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br Introduction Glucokinase GCK hexokinase IV is
2022-02-23

Introduction Glucokinase (GCK, hexokinase IV) is a monomeric enzyme that catalyzes the ATP-dependent conversion of glucose to glucose 6-phosphate, the first and rate-limiting step of glycolysis in the liver and pancreas [1,2]. GCK was first discovered in the early 1960's, and shortly thereafter i
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DNAzymes a series of nucleotide sequences with specific cata
2022-02-23

DNAzymes, a series of nucleotide sequences with specific catalytic activity, have been reported frequently applied in detection assays for such as ions and amino acids, due to the advantage in stability, high cost-effectiveness and modification convenience, by comparison with protein enzymes. The DN
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We have previously designed an azobenzene
2022-02-23

We have previously designed an azobenzene-based molecule, Razo, which could switch the conformations of G-quadruplex structures by photoregulation. 12, 13, 14, 15 However, it lacks selectivity to different G-quadruplexes. Therefore, we want to find a way to modify this molecule so that it could be u
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One effective approach to fine tuning the
2022-02-23

One effective approach to fine-tuning the lipophilicity profile of FFA1 agonists is to ‘decorate’ the 3-phenylpropahoic Benazepril HCl receptor scaffold with polar heterocyclic moieties. Alternatively, this scaffold could be replaced with heterocyclic isosteres (as in Takeda’s compounds 1,2 and 3 a
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Growing evidence supporting the anti
2022-02-23

Growing evidence supporting the anti-inflammatory and tissue-protective effects of FPR antagonists led to the screening of commercial libraries for novel small-molecule FPR antagonists. As result of these screening efforts and/or structure–activity relationship (SAR)-directed design and synthesis, a
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Attractively existing reports suggest that cellular ferropto
2022-02-23

Attractively, existing reports suggest that cellular ferroptosis also probably plays vital role in liver fibrosis [[62], [63], [64]]. Carlson BA et al. illuminated that the ferroptosis regulator GPX4 was important for hepatocyte survival and proper liver function [62]. Sun X et al. showed that Nrf2
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Results of studies on fish FBPase are somewhat confusing
2022-02-23

Results of studies on fish FBPase are somewhat confusing: although fishes skeletal muscles possess relatively high FBPase activity (Knox et al., 1980, Lushchak et al., 2001) and the isozyme present therein has kinetic properties typical to all vertebrates muscle FBPases (Rosenmann et al., 1977), inv
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br Materials and methods br Results br Discussion The
2022-02-23

Materials and methods Results Discussion The development of HCC is a multistep process involving the accumulation of multiple genetic and epigenetic alterations that lead to the activation of oncogenes and inactivation of tumor suppressor genes [20]. Frequent intrahepatic or pulmonary metas
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br Materials and methods br Results and
2022-02-23

Materials and methods Results and discussion Conclusion The as-designed system was based on the assembly of MSN-Cy and TPGS, which was dominated by π-π stacking interactions. By the strong mutual force, Cypate and TPGS formed a compact layer around the MSN core, which blocked the drug leaka
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In addition to indoles two
2022-02-23

In addition to indoles –, two additional structural variants were synthesized to explore the synthetic flexibility and structure–activity relationships of this system. The first of these was the homologation of the acetic Vidofludimus side chain to prepare compound (). The extension of the chain w
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br Acknowledgements This research was
2022-02-22

Acknowledgements This research was supported by the Natural Sciences and Engineering Council of Canada (NSERC) Discovery Grant awarded to RGM. LMW was supported in part by fellowships from the University of Regina and the Government of Saskatchewan Fish and Wildlife Development Fund (FWDF). We wo
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PDEs block GUCY C associated
2022-02-22

PDEs block GUCY2C-associated second messenger signaling by degrading cyclic nucleotides, whereas inhibition of PDEs activity prevents cyclic nucleotide degradation (Fig. 1). Several researchers have described the pathophysiological roles of various PDEs in numerous tumor cell types, including CRC AR
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Electrostatic potential along with measurement and modeling
2022-02-22

Electrostatic potential along with measurement and modeling of corresponding energies is vital for inferring protein properties, lone or complexed with ligands. DelPhi was used for solving Poisson Boltzmann equation, obtaining grid, total reaction and coulombic energies after solvating the proteins
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GW was also the starting point for a study by
2022-02-22

GW4064 was also the starting point for a study by an independent research group. The co-crystal structure of GW4064 with FXR suggested the potential for favorable hydrogen bond interactions between the isoxazole 3-aryl group and several receptor residues such as Tyr373 and Ser336. Replacing the 2,6-
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SGC-CBP30 Previously we have shown that the natural flavonoi
2022-02-22

Previously, we have shown that the natural flavonoid compounds that possess C-4 ketone group and C-5 hydroxy group, such as baicalein, luteolin, myricetin and quercetin, effectively inhibit human GLO I. Considering our interest in inhibitors of GLO I and based on the rationale mentioned above, struc
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