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As part of their ongoing effort in the
2022-03-31
As part of their ongoing effort in the field, Kalypsis recently disclosed that quinazolinones 5 [49], imidazo[1,2-a] [1,2]diazepin 6 [50] and quinolines 7 [51] all had activity as small molecule modulators of TGR5 (Figure 4). Intercept, however, disclosed different bile cas chemical derivatives as
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ATP as a transmitter can be released from injured cells
2022-03-31
ATP as a transmitter can be released from injured AUY-922 and sensory nerve endings (Sperlágh et al., 1995, Sperlágh et al., 1997, Sperlágh et al., 1998, Burnstock, 2013, Burnstock, 2014). ATP can activate the P2X3 receptor in the DRG neurons (Gao et al., 2011a; Xu et al., 2012). In DRG neurons cul
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Oxidative stress results from the disequilibrium between
2022-03-31
Oxidative stress results from the disequilibrium between levels of prooxidant molecules produced and the ability of a biological system to detoxify and neutralize the reactive molecules [14]. OS is a chronic, self-perpetuating state of damage to cells and increased inflammation resulting from the co
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Cortisol is a natural glucocorticoid hormone produced by the
2022-03-31
Cortisol is a natural glucocorticoid hormone produced by the adrenal cortex. Its secretion is stimulated by the sympathetic nervous system, and its main function is to mobilize energy to protect the homeostasis of vital biochemical processes during physical and psychological stress [14]. Chronic lev
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Subsequently we decided to test whether the orexin pathway w
2022-03-30
Subsequently, we decided to test whether the orexin pathway was involved (Delhanty et al, 2012, Delhanty et al, 2013, Pei et al, 2014). Orexin neuronal systems are known to control limbic and neocortical structures (Bonnavion, de Lecea, 2010, Sakurai, 2007). Orexin receptors and possibly orexin synt
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The C terminal regions in both FGF and FGF
2022-03-30
The C-terminal regions in both FGF19 and FGF21 define their KLB interaction [15], [16], [23], [25]. However, less than 40% identity in comparative alignment of C-terminal sequences for these two proteins (Table 1) suggests that their interaction with KLB may require higher-order association with oth
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A common feature of ferroptosis is the iron
2022-03-30
A common feature of ferroptosis is the iron-dependent accumulation of lipid-ROS and the subsequent depletion of polyunsaturated fatty BIIE 0246 phospholipids (PUFA-PLs) [118]. The PUFA chains of membrane lipids are more susceptible to both enzymatic and non-enzymatic oxidation, which results in PUFA
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Potential roles for S P
2022-03-30
Potential roles for S1P in angiogenesis, cancer, and autoimmune diseases such as RA have been reported [73]. In RA synoviocytes, S1P has been shown to enhance expression of prostaglandin E2 (PGE2) and cyclooxygenase-2 (COX-2) in response to the pro-inflammatory cytokines, TNF-α and interleukin (IL)-
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Cell stiffness is determined by the cytoskeleton
2022-03-30
Cell stiffness is determined by the cytoskeleton, an intracellular polymeric network consisting of mmae mg filaments, microtubules, intermediate filaments, and crosslinking proteins [38]. Low cell stiffness has been correlated with reduced formation of well-defined F-actin filaments or bundles [39]
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More specific quantitative assays for DiXaIs are based on
2022-03-30
More specific quantitative assays for DiXaIs are based on the inhibition of chromogenic or clotting activity of Factor Xa. During drug development, Kubitza developed an endogenous Anti-Factor Xa assay [45], which is very sensitive to Rivaroxaban drug concentration. This assay was based on Factor Xa
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DZNep is a PRC inhibitor that inhibits S adenosylhomocystein
2022-03-30
DZNep is a PRC2 inhibitor that inhibits S-adenosylhomocysteine hydrolase, resulting in cellular accumulation of S-adenosylhomocysteine. S-adenosylhomocysteine is a competitive inhibitor of methyl donor for methyltransferases [38]. DZNep targets EZH2 by reduction in the level of the enzyme H3K27me3 a
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In human cancers it has
2022-03-30
In human cancers, it has been identified that FOXC2-AS1 functions as an oncogenic RNA. For instance, in osteosarcoma, FOXC2-AS1 regulates the expression of FOXC2 at the transcription and post-transcription levels to promote doxorubicin resistance by facilitating ABCB1 expression (C.L. Zhang et al.,
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br Methods The study was a cross sectional ecological analys
2022-03-30
Methods The study was a cross-sectional, ecological analysis of country-reported HIV expenditures. We obtained the most recent available and validated data on annual country-reported HIV expenditures in SSA countries between 2012 and 2017 from the UNAIDS (http://aidsinfo.unaids.org/). Many countr
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Figure shows the network of the persons with diagnosed HIV
2022-03-30
Figure 2 shows the network of the 47 persons with diagnosed HIV and their 192 contacts. Of the contacts, 149 (78%) were first-generation contacts and 43 (22%) were second-generation contacts. Color and shape combinations used for network nodes (i.e., persons) allow one to simultaneously discern past
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The H R antagonist JNJ developed by Johnson
2022-03-30
The H3R antagonist JNJ-17216498, developed by Johnson & Johnson, has entered clinical trial studies, but no information regarding its structure has been publicized to date. A phase II study of JNJ-17216498 monotherapy has been completed for patients with narcolepsy, but the results are not publicall
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