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To date types of glucose
2022-07-16
To date, 14 types of glucose transport protein have been discovered, each having its own specific functions with different distributions [33]. Among these, GLUT4 is particularly important for maintaining glucose metabolism homeostasis and insulin sensitivity, since it is involved in glucose transpor
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br BA induced activation of TGR TGR is
2022-07-16
BA-induced activation of TGR5 TGR5 is a membrane-bound G protein-coupled receptor for BAs and its activation is dependent on cAMP formation and further stimulation of protein kinase A [53], [31]. The receptor is expressed in the enterochromaffin cells, smooth muscles, immune cells and more import
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We have isolated various bioactive peptides acting
2022-07-16
We have isolated various bioactive XI-006 acting by binding to the receptors of endogenous bioactive peptides such as opioid, bradykinin, neurotensin, and complements C3a and C5a etc. [24]. Rubimetide is the first example of an agonist peptide of the FPR2 of exogenous origin. Anxiolytic-like activ
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A frequent complication of SIRS and sepsis is the developmen
2022-07-16
A frequent complication of SIRS and sepsis is the development of increased airway resistance and lung inflammation [2], [3]. For example, Uhlig et al. [3] demonstrated that rat lungs exposed to endotoxin present increased airway resistance due to constriction of terminal Methylprednisolone [3] Moreo
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Having shown that some of substitutions
2022-07-16
Having shown that some of substitutions (Cl, CF) at the 2-position of the thiophene improved rat microsomal stability, and polar groups at the 4-position of the aryl ring had a beneficial effect on stability in both human and rat microsomes, we combined these features in a new set of analogs. Methyl
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In conclusion the data reported in
2022-07-15
In conclusion, the data reported in this study have demonstrated an important role for FAAH substrates in the UNC2025 receptor in the modulation of TLR4-induced neuroinflammatory and associated anhedonic responses, but not acute sickness behaviour. Such potent neuroimmunomodulatory effects were sho
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Hippo signaling is unique in that it does
2022-07-15
Hippo signaling is unique in that it does not possess a cognate ligand and receptor system. Instead, numerous upstream sensors that monitor cell morphology, cell polarity, cell-cell contact, and mechanical stress impinge onto the Hippo pathway core kinases, MST, and LATS. This in turn indicates the
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Consideration must be given to
2022-07-15
Consideration must be given to both the tissues themselves and to infiltrating immune cells. As highlighted by Maxwell and Eckardt [88], clinical trials of compounds targeting these pathways will require large numbers of participants and prolonged follow-up to identify rare and late complications or
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The first suggestion that the Hh pathway might
2022-07-15
The first suggestion that the Hh pathway might be involved in the pathogenesis of chronic liver disease was reported at the beginning of this millennium by Shackel et al. who noted that Patch and Gli were upregulated in their microarray analysis of liver tissues from patients with primary biliary ch
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LDE225 Diphosphate Currently the computational chemical biol
2022-07-15
Currently, the computational chemical biology has been applied in hepatitis B antiviral drug discovery research [18]. Tan et al. explored oxime ethers as HBV inhibitors by docking and screening [19]. Allen et al. clarified the resistance of HBV to the nucleoside drug lamivudine [20]. The results sug
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In our previous studies examining erectile responses in sGC
2022-07-15
In our previous studies examining erectile responses in sGCα1−/− mice, we found that the sGCα1 subunit was required to obtain proper erectile responses to substances generally known to exert their actions by sGC.17, 18 Based on our previous observation of residual relaxing responsiveness to exogenou
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The urinary levels of OHP among
2022-07-15
The urinary levels of 1-OHP among the exposed workers were higher than those reported for a Brazilian group of charcoal workers (0.07 μmol mol creatinine) exposed to wood smoke (Kato et al., 2004), and for nonsmoking bus drivers (0.19 μmol mol creatinine) and nonsmoking mail carriers (0.11 μmol mol
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Acute in vivo experiments were performed
2022-07-15
Acute in vivo experiments were performed in normoglycemic 129SVE mice to confirm GPR119 activation and corresponding CHC receptor control. GIP release was utilized as a biomarker for target receptor engagement and plasma GIP levels were measured 45min after oral dosing (). Both 3 and 10mg/kg produc
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Gabapentin A number of synthetic GPR
2022-07-15
A number of synthetic GPR119 agonists have been reported to date, several of which have advanced into clinical trials. Reported GPR119 agonists are often composed of three parts as depicted in : a piperidine or a piperazine ring -substituted with a carbamate or a heteroaryl group at the right side,
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The mD gene obtained from Dr
2022-07-15
The mD1.2 gene obtained from Dr. Dimiter S. Dimitrov was inserted into a pComb3X vector. The transcription and translation of pComb3X plasmid in cells is inhibited by rifampicin, which binds to bacterial DNA-dependent RNA polymerase. However, in the strain BL21 (DE3) expression system, there is over
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