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Furthermore we also found that both activation of
2021-09-06

Furthermore, we also found that both activation of oncogenes and inactivation of tumor suppressor genes occurred in HBV oval cells, which showed opposite pattern in HBV hepatocytes. These genes might take part in neoplastic transformation of oval cells induced by HBV regarding the multipotent role o
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br Substrate Interactions Outside of
2021-09-06

Substrate Interactions Outside of the Catalytic Cleft As for other types of protein–protein interactions, kinase–substrate docking interactions can occur through large binding interfaces or through recognition of short linear sequence motifs. For kinases with a large number of substrates, the use
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In respect of clinical development Takeda
2021-09-03

In respect of clinical development Takeda has pioneered the field with the GPR40 agonist TAK-875 or fasiglifam (Figure 2A), which in phase-II studies decreased HbA1c as efficiently as sulfonylurea without signs of hypoglycemia [24]. This was obtained with surprisingly little effect on systemic insul
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The most classic case of acquired and
2021-09-03

The most classic case of acquired and relapsing epilepsy is temporal lobe epilepsy (TLE), which originates from the hippocampal formation, a structure situated in the mesial temporal lobe (Majores et al., 2007). Our experiment used the prominent pilocarpine-induced TLE model. Systemic administration
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Homeobox genes can promote oncogenesis through multiple mech
2021-09-03

Homeobox genes can promote oncogenesis through multiple mechanisms, including gene translocation, loss of heterozygosity, gene amplification, DNA methylation, Cyanine 3-dCTP remodeling, etc. For instance, translocation-mediated fusion of HOXA9 or HOXA13 on chromosome 7p15 with the nucleoporin gene
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Bikinin br Introduction Erythropoietin EPO is a glycoprotein
2021-09-03

Introduction Erythropoietin (EPO) is a glycoprotein hormone and the principal stimulator of erythropoiesis (Jelkmann, 2011). EPO promotes the proliferation and differentiation of red blood cells, which is important for oxygen transport. Low EPO levels in blood cause anemia; however, excessive lev
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With LML methyl oxo dihydropyridazin yl piperidin yl cyclobu
2021-09-03

With LML-134 (1-(1-methyl-6-oxo-1,6-dihydropyridazin-3-yl)piperidin-4-yl 4-cyclobutylpiperazine-1-carboxylate) containing drug-likeness properties (MW 375.47, five HBA, and MLogP 1.88), Novartis presents an additional drug-candidate to treat excessive sleepiness. A phase I clinical study was perform
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conotoxin mg To interrogate the molecular basis for the myoc
2021-09-03

To interrogate the molecular basis for the myocardial phenotype in mutant hearts, we performed quantitative real-time PCR (qRT-PCR) expression analysis of genes encoding critical endocardium-derived molecules including Nrg1 and Efnb2. Nrg1 expression was reduced in E13.5 mutant hearts as compared to
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Heme activates the master regulator of the anti oxidant stre
2021-09-03

Heme activates the master regulator of the anti-oxidant stress response, NRF2, which mediates the up-regulation of a battery of phase II detoxifying genes [106]. Remarkably, HO-1 induction by NRF2 is regulated via an interplay with the transcriptional repressor BACH1 at the Maf recognition omecamtiv
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On the basis of the structure
2021-09-03

On the basis of the structure of the Rab35/ACAP2 complex, the authors identified Thr76 in switch II of Rab35 as one key specificity determinant (Lin et al., 2019). The crystal structure shows that the hydroxyl group of Thr76 forms a FK228 with Asp756 in ACAP2, while the methyl group is a part of th
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We also examined possible involvement of the NF B signaling
2021-09-03

We also examined possible involvement of the NF-κB signaling pathway in GSK-3 inhibitor-induced suppression of PGE2 production, whereas GSK-3 inhibitors did not have a significant effect on IκB phosphorylation/degradation or NF-κB nuclear translocation. These results are consistent with a previous p
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The GPR receptor is also emerging
2021-09-02

The GPR55 receptor is also emerging as an important therapeutic target. GPR55−/− mice possess no overt phenotype, but were protected in models of inflammatory and neuropathic pain (Staton et al., 2008). Staton et al. (2008) reported that no GPR55 mRNA could be detected by RT-PCR in the animals. Also
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br Acknowledgments This work was financially supported by
2021-09-02

Acknowledgments This work was financially supported by the National Natural Science Foundation of China (No. 81703451) and the China Postdoctoral Science Foundation Grant (No. 2017M611269). Introduction According to the International League Against Epilepsy (ILAE), epilepsy is generally defin
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Boswellia papyrifera Del Hochst mostly grows in Sudanian
2021-09-02

Boswellia papyrifera (Del.) Hochst., mostly grows in Sudanian and Sahelian regions and their oleo-gum resin is used medically in treatment of rheumatism, menorrhagia, amenorrhoea, vaginal infections, ulcers, sores, polyuria, syphilis, bronchitis, scrofulous affections, inflammations, asthma, diarrhe
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To confirm the in vitro
2021-09-02

To confirm the in vitro findings, atorvastatin or pravastatin was given to C57BL6/J mice fed with high fat diet. Doses of atorvastatin were set to be 6 mg/kg and 12 mg/kg, which were within clinical therapeutic doses. The results revealed that treatment of atorvastatin but not pravastatin impaired g
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