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A number of GCK activators for treating
2022-04-01

A number of GCK activators for treating T2D have been developed and tested but not progressed successfully from clinical trials into therapy [45]. Our observations suggest that increased risk of hypoglycemia might be possible, particularly if drugs penetrate into brain. A further possibility is that
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The HH signaling has also been implicated in the
2022-04-01

The HH signaling has also been implicated in the regulation of cancer stem mk-801 (CSC) by promoting their self-renewal [53]. Activated HH signaling has been identified in CSCs of many solid tumors, such as glioblastoma, breast, colon, pancreatic cancer, melanoma, and hematological malignancies, in
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As ghrelin effects are suspected to be mediated
2022-04-01

As ghrelin effects are suspected to be mediated by a heterogeneous population of G-protein-coupled-receptors [2], [21], other so far unknown subtypes of ghrelin receptors differing from the classical GHSR-1a may additionally exist that might also mediate ghrelin effects on the heart. Thus, the real
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More polar substituents introduced on the position of
2022-04-01

More polar substituents introduced on the 5-position of the aniline ring (e.g., dimethyl amine in ) decreased the lipophilicity of the compounds (4.3 for vs 5.1 for ), but did not affect their potency. For instance, was highly potent in vitro and demonstrated a surprising 51% lowering of Aβ42 in m
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br Materials and methods br Results Bgal
2022-04-01

Materials and methods Results Bgal from Alteromonas sp. ML117 had an open reading frame of 3126 bp encoding 1042 amino ABT-869 residues with a predicted mass of 120 kDa and a theoretical pI (isoelectric point) of 5.44. The recombinant Bgal contained a His tag, as well as other additional amin
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The knowledge that piroxicam competes with ligands that bind
2022-04-01

The knowledge that piroxicam competes with ligands that bind to FPR may be of importance for a deeper understanding of the anti-inflammatory effects possessed by this NSAIDs. It has recently been reported that not only phagocytes but also platelets express FPR on their cell surface and that these re
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In addition to the regulation afforded by
2022-04-01

In addition to the regulation afforded by calcineurin/NFAT axis, it has been shown that deregulation of some microRNAs (e.g. miR-155) can induce activation of Fas/FasL-in various cell types [72]. Furthermore, Fas–FasL interactions appear to be an important mechanism for the maintenance of immune pri
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To evaluate the role of increased
2022-04-01

To evaluate the role of increased FPPS expression in paclitaxel-treated cells, we investigated the effects of FPPS on r407 sale progression. DNA content analysis showed that the number of cells accumulating in the G/M phase increased in a dose-dependent manner in paclitaxel-treated cells (A and B),
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br Hydroxyfarnesyl diphosphate was synthesised in three
2022-04-01

12-Hydroxyfarnesyl diphosphate (6) was synthesised in three steps starting from commercially available (E,E)-farnesol (10) (Scheme 5). Chlorination of 10 gave farnesyl chloride (11) in a quantitative yield, which was carried forward without purification. The following step was a selenium dioxide-c
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Recent findings of us suggest that compounds
2022-04-01

Recent findings of us suggest that compounds that inhibit both FAAH and TRPV1 may be more efficacious in pain relief than those targeting only one such protein. As continuation of our efforts to identify new molecules able to target simultaneously both FAAH and TRPV1 receptors, we hypothesized that
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About of human primary melanomas
2022-04-01

About 67% of human primary melanomas and 56% of melanoma metastases display cytoplasmic or nuclear β-catenin accumulation (Xue et al., 2016). Of note, active β-catenin stimulates emergence of metastasizing melanoma in mice harboring BrafV600E or NrasQ61K hyperplasia (Damsky et al., 2011, Delmas et a
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br Results br Discussion Impaired BBB functions evoke vasoge
2022-04-01

Results Discussion Impaired BBB functions evoke vasogenic edema, which elevates intracranial pressure and leads to a life-threatening condition (Sperk, 1994, Unterberg et al., 2004, Simard et al., 2007). In addition, vasogenic edema formation results in the worsen consequence contributing to p
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br Conflict of interest br Introduction Endometriosis is
2022-03-31

Conflict of interest Introduction Endometriosis is defined as the presence of endometrial glands and stroma outside the uterus, most often in the pelvic peritoneum and ovaries. This disorder affects an estimated 10% of women in the reproductive age group and is basically an estrogen-dependent
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calcium channel An important example of a frame is the
2022-03-31

An important example of a frame is the lattice of open subsets of any topological space X. The correspondence is clearly functorial (by taking inverse images), and consequently one has a contravariant functor with the category of topological spaces and continuous maps as domain category. The fun
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br GC C and cGMP of mice and
2022-03-31

GC-C and cGMP: of mice and men As is usually the case for many genes, most of the studies that relate to GC-C have to date been carried out in mouse models, or in cell lines derived from human colorectal cancer tissue. What appeared to be a lacuna was any report of a human disorder that resulted
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