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br Sources of funding br Disclosures
2020-12-31
Sources of funding Disclosures Acknowledgments Introduction Insulin secretion from pancreatic β cells is a fundamental process to maintain blood glucose homeostasis. During glucose-stimulated insulin secretion, high glucose causes closure of ATP-sensitive K+ channels (KATP channels), sub
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Caspase Inhibitor Set I Since the dideoxy analogues and
2020-12-31
Since the 1,2-dideoxy analogues, and , served as substrates for TgTCEA and TgTCEB, respectively, with the higher affinity (lower ) and lower turnover number (lower ) than their authentic substrates, PosA and PosB (such trend was more evident on analogue for TgTCEB than on analog for TgTCEA), an i
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While we previously demonstrated that
2020-12-30
While we previously demonstrated that TraG is inhibited by specific transglycosylase inhibitors and that enzymatic activity is strongly reduced upon mutation of the potential catalytic core (Arends et al., 2013), the enzymatic mechanism of both domains was not assigned. Here, by mass spectrometry an
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In the context of E ligase drug
2020-12-30
In the context of E3 ligase drug discovery, it is critical to identify the appropriate E2/E3 substrate pairing to ensure the development and use of the most physiologically relevant screening assay. There have been many reports of limited E2/E3 activity profiling with a small number of E2 and E3 LY2
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Our data supports the conclusion
2020-12-30
Our data supports the conclusion that the exonuclease activity thought to be intrinsic to Artemis is not a component of the Artemis polypeptide. Many possibilities exist to explain the presence of the exonuclease activity in less-pure fractions of Artemis. It is possible that the exonuclease is simp
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In most cases patients will not present immediately after
2020-12-30
In most cases, patients will not present immediately after SM exposure because SM-induced clinical symptoms typically occur after a latency period of several hours [8], [9], [10]. When they do present, the detection of free, unbound alkylating agent is highly unlikely. For this reason, available rap
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KT203 Finally this study described that
2020-12-30
Finally, this study described that the lead KT203 (1) acted as an efficient alkylating agent for the G4 structure in addition to the previously reported T-T mismatch structure. The shortcoming of probe (1) is the lack of a structure selectivity, but that can be overcome by changing the acridine scaf
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Despite low respiratory rates in citrus
2020-12-30
Despite low respiratory rates in citrus fruit, prolonged periods of storage may cause significant changes in the levels of organic acids (Echeverria and Valich, 1988). V-ATPase and V-PPase catalyze the electrogenic H+ translocation from the cytosol to the vacuolar lumen to generate an inside-acid pH
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Xenobiotic metabolism primarily occurs in liver which contai
2020-12-30
Xenobiotic metabolism primarily occurs in liver, which contains many enzymes to catalyze the transformation of xenobiotic. Usually, cytochrome P-450s (CYP450s) act as the first response for biotransformation of xenobiotic in organisms. CYP450s generally consist of various subfamily enzymes which can
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The in vitro enantioselective metabolism of pesticides has b
2020-12-30
The in vitro enantioselective metabolism of pesticides has been investigated by employing human liver microsomes, which are a reliable resource to perform MCL enantioselective risk assessment in humans (Carrão et al., 2019; de Albuquerque et al., 2018, 2016; Yao et al., 2016). The enantioselective m
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Deregulated Wnt signaling either due
2020-12-30
Deregulated Wnt signaling, either due to pathway mutations or otherwise aberrant pathway activity, is common in CLL [81], [82]. In addition to targets described above, alvocidib also inhibits glycogen synthase kinase 3 (GSK3)-β at higher nanomolar concentrations [37]. Despite intuition and experimen
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The majority of pro inflammatory cytokines are regulated by
2020-12-30
The majority of pro-inflammatory cytokines are regulated by NFκB, and recently, it has been found that p38 MAPK partly regulates NFκB-driven gene atomoxetine hcl mg by increasing the association of the basal transcriptional factor, TATA-binding protein, with the C terminus of p65 subunit of NFκB and
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LY2606368 HCl Our previous studies have shown
2020-12-30
Our previous studies have shown that in a preimplantation mouse embryo the proportion of inner to outer cells (i.e. precursors of ICM and TE, respectively) is regulated by a different frequency of differentiative cell divisions at the 8- and 16-cell stages. Low number of inner blastomeres generated
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br The orphan estrogen related receptor
2020-12-30
The orphan estrogen-related receptor exists as three subtypes (ERRα, ERRβ, and ERRγ) in the human genome. ERRα is expressed in metabolically active tissues such as muscle and adipose. ERRγ is expressed in the spinal cord and CNS. ERRβ appears to play a role in development, as postnatal expression
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While previously reported optimizations on compound focused
2020-12-30
While previously reported optimizations on BGJ 398 focused on the phenyl ring A () and substituents on isoxazole ring, other alternatives to replace isoxazole ring were never explored. Herein, we propose to replace the isoxazole with its bioisosteric substituted phenyl ring B () to explore new che
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