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br Phosphorylation of P c Initial studies In
2024-09-19
Phosphorylation of P450c17 – Initial studies In addition to the molar ratio of POR to P450c17 and the allosteric action of cytochrome b5, a third factor that governs 17,20 lyase activity is the serine/threonine (Ser/Thr) phosphorylation of P450c17 itself. In a search for post-translational factor
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Skeletal pain associated with bone fracture is
2024-09-19
Skeletal pain associated with bone fracture is another area of critical need for a novel pain medication. NSAIDs and opiates are the two major therapies currently used to manage bone fracture pain. However, both of these therapies lead to significant unwanted side effects. Using the osteotomy model
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Fencilli et al reported derivatives of PHA which demonstrate
2024-09-19
Fencilli et al. reported derivatives of PHA-680626 (15) which demonstrated strong anti-proliferative activity against large group of leukaemia cell lines including IM-resistant BAF3 cells expressing mutants like T315I, M351T and E255K. Decrease in Histone H3 phosphorylation led to induction of endo-
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Preliminary results of studies sponsored by the
2024-09-19
Preliminary results of studies sponsored by the manufacturer of ETC-1002 have also shown positive results for monotherapy in statin-intolerant patients and for the combined use of the ACL inhibitor plus other cholesterol-reducing agents. In patients with a documented history of intolerance to statin
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We wanted to investigate the influence
2024-09-19
We wanted to investigate the influence of substituents on the pyrazole ring on the activity, but only a few substituted pyrazole-3-carboxylic acids/esters were commercially available in useful amounts at a reasonable price, for example, 4- and 5-nitro-pyrazole-3-carboxylic acid. The preparation of 4
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Previous studies have demonstrated ATR inhibition is effecti
2024-09-19
Previous studies have demonstrated ATR inhibition is effective for treating cancers combining with chemotherapies in lung adenocarcinoma, gastric cancer, HER2 positive breast cancer and chronic lymphocytic leukemia Bezafibrate to enhance chemotherapy sensitivity [[16], [17], [18],[20], [21], [22]].
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Then Autodock was employed for site directed docking
2024-09-19
Then, Autodock4.2 was employed for site directed docking on AD with the ligands of the cluster(s) having high binding affinities in VS II experiment (Morris et al., 2009). Docking protocols were followed as per our earlier report with 200 GA (genetic algorithm) run (Kalani et al., 2015). Likewise, l
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The structural analysis of the ASK activation
2024-09-19
The structural analysis of the ASK1 activation segment, which was not phosphorylated in the crystal structure, showed interactions mimicking those found in activated kinases. In addition, the isolated unphosphorylated ASK1-CD is active and able to autophosphorylate itself at three sites, Thr813, Thr
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RNA interference assays have shown that the
2024-09-18
RNA interference assays have shown that the inhibition of AMPK expression leads to increases in TNF-α, IL-6 and cyclooxygenase-2 (COX-2) levels after LPS stimulus, whereas the transfection of macrophages with a constitutively active form of AMPKα1 results in decreased LPS-induced TNF-α and IL-6 pro
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On the other hand there was no difference
2024-09-18
On the other hand, there was no difference in effectiveness performing ALK by FISH with regard to the sample site. When it was extracted from the primary tumor, we obtained 27.4% of not-evaluable specimens. Similar percentages were found for node (26.7%) and Epigallocatechin (31.3%) samples (p = 0.
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Ginsenosides are the major bioactive constituents
2024-09-18
Ginsenosides are the major bioactive constituents of the Panax ginseng root, which contain many types of ginsenosides including Rb1, Rg1, Rc, and Rg3. The ginsenoside Rb1 appears to be the most abundant of the bioactive ginsenosides [15]. Rb1 exhibits antiinflammatory, anticarcinogenic, and antioxid
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Though we have proved that VA
2024-09-18
Though, we have proved that VA could suppress hepatic gluconeogenesis, the mechanisms of VA on gluconeogenesis in vivo and in vitro remain unclear. AMP-activated protein kinase (AMPK), which is called an energy receptor enzyme, is widely expressed in liver and other tissues [23]. AMPK has become ano
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br AMPK structure and mechanism of action AMPK
2024-09-18
AMPK: structure and mechanism of action AMPK is a metabolic master switch that regulates downstream signals based on shifts in the surrounding energy reservoir [6]. It is expressed in a number of tissues, including the kidney, the liver, the skeletal muscle, the adipose tissue, and the hypothalam
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br Thymic expression of AChR Both linear
2024-09-18
Thymic expression of AChR Both linear unfolded epitopes of AChR subunits and the intact AChR are avidly expressed in thymus, particularly by thymic epithelial cells and myoid cells [17], [18], [19]. AChR-antibody positive MG patients often show thymic hyperplasia, characterized by lymphoid folli
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In summary we could identify and experimentally confirm two
2024-09-18
In summary, we could identify and experimentally confirm two novel SBEs within the 5-LO promoter and we were able to demonstrate that TGFβ and SMADs stimulate 5-LO promoter activity. Moreover, an elevated 5-LO expression has been linked to different forms of leukaemia. Therefore, the influence of ML
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