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The two competitive bivalent GlxI inhibitors polyBHG nM and
2022-08-26

The two competitive bivalent GlxI inhibitors polyBHG2-62 (=1nM) and polyBHG2-54 (=0.3nM) () were designed based on the transition-state analog -(-bromophenyl--hydroxycarbamoyl) glutathione (BHG) by an examination of the X-ray crystal structure of human GlxI in complex with one CHG at each active sit
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The SNPs of candidate genes
2022-08-25

The SNPs of candidate genes may exert their effect on associated traits through changing of gene expression (Bonafe et al., 2003, Wyszynska-Koko et al., 2006). In agreement, GHSR SNPs were significantly associated with upregulation of this gene in the pituitary gland of GG/GG chickens. The GHRL/GHSR
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Inflammatory pain is very common in the clinic A study
2022-08-25

Inflammatory pain is very common in the clinic. A study demonstrated that galanin was upregulated after nerve injury or inflammation (Ma and Bisby, 1997). It has been reported that galanin plays an important role in the transmission of nociceptive information in the spinal cord of rats with inflamma
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The co crystal structure of GPR complexed with TAK
2022-08-25

The co-crystal structure of GPR40 complexed with TAK-875 provided precise structural information for the rational design of novel GPR40 agonists. The key interactions between the carboxylate with the residues Arg183, Arg258, Tyr91 and Tyr240 of GPR40 were observed. And Trp174ECL2 was oriented nearly
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br G protein coupled receptor
2022-08-25

G-protein coupled receptor 40 (GPR40), also known as a free fatty Ketoconazole receptor, is dominantly expressed in pancreatic β cells and intestine K, L cells., . Besides, GPR40 is also reported to be expressed in brain, but its function is still unknown. It is well documented that GPR40 agonist
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Parkinson s disease is another neurodegenerative disorder af
2022-08-24

Parkinson's disease is another neurodegenerative disorder affecting H3Rs. The most common clinical symptoms of this disease are rigidity, bradykinesia, rest tremor, loss of postural reflexes, and gain impairment owing to progressive degeneration of the dopaminergic neurons in the nigro-striatal neur
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YAP TAZ nuclear function is also influenced by
2022-08-24

YAP/TAZ nuclear function is also influenced by interaction with the TEAD family of transcription factors [96, 97, 98, 99, 100, 101]. The RAC1 Dextran sulfate sodium salt exchange factor protein TIAM1 has recently been linked to YAP/TAZ regulation in the nucleus and cytoplasm. Nuclear TIAM1 inhibits
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Based on our results we propose
2022-08-24

Based on our results, we propose three possible mechanisms of HER2 loss after trastuzumab-based therapy (Fig. 3). The first possibility is a result of the differential effects of treatments on clonal subsets. In breast cancer, such selective pressure has been suggested to preferentially eradicate HE
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Based on our results we propose
2022-08-24

Based on our results, we propose three possible mechanisms of HER2 loss after trastuzumab-based therapy (Fig. 3). The first possibility is a result of the differential effects of treatments on clonal subsets. In breast cancer, such selective pressure has been suggested to preferentially eradicate HE
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A series of P P ureas were explored first
2022-08-24

A series of P3-P4 ureas were explored first and their anti-NS3 protease activity, antiviral properties in a HCV replicon cell-based assay and PK profiles examined. Installation of a methyl group on the P4 side nitrogen Firefly Luciferase mRNA of the urea yielded , a molecule which retained intrinsic
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br Consequence physiological function of ROS dependent inhib
2022-08-24

Consequence/physiological function of ROS-dependent inhibition of GSNOR Plants response to environmental changes induced by abiotic and biotic factors by enhanced accumulation of ROS resulting in temporary imbalance of the cellular redox homeostasis. This as oxidative stress/burst termed event tr
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To further investigate the relationship
2022-08-24

To further investigate the relationship between the pro-neurogenic and therapeutic actions, we analyzed the effect of VP2.51 in the presence of the antimitotic agent TMZ. No overt side effects were found at the time of testing as assessed by direct observation of the behavior of the animals in their
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The observed glucose intolerance and
2022-08-24

The observed glucose intolerance and elevated fasting blood glucose in this study is in consonance with earlier study (Ferris and Kahn, 2012). These have been the common features of GC exposure and are not unexpected. Previous researches that reported IR during GC exposure have shown controversy con
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Nogo-66 (1-40) Several previous reports have demonstrated th
2022-08-24

Several previous reports have demonstrated that epithelial cell migration is important in promoting mucosal repair after damage caused by DSS and nonsteroidal anti-inflammatory drugs [33], [34], [35]. Cell migration is coordinated by many factors, including fibronectin and its receptor integrin α5,
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After initial validation of the
2022-08-24

After initial validation of the ability of Ad5-Cre virus to express Cre recombinase protein in glial cells in vitro and in vivo, we employed this virus to induce site-specific deletion of our target GlyT1 in the thalamus, through injection of the cKO GlyT1 mice. This transgenic line was constructed
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