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To further investigate if GPR was the
2021-09-26

To further investigate if GPR40 was the functional target of these phenylpropiolic retinoic acid receptor analogs, GW-1100, a selective antagonist of GPR40-mediated Ca2+ elevations in HEK293 cells with an IC50 value equal to 1 μM, was used to inhibit agonist-induced intracellular calcium flux [15].
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It has been reported that the FDP synthase in
2021-09-26

It has been reported that the FDP synthase in Hevea latex has a major role to produce the starter substrate FPP for the prenyl chain elongation in natural rubber biosynthesis (Takaya et al., 2003). Accumulation of HbFDP mRNA transcripts in different tissue types including latex (natural rubber) prod
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br Materials and methods br Results br Discussion The COMPAS
2021-09-26

Materials and methods Results Discussion The COMPASS family of histone methyltransferases exhibits HMT activity towards histone 3 lysine 4 residue with KMT2F and KMT2G being the major H3K4 methylases (Shilatifard, 2006). They play an important role in the formation and progression of leukem
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We notice that previous reports of arsenic exposure
2021-09-26

We notice that previous reports of arsenic exposure are not completely consistent with each other, in terms of exposure-changed histone acetylations. In an early investigation, As exposure (7.5 μM) of HepG2 tyramide synthesis increased H3K9ac after 24 h, when analyzed by methods of immunofluorescenc
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Based on our results we propose three possible mechanisms of
2021-09-26

Based on our results, we propose three possible mechanisms of HER2 loss after trastuzumab-based therapy (Fig. 3). The first possibility is a result of the differential effects of treatments on clonal subsets. In breast cancer, such selective pressure has been suggested to preferentially eradicate HE
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In our substudy patients carrying the Ile Val
2021-09-26

In our substudy, patients carrying the Ile/Val or Val/Val genotypes had significantly worse DFS compared to patients carrying the Ile/Ile genotype, after adjustment for potential confounders. Two previous studies examining the association between HER2 Ile655Val polymorphism and trastuzumab response
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We also conducted analyses on the functional category of UP
2021-09-26

We also conducted analyses on the functional category of UP_Keywords and on KEGG pathways for further understanding. The UP_Keywords analysis (D) demonstrated that acetylation and phosphoprotein were highly enriched categories. KEGG pathways categories (E) of ribosome biogenesis in eukaryotes, DNA r
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As disclosed in our preceding paper
2021-09-24

As disclosed in our preceding paper, medicinal chemistry SAR optimization of an HTS hit led to the discovery of , a potent and selective GPR119 agonist. This scaffold differs significantly from the ‘classical’ GPR119 pharmacophore, exemplified by the examples and (). Notably, Sennoside C lacks an e
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Although we showed that RBL H Sc cells took
2021-09-24

Although we showed that RBL-2H3 Sc98 retinoic acid receptor took up histamine from the microenvironment, it was unclear which transporter mediated its passage across the plasma membrane. Other biogenic amines have selective transporters that belong to the neurotransmitter sodium symporter family, i
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In conclusion we demonstrated that the atypical high
2021-09-24

In conclusion, we demonstrated that the atypical high-basal activity of the mGlu3 notch signaling results mostly from its activation by low ambient glutamate concentrations. This is due to a unique interaction network located in the extracellular domain of the mGlu3 receptor. This network acts as “
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Shikonin represents naphtoquinonic compound isolated from
2021-09-24

Shikonin represents naphtoquinonic compound isolated from the Chinese plant Lithospermum erythrorhizon[20]. Shikonin treatment inhibits AKT and ERK signaling pathways and induces apoptosis through FOXO transcription factors and mitochondrial pathway [21], [22]. Recent results suggest inhibition of l
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A majority of investigations of the GCK PFK
2021-09-24

A majority of investigations of the GCK-PFK-2/FBPase-2 interaction have taken place within cells. Immunofluorescence studies in several fixed cell lines indicate that GCK colocalizes with PFK-2/FBPase-2 in the cytoplasm following overexpression [[68], [69], [70]]. Live cell imaging conducted on KX2-
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The ER EK polymorphism is located in the
2021-09-24

The ER22/23EK polymorphism is located in the transactivation domain of the GR gene. A single nucleotide polymorphisms (SNPs) has been identified in both of the two adjacent codons (22 and 23). These SNPs are fully linked and are associated with relative GC resistance[32], [44]. Although no associati
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We speculated modulation of redox balance in
2021-09-24

We speculated modulation of redox balance in brain, by activation of GIP receptor pathway. QA is known to mediate production of ROS, lipid peroxidation by its interactions with Fe2+ and formation of QA-Fe2+ complex (Braidy et al., 2010, Rios and Santamaria, 1991, Stipek et al., 1997). QA induces NOS
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EPZ5676 receptor Reports described a range of
2021-09-24

Reports described a range of synthetic GPR40 agonists with desirable safety and efficacy profiles, compared with existing antidiabetic therapies such as insulin and sulfonylureas [[20], [21], [22], [23], [24], [25], [26], [27], [28]]. Among them, several small molecules were tested in the clinical t
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