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Inhibitors against the proteasome a component of the ubiquit
2021-11-05

Inhibitors against the proteasome, a component of the ubiquitin-proteasome pathway that degrades cellular proteins, provide a new strategy for targeting the 26S proteasome [25]. Proteasome inhibitors can exhibit potent anti-cancer effects against different tumor Ginkgolic Acid C15:1 synthesis and we
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Knock out mice of FXR showed enhancing cholesterol metabolis
2021-11-05

Knock-out mice of FXR showed enhancing cholesterol metabolism in vivo and reducing serum levels of total cholesterol. Additionally, the results of FXR-deficiency mice revealed potential effects on the improvement of obesity and diabetes.19, 20 As a natural FXR ligand, guggulsterone possesses antagon
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br FXR FGF in the
2021-11-05

FXR–FGF15/19 in the control of BAs synthesis The nuclear receptor FXR is the master regulator of BAs homeostasis, modulating their synthesis, interleukins and uptake [15]. FXR decreases BA de novo hepatic biosynthesis by reducing the expression of CYP7A1. At the canalicular membrane, newly-synth
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We have isolated various bioactive
2021-11-05

We have isolated various bioactive tgx acting by binding to the receptors of endogenous bioactive peptides such as opioid, bradykinin, neurotensin, and complements C3a and C5a etc. [24]. Rubimetide is the first example of an agonist peptide of the FPR2 of exogenous origin. Anxiolytic-like activity
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Trifluoromethyl ketones and fluorophosphates were the first
2021-11-05

Trifluoromethyl ketones and fluorophosphates were the first generation FAAH inhibitors identified. They showed good in vitro FAAH inhibition potency, but most of them exhibited poor selectivity for FAAH over other serine hydrolases (such as the triacylglycerol hydrolase and the membrane-associated h
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Recent studies have shown that
2021-11-05

Recent studies have shown that epigenetic modification is involved in neuropathic pain. For instance, peripheral noxious stimulation changes DNA methylation and histone modifications, which are related to pain hypersensitivity under chronic pain conditions [8]. Importantly, the epigenetic abnormalit
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Among RASs observed in patients from group
2021-11-04

Among RASs observed in patients from group 2, RAS T54S was identified in one patient infected with subtype 1b. This mutation had been shown to cause resistance to boceprevir and telaprevir, but not to simeprevir [36]. This was confirmed here since this patient achieved SVR after 12 weeks of treatmen
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This data is in accordance with our
2021-11-04

This data is in accordance with our recent results on the influence of cholesterol-depleting agent methyl-β-cyclodextrin on platelets (Borisova et al., 2011a). Dissipation of the proton electrochemical gradient of secretory granules by methyl-β-cyclodextrin did not evoke the release of endogenous gl
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Heart failure affects approximately million
2021-11-04

Heart failure affects approximately 6.5 million people over 20 years of age in the United States, with its prevalence estimated to increase about 45% by 2030 to almost 8 million . It is a chronic disease with complex etiology and heterogeneity in its pathological manifestations. Major risk factors f
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One major mode of bioelectric action is
2021-11-04

(2) One major mode of bioelectric action is that of an amplifier of subcellular symmetry-breaking mechanisms into tissue-wide order. An example is the patterning of the embryonic left (L)-right (R) axis reviewed in References [57, 58]; the following scheme describes the data obtained largely from th
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Cx mimetic peptides short synthetic peptides corresponding t
2021-11-04

Cx mimetic peptides, short synthetic peptides corresponding to intracellular amino BAY 41-8543 sequences of diverse Cx have better specificity compared to traditional GJ blockers and openers. In particular, it was reported that Cx mimetic peptides reversibly inhibited GJ channel function in a concen
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br Introduction As a fundamental metal dependent hydrolytic
2021-11-04

Introduction As a fundamental metal-dependent hydrolytic enzyme, inorganic pyrophosphatase (PPase) exhibits a specific catalytic ability, in which one molecule of inorganic pyrophosphate (PPi) can be transformed into two orthophosphate (Pi) ions [1,2]. The process of transformation is extremely e
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In the intestine ethanol exposure
2021-11-04

In the intestine, ethanol exposure can change the composition of gut microbiota and promotes the growth of intestinal gram-negative bacteria, which results in the accumulation of endotoxins such as, LPS. Ethanol also impacts the integrity of the gastrointestinal mucosal barrier, increasing intestina
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br Introduction GPR also known as free fatty acid receptor
2021-11-04

Introduction GPR40 (also known as free fatty perhexiline receptor 1), a member of the G-protein coupled receptor (GPCR) family, is expressed in pancreatic beta cells, intestine and the central nervous system (Bekinschtein et al., 2008; Itoh et al., 2003). It is activated by medium- and long-chai
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Ac-IETD-AFC synthesis Sometime ago we have described diamino
2021-11-04

Sometime ago we have described diamino-1,3,5-triazines as histamine H4R ligands,12, 13 and aryl derivatives of the 1,3,5-triazine, which attenuated inflammatory and nociceptive response in vivo in the rodent models of inflammation induced by Ac-IETD-AFC synthesis and zymosan. In this work we describ
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