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In this study according to the critical pharmacophore
2021-12-27

In this study, according to the critical pharmacophore T31, Y113 and R140 of FBPase, using the strategy of pharmacophore-based virtual screening, a series of novel scaffold inhibitor targeted the AMP binding site of FBPase were screened, their inhibitory activities against FBPase were further tested
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Atglistatin Over of all melanomas have activating BRAF mutat
2021-12-27

Over 50% of all melanomas have activating BRAF mutations [29] and inhibition of the Ras/Raf/MEK/ERK signaling pathways is one of the most promising treatments for malignant melanoma [30]. However, studies using BRAF inhibitors have identified various feedback mechanisms to activate BRAF pathway in m
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The top panel of Fig depicts the
2021-12-27

The top panel of Fig. 3 depicts the average number of planaria visible during each observation for all cohorts in the group testing following light exposure. Although there was considerably more variability than in the light-exposure conditions, a t-test showed no significant difference in count bet
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In an effort to further improve the intrinsic potency
2021-12-27

In an effort to further improve the intrinsic potency, we evaluated the effect of the C4-substituent of the triazole (). Replacement of the phenyl group with a cyclohexyl or with a 2-pyridyl substituent led to losses in potency. Increasing the size of the substituent to a bi-phenyl or naphthyl gr
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br Animal models of NASH The human
2021-12-27

Animal models of NASH The human NAS system (see above) is largely reproducible in NAFLD mouse models [37] and, therefore, has been increasingly applied in the preclinical assessment of liver histological responses to test compounds. In general, the NAS system is well suited for this purpose, alth
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It has been found that WHI
2021-12-27

It has been found that WHI-P131, a JAK3 inhibitor, induced apoptosis of CD4+ T MPTP hydrochloride (Cetkovic-Cvrlje et al., 2012). Also, other JAK3 inhibitors (AG490 and WHI-P154) caused apoptosis in anaplastic large cell lymphoma (Amin et al., 2003). Taking into account the proapoptotic action of J
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In conclusion the present study demonstrated that
2021-12-27

In conclusion, the present study demonstrated that peripheral nerve exposure to HIV gp120 increased the expression levels of the P2Y12 receptor in DRG SGCs and enhanced mechanical and thermal hyperalgesia in rat models. Up-regulation of the P2Y12 receptor in DRG SGCs further promoted the release of
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There are three classes of receptors for
2021-12-27

There are three classes of receptors for herpes virus gD have been described [18,24]. Among those three, herpes virus entry mediator A (HveA) is also known as HVEM. This receptor is a member of the tumor necrosis factor receptor (TNFR) superfamily [25]. The other class of receptors is HveC which is
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In this report we characterized MRJP containing aggregates
2021-12-27

In this report, we characterized MRJP-containing Caspase-6, human recombinant protein and other (glyco)proteins from honey. Honey glycoproteins demonstrated potent anti-C. elegans activity. It has been reported that molecules that kill C. elegans are likely to be toxic to parasitic nematodes (Burns
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Glutamate is a ubiquitous principal excitatory
2021-12-27

Glutamate is a ubiquitous principal excitatory neurotransmitter in the comt inhibitors that plays a central role in a variety of brain functions (Delgado, 2013, Hawkins, 2009). Several studies reported that CSF glutamate was associated with mental illness, including major depressive disorder, anxio
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The lactam compounds including ceftriaxone CEF have shown to
2021-12-27

The β-lactam compounds, including ceftriaxone (CEF), have shown to attenuate drug-seeking in several drugs of abuse including methamphetamine [31], cocaine [32,33], nicotine [34] and morphine [35]. Moreover, in our laboratory, we have shown that CEF can reduce chronic alcohol drinking via upregulati
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In teleosts GR is expressed in almost every cell and
2021-12-27

In teleosts, GR is expressed in almost every cell and regulates genes controlling development, metabolism, and immune response [17,18]. Several teleosts contain two GR genes, GR1 and GR2 [8]. Other groups have found only one GR in some species thus far, such as the Japanese flounder, brown trout, an
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Many neutral and acidophilic galactosidases have been
2021-12-24

Many neutral and acidophilic β-galactosidases have been purified from microorganisms [14], while only a few alkalophilic β-galactosidases have been reported [19]. An alkalophilic β-galactosidase, BGal_375, was obtained and researched for the characterization of its hydrolytic activity. BGal_375 show
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Knock out mice of FXR
2021-12-24

Knock-out mice of FXR showed enhancing cholesterol metabolism in vivo and reducing serum levels of total cholesterol. Additionally, the results of FXR-deficiency mice revealed potential effects on the improvement of obesity and diabetes.19, 20 As a natural FXR ligand, guggulsterone possesses antagon
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FFAs concentration response curves for increasing intracellu
2021-12-24

FFAs concentration–response curves for increasing intracellular calcium and receptor phosphorylation showed a difference of ≈1 order of magnitude indicating a relatively large receptor reserve, which is expected for a transfected model, and that high receptor occupancy is necessary to induce recepto
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