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The biochemical cell culture activities and properties of bi
2021-12-20
The biochemical, cell culture activities and properties of bicyclic carboxamides are compiled in , with the prototype of the series, 4-fluorobenzyl carboxamide , displaying an antiviral profile comparable to the spirocyclic carboxamide . The introduction of a small hydrophobic methyl () and chlori
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The effects of C on the NF B pathway
2021-12-20
The effects of C646 on the NF-κB pathway could be explained by the role for p300 that has been described in the regulation of the NF-κB pathway [5]. For instance, acetylations of the p65 NF-κB subunit on lysines 218, 221 and 310 are mediated by the HATs p300 and PCAF [11] and increase transcriptiona
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In summary we propose a
2021-12-18
In summary, we propose a model that explains the possible mechanism the HULC mediates activation of HBV in liver cancer Punicalin (Fig. 8). In the model, HULC promotes the expression of miR-539 by stimulating HBx-co-activated STAT3. Then, miR-539 down-regulates APOBEC3B, leading to an increase of H
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A nitric oxide donor glyceryl
2021-12-18
A nitric oxide donor, glyceryl-trinitrite, and the substrate for nitric oxide, l-arginine, have been used to treat preterm labor. However, these studies are preliminary. The beneficial effect of nitric oxide donors needs to be confirmed by more controlled studies. The probable pitfall of using nitri
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After establishing improved GSNOR potency some of the potent
2021-12-18
After establishing improved GSNOR potency, some of the potent inhibitors were further evaluated for microsomal stability and CYP inhibition studies (). Majority of the tested analogs revealed high metabolic stability in human and rat liver microsomes, and moderate to low stability in mouse liver mic
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In addition researchers studying GPR agonists favor the deve
2021-12-18
In addition, researchers studying GPR119 agonists favor the developing of candidate drugs that are more potent than DPP-4 inhibitors given that the latter are moderate agents in the treatment of DM. Although it masitinib is unclear why Sanofi-Aventis chose to terminate collaboration with Metabolex
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The unique ability of R PabI to specifically excise
2021-12-18
The unique ability of R.PabI to specifically excise EPZ 005687 from a palindromic sequence is based on a novel structural architecture that is distinct not only from other DNA glycosylases but also from other proteins [88]. In the absence of DNA, R.PabI forms a dimer with a central, highly twisted
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Pediatric cancers are fundamentally different from adult
2021-12-18
Pediatric cancers are fundamentally different from adult tumors and usually display a lower mutational burden and a faster growth rate. About 30% of all childhood malignancies are solid tumors and, in a majority of cases, respond well to chemotherapy. However, in particular in neuroblastoma the succ
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Transient forebrain ischemia in rodents induces
2021-12-18
Transient forebrain ischemia in rodents induces a reduction in expression of mRNA encoding the AMPA receptor subunit GluR265, 66, 67, 68, 69 (Fig. 3). gluR2 mRNA expression is markedly reduced in the CA1 region (the Z-FA-FMK australia region most vulnerable to ischemia-induced damage), but not in t
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Consistent with recent independent studies we confirm that t
2021-12-18
Consistent with recent independent studies, we confirm that the GCG-induced increase in oxygen consumption is only partially blunted in Fgf21−/− mice [32], implicating additional GCGR-dependent mechanisms contributing to the acute GCG-dependent enhancement of energy expenditure. Notably, glucagon ad
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br Declaration of competing interests
2021-12-17
Declaration of competing interests Acknowledgements The authors wish to thank the Natural Science Foundation of Jiangsu Province (BK20171261), the project of outstanding scientific and technological innovation group of Jiangsu Province, the National Science Fund for Distinguished Young Scholar
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LPCs have been previously described as potential
2021-12-17
LPCs have been previously described as potential anti-diabetic factors due to stimulation of secretory activity from the isolated rodent pancreas, L-type cells, ands insulin-producing cell lines, with LPC 18:1 as the main structure of interest (Soga et al., 2005, Sakamoto et al., 2006, Overton et al
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To meet the requirement of ferroptosis based therapy
2021-12-17
To meet the requirement of ferroptosis-based therapy, a couple of small molecule drugs and nanomaterials were introduced to the design of ferroptosis inducers, separately. As we know, iron is a key regulator of ferroptosis. When small molecule drugs are employed to induce ferroptosis, the endogenous
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The release of FBPase and aldolase from
2021-12-17
The release of FBPase and aldolase from subcellular structures of muscle was dependent on the presence of the crowding agent imitating the physiological conditions – PEG 8000 (Table 1). The amount of both enzymes associated with structures of muscle mma f was about 6–7 times higher in the presence o
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Adipocytes play diverse roles in energy homeostasis
2021-12-17
Adipocytes play diverse roles in energy homeostasis by controlling energy consumption [8] and function as a source of proteins and cytokines, which mediate numerous physiological functions [9]. Excessive accumulation of adipocytes, as well as an increase in either their size or number, causes obesit
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