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In conclusion we have designed and characterized a
2021-10-27

In conclusion, we have designed and characterized a novel series of EAAT-blockers, exemplified by (-[4-(2-bromo-4,5-difluorophenoxy)phenyl]--asparagine)—a potent, selective, competitive non-substrate inhibitor of EAAT-2. As one of the most potent and selective EAAT-2 inhibitors identified to date,
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A-740003 synthesis The findings in mice were echoed in the h
2021-10-27

The findings in mice were echoed in the human studies, in which the effects of higher doses of LY3298178 caused greater weight loss than the selective GLP-1RA dulaglutide. In patients with T2DM, LY3298176 demonstrated meaningful weight loss after only four weeks of treatment. This was consistent wit
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br Presenilins and apoptosis Apoptosis
2021-10-27

Presenilins and apoptosis Apoptosis, also known as programmed cell death, has a critically important role in tissue homeostasis, development, normal ageing and the pathogenesis of several diseases, including cancer and neurological disorders. The presenilins were first linked to apoptosis when ce
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Nano biocatalyst prepared by assembling an enzyme on
2021-10-27

Nano-biocatalyst, prepared by assembling an enzyme on nanomaterial (NM) carriers is an emerging innovation in the field of nanobiotechnology. Some of the advantages of using NM as supports in VU 0155069 to conventional porous supports are effective enzyme loading due to large surface area with redu
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G quadruplex DNA structures may exist in either
2021-10-27

G-quadruplex DNA structures may exist in either positive or negative strand of a promoter to regulate gene expression. The positive strand of the HOXC10 promoter is overall C-rich in the 1000 bp upstream of the TSS (36.6% of C versus 24.1% of G) and contains many C-runs; thus, G-quadruplex structure
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pgc-1α inhibitor We have isolated various bioactive peptides
2021-10-27

We have isolated various bioactive pgc-1α inhibitor acting by binding to the receptors of endogenous bioactive peptides such as opioid, bradykinin, neurotensin, and complements C3a and C5a etc. [24]. Rubimetide is the first example of an agonist peptide of the FPR2 of exogenous origin. Anxiolytic-l
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br Methods br Results It is
2021-10-27

Methods Results It is well known that during the onset of vasoconstriction there is an increase in intracellular Ca2+ which activates myosin light-chain kinase followed by cycling of actin-myosin cross-bridges in VSMCs. Recently, it has been recognized that mineralocorticoid receptor antagonis
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PK profiles of were evaluated and found
2021-10-27

PK profiles of were evaluated and found to be improved compared to compound presumably due to interruption of β-oxidation. Low clearance and high plasma exposure were considered to be suitable profiles as an oral agent (). We first examined in vitro insulinotropic effects of compound from MIN6 cell
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It has been demonstrated that
2021-10-27

It has been demonstrated that RA regulates gene Disuflo Cy3 azide through an epigenetic mechanism during stem cell and cancer cell differentiation. In neuroblastoma cells, RA induced neural maturation through RET gene transcriptional activation by increasing H3K4me3 levels at the promoter region an
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Recent studies in our laboratory demonstrated that several h
2021-10-27

Recent studies in our laboratory demonstrated that several histamine H1 receptor antagonists induce apo A-I gene expression while histamine itself represses it [20]. In humans, there are three histamine receptor genes (H1, H2, and H3) that code for G-protein-coupled receptors (GPCR's) which bind his
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In autoimmune diseases lymphocytes penetrate into the
2021-10-26

In autoimmune diseases, lymphocytes penetrate into the inflammatory lesions of tissues, where it is prominently hypoxic or even anoxic, and utilize glycolysis for an energy supply after activation or under hypoxia (Sitkovsky and Lukashev, 2005; Palazon et al., 2014), which is modulated by the oxygen
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Human epidermal growth factor receptor HER neu also known
2021-10-26

Human epidermal growth factor receptor 2 (HER2/neu, also known as CerbB-2, or ERBB-2) is a proto-oncogene located on chromosome 17q21, which encodes a transmembrane protein with tyrosine kinase activity, and belongs to the HER receptor family (EGFR, named also HER1, HER3, and HER4) [6]. HER2 is invo
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Tideglusib Heavy alcohol consumption reported by three of fi
2021-10-26

Heavy alcohol consumption, reported by three of five referred patients with chronic HCV infection and cirrhosis, is a risk factor for cirrhosis in p.C282Y homozygotes [19], [47] and adults with chronic HCV infection [48]. Although none of the present referred patients were diagnosed to have porphyri
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It was revealed that various injured or infected organs of
2021-10-26

It was revealed that various injured or infected organs of Hippeastrum produce a mixture of an orange-colored chalcone and flavans which can be oxidized to red-colored dimer (Wilmowicz et al., 2014, Wink and Lehmann, 1996), preventing the penetration of injured tissues by Phoma narcissi, Botrytis ci
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To investigate the simultaneous effects of possible confound
2021-10-26

To investigate the simultaneous effects of possible confounding factors in the urinary 1-OHP excretion, multivariate regression analysis was performed (Table 3). Based on stepwise regression analysis, four independent variables (age, CYP1A1⁎4, GSTM1 and GSTP1 polymorphisms) entered into the final mo
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