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equol Similarly Somavarapu and Kepp constructed a PS homolog
2022-06-01

Similarly, Somavarapu and Kepp [29] constructed a PS1 homology model using 4HYG as a template, plus modeling the TM6-TM7 intracellular segment (amino acids 273 to 374). In this study, the authors considered for the first time the mature and immature (not autoproteolyzed) forms of PS1 component, sinc
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br Results br Discussion Immune mediated chronic
2022-06-01

Results Discussion Immune-mediated chronic inflammatory diseases (e.g. rheumatoid arthritis, psoriasis, multiple sclerosis, and inflammatory bowel disease) are characterized by a dysregulated migration of leukocytes from blood vessels into inflamed tissues. To date, several new targets and inh
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Type II diabetes is characterized by an inability to maintai
2022-06-01

Type II diabetes is characterized by an inability to maintain glucose homeostasis due to insulin desensitization and/or insufficient insulin secretion. GPR40, also known as free fatty pyruvate dehydrogenase kinase receptor 1 (FFAR1), is a member of the G-protein-coupled lipid-activated family of re
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In human cancers it has been identified that FOXC AS
2022-06-01

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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The ETB receptor has been
2022-06-01

The ETB receptor has been shown to decrease sodium transport in the renal medullary collecting duct and medullary thick ascending limb of Henle10, 11, 12, 13, 18. However, both inhibitory and stimulatory effects of endothelin have been reported in the proximal tubule16, 47, 48, 49. In the rat, endot
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The finding that a peptide consisting
2022-06-01

The finding that a peptide consisting of d-amino acids binds to LSD1-CoREST1 with equal affinity as the l-amino cudc ligand indicates that the assays detect a generally non-specific association between two highly charged molecules. Nonetheless, p53-CTD is an effective inhibitor of LSD1 and its bind
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In cancer cells HIF upregulates
2022-06-01

In cancer cells, HIF-1α upregulates HK-II expression by binding to the hypoxia-responsive element in the HK-II promoter region to adapt to hypoxic conditions [20]. In the present study, we observed that mangiferin transiently increased HIF-1α expression in endothelial cells, suggesting another possi
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br Introduction Although effective hepatitis B virus
2022-05-31

Introduction Although effective hepatitis B virus (HBV) vaccines are in use worldwide, HBV-related liver diseases are still a major public health concern, causing considerable morbidity and mortality. Approximately 257 million people are currently suffering from chronic hepatitis B and 887,000 de
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br FFA GPR was deorphanised as
2022-05-31

FFA4 GPR120 was deorphanised as the second receptor for long-chain fatty acids in 2005 [5]. Initial focus highlighted expression in the lower gut, the capacity of unsaturated fatty acids to promote release of the incretin glucagon-like peptide-1 (GLP-1) from the enteroendocrine cell line STC-1, a
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With the administration of OM fatty acids it
2022-05-31

With the administration of OM3 fatty acids, it has previously been shown that the activation of GPR120 is linked to the secretion and circulating levels of the adipokine adiponectin [123] promoting anti-inflammation (downregulation of NF-κB) and insulin sensitivity [124]. Interestingly, Nrf2 also de
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After the synthesis of methylsulfonyl or tetrazole surrogate
2022-05-31

After the synthesis of methylsulfonyl or tetrazole surrogate derivatives, compounds synthesized by introducing hydrogen, fluoro, and methyl groups into the head group of GPR119 agonists were synthesized. Compounds – were synthesized by reacting hydroxybenzaldehyde with fluorine, hydrogen, or a methy
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br Introduction Over the past two
2022-05-31

Introduction Over the past two decades, the prevalence of obesity and obesity-associated metabolic diseases, such as T2D, insulin resistance, atherosclerosis and stroke, have been dramatically increased globally [1], [2], and obesity has been suggested to be the leading cause of the reduced life
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Curcumin is the active ingredient extracted
2022-05-31

Curcumin is the active ingredient extracted from the natural medicine turmeric rhizome (Goel et al., 2008, Aggarwal and Harikumar, 2009). Studies have shown that curcumin has anti-tumor, anti-inflammatory, antioxidant and antimicrobial properties (Larsen et al., 2007, López-Lázaro, 2008). Although c
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No compounds in this series showed any appreciable activity
2022-05-31

No compounds in this series showed any appreciable activity at GlyT2 and can thus be considered GlyT1-selective. For the GlyT2 IC was >20μM. To determine CNS penetration of -(2-(azepan-1-yl)-2-phenylethyl)-benzenesulfonamides, select compounds were evaluated in a cassette CNS exposure screen in ma
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ICH induced striatal lesion produced a reduction
2022-05-31

ICH-induced striatal lesion produced a reduction of EAAT1 expression analogous to the decreased glutamate uptake at 6 h. The combined reduction of excitatory amino NPS-2143 hydrochloride transporters and of glutamate uptake activity might explain the well-known glutamate excitotoxicity following br
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