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Current studies have identified five orphan
2022-05-27

Current studies have identified five orphan G protein-coupled receptors (GPCRs) that can be activated by free fatty acids (FFAs), GPR40, GPR41, GPR43, GPR84, and GPR120. Short-chain fatty acids (FAs) are specific agonists of GPR41 and GPR43 [21] and middle-chain FAs agonize GPR84 [22]. Long-chain FAs
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Introduction High mobility group box
2022-05-27

Introduction High mobility group box 1 (HMGB1) is a nuclear protein that plays a fundamental role in the regulation of DNA-associated events such as DNA repair, transcription, and replication. HMGB1 can be translocated to the cytosol, plasma membrane, and extracellular space in response to various
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Besides its carcinogenic role WTAP was also discovered
2022-05-27

Besides its carcinogenic role, WTAP was also discovered to participate in several physical processes in normal cells. As previously reported, WTAP was involved in cell proliferation, survival, apoptosis [7,29,30], eye development [8] and embryonic development [7] owing to its complex function in tra
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Sperm capacitation was negatively r p related with CR while
2022-05-27

Sperm capacitation was negatively (r = −0.68; p ive but not significant (r = 0.22). No significant relationship was observed between the expression levels of either CB1 receptor or FAAH and any of the sperm quality parameters studied. The scatter plot distribution of spermatozoa expression of CB1 an
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Regulation of gene expression in mammalian cells is governed
2022-05-27

Regulation of gene expression in mammalian cells is governed by the epigenetic machinery, which includes several distinctive yet entangled branches. DNA and histone modifying enzymes, non-coding regulatory RNAs, and ATPase-dependent chromatin remodeling proteins all contribute to the dynamic alterat
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In summary P P macrocyclization proved to
2022-05-27

In summary, P2-P4 macrocyclization proved to be an effective strategy to drive activity in this series of HCV NS3 protease inhibitors while microsomal stability was enhanced by the introduction of steric bulk along the tether. This modification augmented the previously-described tactic of improving
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Introduction Although G protein coupled receptor GPR was
2022-05-27

Introduction Although G-protein-coupled receptor 55 (GPR55) was considered a cannabinoid receptor, it differs phylogenetically from cannabinoid type 1 (CB1) and type 2 (CB2) receptors as it lacks the classic cannabinoid-binding pocket (Baker et al., 2006). GPR55 is sensitive to an array of cannabin
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Because of its excellent GPR potency good hERG selectivity
2022-05-26

Because of its excellent GPR119 potency, good hERG selectivity and favorable rat t, BH3I-1 was scaled-up and further profiled. The synthetic protocols described in , were both suitable for a multi-gram scale synthesis of compound . An off-target screen was performed against an extensive panel of
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br Author contributions br Acknowledgements The
2022-05-26

Author contributions Acknowledgements The work was financially supported by a grant from the Investigator-Initiated Studies Program (Ref. #38124) from Merck Sharp & Dohme, and, in part, from Research Grants Council of the Hong Kong Special Administrative Region, China (Ref. No.: 14110314), awa
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Another group of secreted proteins that determine the virule
2022-05-26

Another group of secreted proteins that determine the virulence of V. dahliae are effectors and microbe associated molecular patterns (MAMP) that regulate plant immunity [10]. So far, there is only one Ramiprilat gene Ave1 cloned in V. dahliae, yet it does not exist in race 2 strains such as V592 a
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br Regulation of Glu transporters
2022-05-26

Regulation of Glu transporters The pivotal role of Glu transporters in the fine tuning and turnover of this excitatory amino all-trans Retinal calls for a detailed characterization of its regulation. Several general mechanisms that modify Glu uptake activity have been described. These include tra
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A oligomers increased ubiquitination of GLT in astrocytes
2022-05-26

Aβ1-42 oligomers increased ubiquitination of GLT-1 in astrocytes. Previous studies found that astrocytic GLT-1 is internalized from the cell surface by ubiquitination of lysines located in the cytoplasmic C-terminus of the transporter (Gonzalez-Gonzalez et al., 2008, Martinez-Villarreal et al., 2012
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Rare mutations can impair the molecular function of GR
2022-05-26

Rare mutations can impair the molecular function of GR and alter tissue sensitivity to GCs in humans, resulting in primary generalized GC resistance (PGGR) and hypersensitivity (PGGH) [14]. Familial and sporadic PGGR, or Chrousos Syndrome, is characterized by general and partial insensitivity of tis
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br Results br Discussion Our cardiomyocyte specific GR knock
2022-05-26

Results Discussion Our cardiomyocyte-specific GR knockout mice did not show spontaneous cardiac hypertrophy unless pressure overload was given to the heart. This finding is somewhat different from previous work of a cardiomyocyte-specific GR nisoldipine mg mouse model using GR-floxed mice with
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While ghrelin s role in addictive
2022-05-26

While ghrelin's role in addictive behaviors has been most extensively explored with alcohol, ghrelin has also been implicated in biobehavioral substrates of other drugs of abuse. For example, preclinical experiments suggest that GHS-R1a blockade may improve nicotine [155,156], opioids [[157], [158],
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