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To study the effects of GPR at
2022-03-31

To study the effects of GPR40 at the whole-animal level, GPR40 mice have been generated in two different genetic backgrounds [18], [19]. GPR40 mice from both backgrounds were apparently healthy with no overt signs of metabolic or other abnormalities. As expected, pancreatic islets taken from GPR40 m
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In conclusion we provided the first evidence
2022-03-31

In conclusion, we provided the first evidence of a modification and regulation of GCK by O-GlcNAc modification that until now was not explored. This discovery provides important clues in the prevention of hyperglycemia and development of novel therapeutic drugs to treat type 2 diabetes. Acknowled
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In the absence of HH ligand HH signaling is
2022-03-30

In the absence of HH ligand, HH signaling is actively maintained in a repressed state by the activity of the HH receptor Patched (PTCH). PTCH is a 12-transmembrane domain protein whose intracellular localization is concentrated at the 5-Methyl-CTP of the primary cilium, a single antenna-like structu
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br Acknowledgments This work was supported by the
2022-03-30

Acknowledgments This work was supported by the NIH (R01DK103884 to JMZ, R01DK100659 to JKE, and F32DK104659 and K01DK111644 to CMC), the Diana and Richard C. Strauss Professorship in Biomedical Research, the Mr. and Mrs. Bruce G. Brookshire Professorship in Medicine, the Kent and Jodi Foster Dist
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However ghrelin has a short half life of min because
2022-03-30

However, ghrelin has a short half-life of 15–20 min, because it is a natural peptide containing 28-amino acids, its clinical usefulness as a therapeutic agent may be limited (Mosińska et al., 2017; Vestergaard et al., 2007). Hence, many efforts have been made to elucidate the smallest segment of ghr
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GSIs were shown to effectively decrease A levels at
2022-03-30

GSIs were shown to effectively decrease Aβ levels at doses close to or higher than their IC50 values in cell culture models. Surprisingly, they also slightly increase Aβ levels at low doses, (significantly below the IC50) also known as “Aβ rise”, due to various mechanisms including inhibition of cel
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Photoincorporation of pTFDBzox AP occurred predominantly
2022-03-30

Photoincorporation of 21-pTFDBzox-AP occurred predominantly in the β3 subunit, very modestly in the α1 subunit and not at all in the γ2 subunit. These observations taken together with the sensitivity of 21-pTFDBzox-AP enhancement of GABA currents to the α1 M1 mutation Q242 W4 suggest that the 21-pTF
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Acknowledgments This work was supported by the Natural
2022-03-30

Acknowledgments This work was supported by the Natural Science Foundation of China (Nos. 21602254, 81603194), the Natural Science Foundation of Jiangsu province, China (BK20160767) and National Found for Fostering Talents of Basic Science (NFFTBS, J1310032). Introduction Glucocorticoids (GC) pl
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In addition to attenuating joint inflammation via
2022-03-30

In addition to attenuating joint Phenformin via T cells, Cpd43 could also decrease the severity of CIA/AIA by suppressing the function of innate leukocytes such as neutrophils and macrophages via FPRs, as has been shown in other acute inflammatory models including neutrophil/macrophage-mediated K/B
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plk inhibitor Besides its carcinogenic role WTAP was also di
2022-03-30

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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Remarkably most of these molecules are
2022-03-30

Remarkably, most of these molecules are also quite effective in interfering with the proliferation of the drug-resistant cancer cell lines, with IC50 values ranging from 0.59 to 2.93 μM against MCF-7/ADR cells, and from 0.160 to 1.17 μM against NSCLC-resistant H1975 cells. Among these molecules, com
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Trifluoromethyl ketones and fluorophosphates were the
2022-03-30

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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Introduction Human immunodeficiency virus HIV
2022-03-30

Introduction Human immunodeficiency 87 8 (HIV) persue to be a major global public health problem (Joint United Nations Programme on HIV/AIDS, 2018). Globally, 36.9 million (range, 31.1 million–43.9 million) people were living with HIV in 2017 (UNAIDS, 2018a). The burden of the epidemic varies cons
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In this review we focus on the structure
2022-03-30

In this review, we focus on the structure and function of the KDM4A protein, its role in cancer development, and the importance of this enzyme as a therapeutic target. For further review of the KDM4 family, see Shi et al., Whetstine et al., and Berry et al. , , . KDM4A protein structure and enzymol
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Histone acetylation is regulated by two groups of enzymes
2022-03-30

Histone acetylation is regulated by two groups of enzymes, histone acetyltransferases (HATs) and deacetylases (HDACs), with antagonizing functions (Wang et al., 2009b). Among members of HATs, p300 and CBP are homologous. Both are global transcriptional co-activators (Ogryzko et al., 1996), and play
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