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Some aspects of intercellular Ca wave spread are similar
2022-08-18
Some aspects of intercellular Ca2+ wave spread are similar to the phenomenon of spreading depression and associated with migraine headache [57]. These depolarization waves, followed by electrical inhibition, are evoked by transient hypoxia and other types of pim kinase inhibitor injury and spread s
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Two excellent GSMs with clear pharmacological effect
2022-08-18
Two excellent GSMs with clear pharmacological effect across rats, dogs, monkeys, and human subjects are BMS-932481 and BMS-986133 with IC50 at 6.6 and 3.5 nM to reduce Aβ42, respectively. Both GSMs exhibit dose- and time-dependent activity in vivo by decreasing Aβ1-42 and Aβ1-40 levels while increas
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Another small compound targeting IBAT has
2022-08-18
Another small compound targeting IBAT has been evaluated in Phase I clinical trial (EudraCT 2013-001175-21) [86]. The oral administration of A4250 to healthy subjects did not give rise to any serious adverse events, was well tolerated and had a similar safety profile as elobixibat; however, it cause
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Emerging evidence has shown that pharmacological FXR agonism
2022-08-18
Emerging evidence has shown that pharmacological FXR agonism attenuates chronic alcohol treatment-induced liver injury and steatosis [18], [19], while whole-body FXR knockout worsens alcohol-induced liver injury [19]. This suggests that FXR plays an important role in ALD development. However, defici
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br Experimental br Acknowledgments br Human immunodeficiency
2022-08-18
Experimental Acknowledgments Human immunodeficiency virus-1 (HIV-1) is the causative agent of acquired immunodeficiency syndrome (AIDS), and without treatment results in a debilitating disease that cripples the immune system of the patient, increasing susceptibility to opportunistic diseases
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br STAR Methods br Acknowledgments We thank Emeritus Profess
2022-08-18
STAR★Methods Acknowledgments We thank Emeritus Professor Chikashi Shimoda and Professor Taro Nakamura of the National BioResource Project/Yeast Genetic Resource Center (NBRP/YGRC) at Osaka City University (Osaka, Japan) for Schizosaccharomyces pombe meiotic cDNA library, yeast plasmids, yeast
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Finally worth of mention are few papers
2022-08-17
Finally, worth of mention are few papers that report on the discovery of HO-2 selective inhibitors. In 2013, starting from the screening of a Mepivacaine HCl library, the above-mentioned Canadian research group identified Clemizole (Table 6) as a new hit compound for the development of the first se
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br Introduction Topological hedgehogs keep generating intere
2022-08-17
Introduction Topological hedgehogs keep generating interest in point-set topology as they are a rich source of counterexamples and applications (for a comprehensive survey on topological hedgehogs we refer to [1]; see also [9]). They may be described as a set of spines identified at a single poin
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br Acknowledgements This work was financially
2022-08-17
Acknowledgements This work was financially supported by the National Natural Science Foundation of China (Grant No. 81803033) and the “Double First-Class” University project (CPU2018GF02). Introduction Atrial fibrillation (AF) is the most common progressive cardiac rhythm disorder. Studies ha
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It is important to note that
2022-08-17
It is important to note that upon RIG-I activation, IRF-3, p38, and ERK were activated by 3p-siHBx, leading to upregulated IFN response (Fig. 6). This suggests that 3p-siHBx has specific effects on HBV replication. In addition, 3p-siHBx induced type III IFN response (Fig. 6D), which could also inhib
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br Discussion Regulation of redox homeostasis is critical
2022-08-17
Discussion Regulation of redox homeostasis is critical in the maintenance of normal cell functions, and both glutathione S-transferase and peroxiredoxin enzymes are important contributors to this process. There are numerous reports of aberrant expression patterns of GSTP linked with cancer and wi
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The number of small molecule GSK inhibitors is continuously
2022-08-17
The number of small molecule GSK-3 inhibitors is continuously rising and many have been tested in animals. These studies have provided additional support for specific roles of GSK-3 in neuronal functions under both normal and pathological conditions. Inhibition of GSK-3 has profound effect on neurop
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Calcium mobilization FLIPR assay CHO K cells
2022-08-17
Calcium mobilization (FLIPR) assay: CHO-K1 cells expressing an NFAT-β-lactamase reporter and the promiscuous Gα-subunit Gqi5 were stably transfected with either empty vector (pCDNA3.1, Invitrogen) or vector expressing HA-GPR81, GPR109A or GPR109B. Cells were seeded at 10,000cells/well in 384-well cu
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br Materials and methods br
2022-08-17
Materials and methods Results Discussion In this study, we demonstrated that zaprinast (a cGMP-PDE inhibitor) induced the intracellular calcium mobilization in the Quinupristin-Dalfopristin Complex mesylate coexpressing GPR35 and Gqi5, Gqo5, or Gα16. Induction of intracellular calcium mobil
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In contrast to UDG SMUG
2022-08-17
In contrast to UDG, SMUG1 exhibits dramatically lower product yield in its excision of U, and this is not dependent on sequence context. Though we cannot rule out that a small amount of the product is derived from a duplex contaminant, our extensive purification techniques limit the amount of contam
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