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The optimization of the lead compound was
2019-11-19

The optimization of the lead compound () was initiated and the initial key SAR and the results of the structural modifications of lead compound are summarized in . Replacement of the carboxylic synthase moiety with other functional groups led to loss of functional activity against EP4 receptor. Alth
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Inappropriate heme metabolism has been linked to several neu
2019-11-19

Inappropriate heme metabolism has been linked to several neuropsychiatric disorders. In the hippocampi of Alzheimer\'s disease (AD) patients, for example, heme was found to binds intracellular amyloid β (Aβ), resulting in reduced heme bioavailability and its functional deficiency (Atamna and Frey, 2
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br Guidance of B cell localization by
2019-11-19

Guidance of B cell localization by EBI2 EBI2 expression and B cell disease Although chemoattractant receptors of the GPR family play essential roles in coordinating the migration of lymphocytes for efficient responses against pathogens, their dysregulation can result in the initiation or progr
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Studies have focused on a hydrophobic cage
2019-11-19

Studies have focused on a hydrophobic cage at the CULT domain, conserved from bacteria to mammals, as it binds to substrates and IMiDs (Chamberlain et al., 2014, Lupas et al., 2015). In addition, CRBN ligand-mediated protein degradation was highly conserved, which was confirmed in vertebrates by foc
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In another study Nutlin a mediated p
2019-11-19

In another study, Nutlin-3a-mediated p53 activation induced strong negative impact on NF-κB signaling in LPS-stimulated neutrophils and macrophages [34]. Nutlin-3a limited cellular immune response to LPS, partly by attenuating DNA binding activity of NF-κB and impairing transcription of its target c
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MicroRNA miRNA is a class
2019-11-19

MicroRNA (miRNA) is a class of highly conserved, non-coding small molecules containing 19–25 nucleotides. miRNAs are involved in the regulation of genes associated with cancer development and progression and therefore can act as oncogenes, by contributing to tumor formation,17, 18 or as tumor suppre
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Valproic acid VPA is a first line treatment for epilepsy
2019-11-19

Valproic GX-674 receptor (VPA) is a first-line treatment for epilepsy and bipolar disorder, although its therapeutic mechanism of action is not fully understood. Considerable evidence suggests that VPA can act through the GABAergic system, NMDA receptors, and/or sodium channels (for review, see Lös
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This study was aimed to assess a number of esterase
2019-11-18

This study was aimed to assess a number of esterase activities, namely erythrocyte AChE, plasma BuChE and BeChE, and serum PON1 towards a number of substrates, as well as the major genetic polymorphisms of BCHE and PON1in a cohort of greenhouse workers exposed to low toxicity pesticides under an int
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Arsenic could cause apoptosis in both benign and malignant c
2019-11-18

Arsenic could cause apoptosis in both benign and malignant cells (Akao et al., 2000, Gupta et al., 2003, Namgung and Xia, 2001). However, at present, little is known about the consequences of arsenic-treated urothelial cells in autophagy and expression of its related proteins. In addition, the alter
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It is well known that CysLTs exert potent contractile action
2019-11-18

It is well known that CysLTs exert potent contractile action on human bronchial smooth muscles through activation of CysLT1 receptors. Indeed, in vitro antigen-induced contraction of passively sensitized human bronchial tissue is markedly suppressed by a pre-treatment with CysLT1 receptor antagonist
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A French cohort study reported that micronized progesterone
2019-11-18

A French cohort study reported that micronized progesterone or didrogesterone used with oral or percutaneous estradiol showed no increase or decrease in the risk of breast cancer compared to synthetic progestins for at least 4 years of treatment [22] and even after 8 years [23]. Although the results
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The monomeric oligomeric states of
2019-11-18

The monomeric/oligomeric states of DDR2-V5-His and DDR2-Fc were confirmed by Western blotting under reducing and non-reducing conditions. As shown in Fig. 1b, DDR2-V5-His exhibited a relative molecular mass of ~60 kDa under both reducing and non-reducing conditions, consistent with this protein bein
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In this review we present
2019-11-18

In this review, we present compelling evidence in support of DHODH as an essential enzyme for the survival of cancer cells. DHODH, and its relationship to de novo pyrimidine metabolism, will be discussed along with factors that influence its regulation and expression. We will show evidence of DHODH\
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br Acknowledgement br Introduction Recent developments
2019-11-18

Acknowledgement Introduction Recent developments in cancer immunotherapies have demonstrated durable responses, suggesting that effective immunotherapy would hold promise to improve patient outcome (Gunturu et al., 2013; Hodi et al., 2003; Lutz et al., 2011; Ribas et al., 2009). However, attem
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The mechanism underlying the increased PON
2019-11-18

The mechanism underlying the increased PON1 levels found in greenhouse workers may be accounted for by an increased protein Walrycin B following pesticide interaction with different nuclear receptors as also occurs with other chemicals, such as polyphenols and statins [28]. A number of nuclear rece
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