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In addition to the role of
2022-02-17

In addition to the role of TGR5, the FXR-FGF15/19 axis has been implicated in other aspects of glucose metabolism and metabolic disorders. In humans, both obesity and type 2 diabetes mellitus (T2DM) are associated with lower plasma FGF19 levels [67,68]. A derivative of the naturally occurring FXR ag
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SKI-606 In summary we discovered azaindole substituted
2022-02-17

In summary, we discovered 7-azaindole substituted -hydroxypyridone as a potent zinc-binding GLO1 inhibitor (IC=11nM) through lead generation from HTS and structure-based inhibitor design. The X-ray cocrystal structure and the comparison of binding energies with the indole counterpart revealed that b
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br Introduction Verticillium dahliae Kleb is a
2022-02-17

Introduction Verticillium dahliae (Kleb.) is a soil-borne fungal pathogen that is able to infect hundreds of plant species, and causes vascular wilt disease [1], [2]. In nature, the infection of V. dahliae initiates from the germination of resting structures called microsclerotia [3]. The germina
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Here we performed TEM and AFM
2022-02-17

Here, we performed TEM and AFM imaging to study APE1–DNA interactions. The results showed that APE1 can dynamically polymerize on DNA in an apparently sequence-independent manner. We propose that this protein polymerization allows for scanning of the structural properties of DNA with short residence
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In this study we present the synthesis and
2022-02-17

In this study, we present the synthesis and structure–activity studies of a structurally distinct series possessing high potency and selectivity in HEK cell lines together with a potentially promising overall biopharmacological profile. Focusing on creating sufficient structural dissimilarity with g
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The SLC A mutations identified in both families
2022-02-17

The SLC45A1 mutations identified in both families appear to be hypomorphic given that they resulted in a reduction but not abolition of intracellular glucose transport by SLC45A1 in our in vitro assay. It is tempting to speculate that recessive mutations causing a more severe dysfunction of the tran
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NMDARs are glutamate gated ionotropic receptors that are inv
2022-02-17

NMDARs are glutamate-gated ionotropic receptors that are involved in excitatory neurotransmission and plasticity (Traynelis et al., 2010). There have been several reports showing that neurosteroids acting as negative modulators of NMDARs exert neuroprotective activity in both in vitro and in vivo mo
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br Competing interests br Authors contributions br Transpare
2022-02-17

Competing interests Authors contributions Transparency document Introduction Non-alcoholic fatty liver disease (NAFLD) is a spectrum of liver diseases ranging from simple steatosis to non-alcoholic steatohepatitis (NASH), which may further progress to liver cirrhosis and liver carcinoma
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cell metabolism Ning et al showed that LPC appeared to incre
2022-02-16

Ning et al. showed that LPC 18:1 appeared to increase insulin release through both GPR119-dependent and -independent mechanisms (Ning et al., 2008). In our study, we have shown that not only GPR119 but also GPR40 and GPR55 participate in LPC-stimulated insulin secretion (Fig. 4, Fig. 5) and target p
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Recently the classical view of the compartmentalization
2022-02-16

Recently, the classical view of the compartmentalization of the plant isoprenoid metabolism has been re-evaluated, following the demonstration of the partial peroxisomal localization of the mevalonic orthopoxvirus variola (MVA) pathway, generally regarded as cytosolic. Using GFP-tagging approaches,
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EZH affects cancer by regulating the expression
2022-02-16

EZH2 affects cancer by regulating the expression of target genes [22]. EZH2, together with SUZ12 and EED, forms the polycomb repressive complex 2 (PRC2), which catalyzes trimethylation of histone H3 lysine 27 (H3K27me3) [23,24]. PRC2 may recruit other polycomb complexes, DNA methyltransferases, and
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br Introduction Before planning population based genetic
2022-02-16

Introduction Before planning population-based genetic analysis or GWAS, it is important to annotate the sequence of the gene because these sequences represent the major sites such as promoter and transcription factor fxr agonist which may ultimately affect the expression of the gene. Similarly,
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tezacaftor mg Classical drugs target the viral enzymes rever
2022-02-16

Classical drugs target the viral tezacaftor mg reverse transcriptase (RT), protease and integrase (IN) [[4], [5], [6]]. Raltegravir (ISENTRESS/MK-0518) is the prototypical integrase strand transfer inhibitor (INSTI) leading to an extremely strong reduction in viral load [7] and it has been approved
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In conclusion the most salient observation from this study w
2022-02-16

In conclusion, the most salient observation from this study was that PAE reduced the expression of HDC protein expression in dentate gyrus, cerebral cortex, and cerebellum, but not in the caudate nucleus or ventral hypothalamus. The regional basis for this heightened sensitivity is not known, but it
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A recent novel and important
2022-02-16

A recent novel and important finding is that YAP connects cellular growth with anabolism; YAP suppresses the transcriptional induction of genes which importantly regulate gluconeogenesis in the liver; namely glucose-6-phosphatase catalytic subunit (G6PC) and phosphoenolpyruvate carboxykinase 1 (PCK1
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