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In a recent study Neelaveni et
2021-10-15
In a recent study, Neelaveni et al. [47] revealed that new thiazolidinedione derivatives (Fig. 6 a and 6 b) produced dual PPARγ and FFAR1 agonistic activity at micromolar concentrations with insulin sensitizing effects and enhanced insulin secretion from the pancreas. These derivatives were reported
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EZH mutations or amplifications have been found
2021-10-15
EZH2 mutations or amplifications have been found in a broad spectrum of human cancers including B cell lymphoma, ovarian cancer, breast cancer, melanoma, bladder cancer, gastric cancer, and other cancers (Kim and Roberts, 2016). Given the evidence of EZH2 as a cancer driver, numerous efforts have be
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Development of few more dihydroxy pyrimidine and N
2021-10-15
Development of few more dihydroxy-pyrimidine and N-methylpyrimidone analogues as HIV-integrase inhibitors was attempted involving substitution of variety of five- and six-membered rings via the introduction of a simple methyl substituent in the α-position of the C-2 side chains in order to improve p
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Consideration must be given to both the tissues
2021-10-15
Consideration must be given to both the tissues themselves and to infiltrating immune cells. As highlighted by Maxwell and Eckardt [88], clinical trials of compounds targeting these pathways will require large numbers of participants and prolonged follow-up to identify rare and late complications or
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An isoflavone type secondary metabolite Glabrescione
2021-10-15
An isoflavone type secondary metabolite, Glabrescione B (GlaB), from Derris glabrescens (Benth.) J.F. Macbr. from the family Fabaceae, was found to possess the capacity to bind the Gli1 zinc finger domain and to further block DNA binding capacity [118]. Pyrvinium, an anthelmintic drug approved by th
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Conformational changes are observed in the LBDs after ligand
2021-10-15
Conformational changes are observed in the LBDs after ligand binding, including partial cleft closure for GluN2A and complete cleft closure for GluN1. For GluN2A, additional conformational rearrangements in the protein and ligand may be required before the ligand can be accommodated within lobe 2. F
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Serotonin hydroxytryptamine HT is a monoamine with dual func
2021-10-14
Serotonin (5-hydroxytryptamine, 5-HT) is a monoamine with dual functions in the developing and matured brain. 5-HT regulates development of the mecamylamine receptor as a neurotrophic factor and is involved in emotion and cognition as a neurotransmitter in adulthood (Gaspar et al., 2003; Daubert and
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To address this we developed approaches
2021-10-14
To address this, we developed approaches to image at high spatial and temporal resolution live WPB fusions as well as the release of VWF and other WPB cargo by spinning disk microscopy and combined laser ablation and total internal reflection fluorescence (TIRF) microscopy. Our live cell imaging rev
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Our results further indicate that low expression of p CBP
2021-10-14
Our results further indicate that low expression of p300/CBP in CRC is directly associated with poor clinical therapeutic outcome of 5-FU treatment, potentially providing a new set of biomarkers to predict chemo-sensitivity. Although the ability of low expression of p300/CBP to predict poor prognosi
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Migration chemotaxis and trafficking of leukocytes including
2021-10-14
Migration, chemotaxis and trafficking of leukocytes, including eosinophils from the peripheral blood into the site of inflammation requires their adhesion to endothelial psoralen receptor (Ley et al., 2007). Despite ongoing research, the histamine effect on eosinophils adhesion to endothelium cells
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HBV is an enveloped double stranded DNA virus
2021-10-14
HBV is an enveloped, double-stranded DNA virus, which is transcripted into four major transcripts [6]. Among them, the 3.5 kb pregenomic RNA (pgRNA) directs the translation of HBV polymerase, core protein and acts as template for reverse transcription. So viral transcription is a key step of virus
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Currently the computational chemical biology has been applie
2021-10-14
Currently, the computational chemical biology has been applied in hepatitis B antiviral drug discovery research [18]. Tan et al. explored oxime ethers as HBV inhibitors by docking and screening [19]. Allen et al. clarified the resistance of HBV to the nucleoside drug lamivudine [20]. The results sug
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Introduction Hepatocellular carcinoma HCC is the fifth most
2021-10-14
Introduction Hepatocellular carcinoma (HCC) is the fifth most lethal malignant tumor worldwide and is the second leading cause of cancer-related death [1]. For HCC patients, ras gtpase virus (HBV) infection is the important causative risk factor in Asia-Pacific regions [[2], [3], [4]]. In China, m
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br Materials and methods br Results
2021-10-14
Materials and methods Results Discussion In this study, we demonstrated that zaprinast (a cGMP-PDE inhibitor) induced the intracellular calcium mobilization in the MLN9708 coexpressing GPR35 and Gqi5, Gqo5, or Gα16. Induction of intracellular calcium mobilization by zaprinast in the GPR35-e
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br Introduction High dose niacin or
2021-10-14
Introduction High dose niacin, or nicotinic acid, has been used as an athero-protective drug for more than 50 years (Carlson, 2005, Offermanns, 2006). When taken in pharmacological doses (>1g/day), the nicotinic GSK503 form of niacin modulates plasma lipid profiles including decreasing circulatin
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