurotransmitter glutamate (Fig. 2A) [27]. This first-generation cyclopropene-glutamate expanded the only other documented report of a cyclopropene-neurotransmitter (cyclopropene-GABA analog by Reissig and coworkers) [2
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