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Encouraged by this observation a systematic SAR study on
2023-03-02

Encouraged by this observation, a systematic SAR study on the A ring -alkoxy was conducted as summarized in . The A ring methoxy-containing KRCA-0008 was proven an optimal substituent in terms of potency after all and its bigger size derivatives were detrimental in both biochemical and H3122 cellula
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br Conclusion br List of abbreviations br
2023-03-02

Conclusion List of abbreviations Acknowledgment The studies performed by our laboratory and presented in this review were supported by the Ministry of Education, Culture, Sports, Science and Technology of Japan, (KAKENHI 17590618 [to H.I.] and KAKENHI 22249017 [to Y.Y.]), and the Japanese S
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The diagnosis of ICP is
2023-03-02

The diagnosis of ICP is currently based on the presence of pruritus, raised fasting serum TBS levels above 10μmol/L, and/or elevated serum transaminases (in the absence of diseases that cause cholestasis or pruritus) as well as spontaneous relief of signs and symptoms within four to six weeks after
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In the mammalian brain synapse
2023-03-02

In the mammalian brain, synapse formation is followed by a period of synapse refinement, and autophagy has been shown to play an important role in this process. For example, Tang and colleagues found that autophagy is required for the developmental pruning of dendritic spines, and that this pruning
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In the mammalian brain synapse
2023-03-02

In the mammalian brain, synapse formation is followed by a period of synapse refinement, and autophagy has been shown to play an important role in this process. For example, Tang and colleagues found that autophagy is required for the developmental pruning of dendritic spines, and that this pruning
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To identify the kinase s mediating H
2023-03-02

To identify the kinase(s) mediating H3.3S31 phosphorylation, we devised a 96-well-plate-compatible immunostaining assay, with Iohexol specific for H3.3S31ph, and utilized it to screen both a Qiagen siRNA library covering 720 human kinases and a kinase inhibitor library (Selleck) containing 194 comp
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Consistent with a damaging role for
2023-03-02

Consistent with a damaging role for increased 12/15-LOX activity in stroke, systemic administration of the 12/15-LOX inhibitor, LB1, 2 h after permanent focal cerebral ischemia significantly reduced infarct size 24 h after the ischemia, and the treatment group demonstrated improved behavioral and he
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br Materials and Methods br Results br Discussion XHP is
2023-03-01

Materials and Methods Results Discussion XHP is a traditional Chinese anti-cancer medicine that is widely used for the treatment and adjuvant treatment of breast cancer. XHP has been shown to induce apoptosis in various breast cancer mps1 in vitro, including Hs578T, MCF-7, and MDA-MB231 cel
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br Conclusions br Introduction In the modern life of
2023-03-01

Conclusions Introduction In the modern life of humans, Aliskiren receptor are widely prescribed for therapy against bacterial diseases to prevent the onset of bacterial infections during a viral disease (Goossens et al., 2005; Van Boeckel et al., 2014). They have been massively administered a
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Based on structure activity relationship of several
2023-03-01

Based on structure activity relationship of several SARM templates, Ligand Pharmaceuticals chose LGD2226 as their first clinical candidate (Miner et al., 2007). Although LGD2226 demonstrated myo- and osteo-anabolic activity and maintenance of sexual function in various preclinical models, the develo
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Treatment of RAW cells with AP
2023-03-01

Treatment of RAW264.7 Zafirlukast with AP(+)-exosomes caused an increase in their phagocytic activity. In the presence of amastatin, phagocytic activity was not completely suppressed, suggesting that at least two components were responsible for the activity; one of which is aminopeptidase(s). When
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ERAP has been crystallized in two different conformations wh
2023-03-01

ERAP1 has been crystallized in two different conformations, wherein the C-terminal domain IV is either closely interacting with domains I/II and enclosing the active site (termed ‘closed’), or is rotated away in a hinge motion which exposes the active site (‘open’). This large motion correlates with
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These findings suggest that eventually more than
2023-03-01

These findings suggest that eventually more than one 12/15-lipoxygenase isoform may play a role in human atherosclerosis. Humans have two 12-lipoxygenases and two 15-lipoxygenases which show different expression patterns, substrate specificities and stereo-selective metabolism [1]. However, in IRAK
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Moreover mice exposed to high cholesterol diet have mildly a
2023-03-01

Moreover, mice exposed to high-cholesterol diet have mildly activated astrocytes, increased expression of ApoE and aquaporin-4 in the hippocampus, and altered levels of proteins associated with Aβ metabolism (Chen et al., 2016), which is related to a higher demand for cholesterol transport and the n
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We stimulated HNEpC cells with LPS found
2023-03-01

We stimulated HNEpC cells with LPS found that the secretion of inflammatory cytokines and the expression of AHR was increased significantly, and miR124 was reduced. It has been found that LPS as a foreign substance can bind to the TLR family of proteins to activate intracellular AHR signaling [[19],
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