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P Benzoxaborole substituted macrocyclic compounds based on I
2022-08-31

P4-Benzoxaborole-substituted macrocyclic compounds based on ITMN-191 scaffold were prepared using a general scheme as shown in . ITMN-191 was prepared by following a patent procedure. The P4 BOC group was removed by treatment with TFA in dichloromethane to give amine . The coupling of the amine to 6
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GPR shares a amino acid sequence identity in humans
2022-08-31

GPR81 shares a 52% amino Ac-DEVD-pNA sequence identity in humans to GPR109A [1], [2], [3]. In addition, GPR81 is localized more specifically to the adipose tissue [3]. In 2008, lactate was discovered to be the endogenous ligand for GPR81 [9], [10]. Plasma lactate levels reach concentrations capable
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br Introduction Inflammatory bowel diseases IBDs including C
2022-08-30

Introduction Inflammatory bowel diseases (IBDs) including Crohn's disease and ulcerative colitis (Baumgart and Sandborn, 2012; Beaugerie et al., 2006) are typically characterized by chronic, progressive, and relapsing inflammation of the intestine. Although the exact pathogenesis of IBD is unknow
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High energy adjusted free glutamate
2022-08-29

High energy-adjusted free glutamate intake among adults with high education level (above college) or high poverty income ratio (≥3.50) might be a consequence of the difference in intake of some foods such as vegetables and fruits, reflecting upon their socioeconomic status. Previous studies have sho
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Given the proposed importance of conformational dynamics
2022-08-29

Given the proposed importance of conformational dynamics to GCK's allosteric regulation, a number of biophysical methods have been utilized to probe the enzyme's dynamic structural landscape. Investigations into the mechanism of Radicicol binding, using changes in the enzyme's intrinsic fluorescence
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Since the late s synthetic GC e
2022-08-29

Since the late 1940s, synthetic GC (e.g. prednisone, prednisolone, dexamethasone) have been used extensively in the treatment of chronic inflammatory conditions such as rheumatoid arthritis and asthma, and for their immunosuppressant action in preventing organ rejection post transplantation. Cortico
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br Results br Discussion ER and
2022-08-29

Results Discussion ER and GR play opposite phenotypic roles in the normal endometrium, with ER promoting growth and GR inhibiting growth. Here, we show that in endometrial cancer, GR expression is associated with worse outcomes and higher-grade tumors, and this association is observed only in
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The GABA A receptors containing the subunit are crucial for
2022-08-29

The GABA-A receptors containing the δ subunit are crucial for the mediation of non-synaptic inhibition in the dentate gyrus; thus, the decreased expression of the δ subunit may suggest a decrease in the inhibitory tone and an increase in the neuronal excitability. Moreover, the GABA-A receptors cont
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NMDARs are glutamate gated ionotropic receptors that are inv
2022-08-29

NMDARs are glutamate-gated ionotropic receptors that are involved in excitatory neurotransmission and plasticity (Traynelis et al., 2010). There have been several reports showing that neurosteroids acting as negative modulators of NMDARs exert neuroprotective activity in both in vitro and in vivo mo
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br Competing interests br Authors contributions br Transpare
2022-08-29

Competing interests Authors contributions Transparency document Introduction Non-alcoholic fatty liver disease (NAFLD) is a spectrum of liver diseases ranging from simple steatosis to non-alcoholic steatohepatitis (NASH), which may further progress to liver cirrhosis and liver carcinoma
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Over of all melanomas have activating
2022-08-27

Over 50% of all melanomas have activating BRAF mutations [29] and inhibition of the Ras/Raf/MEK/ERK signaling pathways is one of the most promising treatments for malignant melanoma [30]. However, studies using BRAF inhibitors have identified various feedback mechanisms to activate BRAF pathway in m
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Over of all melanomas have activating
2022-08-27

Over 50% of all melanomas have activating BRAF mutations [29] and inhibition of the Ras/Raf/MEK/ERK signaling pathways is one of the most promising treatments for malignant melanoma [30]. However, studies using BRAF inhibitors have identified various feedback mechanisms to activate BRAF pathway in m
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br Results br Discussion In this study six
2022-08-26

Results Discussion In this study, six new T30695 variants were synthesized with the acyclic R or S glycerol linker instead of GNE-617 synthesis unit at 4, 8 or 12 T residue. Based on our previous studies on TBA-GQ, this type of modification should provoke local changes in GQ conformations in
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br Histamine H R The cloning of the H
2022-08-26

Histamine H4R The cloning of the H3R (Lovenberg et al., 1999) provided a template for the search of other Golgicide A receptors, and resulted in the most recent discovery of histamine H4R. This concluded with six independent groups that have reported the cloning of the H4R (Leurs et al., 2009, L
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As GSH cellular redox status is critical for
2022-08-26

As GSH cellular redox status is critical for various biological phenomena including apoptosis and inflammation [34], [35] we hypothesized that inflammation could modulate GSTP1-1 gene expression. Indeed, reactive oxygen species (ROS) are released at inflammation sites and can be eliminated from thio
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