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Reports described a range of synthetic GPR agonists with des
2022-08-18
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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In the previous paper we described
2022-08-18
In the previous paper, we described the design and synthesis of tricyclic thiazoles as FBPase inhibitors, and a series of SAR studies led to the identification of phosphate 3 and difluoromethylenephosphonate 4 exhibiting potent FBPase inhibitory activities (IC50=13, 47nM, respectively) (Fig. 2). In
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Cy3 hydrazide mg br Results and discussion Computer modellin
2022-08-18
Results and discussion Computer modelling studies suggested that the endocyclic oxygens in furocoumarin derivatives, such as Cy3 hydrazide mg 3a (Fig. 1), could also coordinate metal ions in the HIV-1 IN enzyme active site and inhibit the integration of viral DNA. The coumarin moiety is found in
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While phosphorylation site motifs are
2022-08-17
While vegfr2 site motifs are typically described in terms of residues that promote phosphorylation, negatively selected residues can also be an important component of substrate recognition. Such ‘forbidden’ resides can act as a filter to prevent phosphorylation of a site by the ‘wrong’ kinase, whic
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Cdc is also linked to the adherens junction via
2022-08-17
Cdc42 is also linked to the adherens junction via IQGAP1, however, it appears to have an opposite effect on junctional stability. When Cdc42 is inactive, IQGAP1 binds to β-catenin, displacing α-catenin, resulting in the loss of α-catenin-linked Zebularine filaments from the adherens junction and re
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The Berlin patient is a unique case and dependent on
2022-08-17
The Berlin patient is a unique case and dependent on the histocompatibility-matched CCR5Δ32/Δ32 homozygous donors. These donors occur at a little higher rate in the European Caucasian population, but they are very rare in Asians and Africans.15, 16, 17 The recently developed genome-editing technolog
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Resolving the molecular details of glyco proteome variation
2022-08-17
Resolving the molecular details of (glyco)proteome variation in different tissues and organs of the human body is critical for the understanding of human biology and disease [59]. Glycoproteomic analysis of disease-related tissues and cells has provided valuable information to identify promising tar
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In the present study co administration of TM
2022-08-17
In the present study, co-administration of TM (AT1 receptor blocker) and PD (AT2 receptor blocker) were made in ischemic mice to explore the significance of AT2 receptors in cerebral ischemia while blocking central AT1 receptors. Also to prove that AT2 receptors should be free after ischemic injury
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The transporter was successfully expressed in MSCs and HEK
2022-08-17
The transporter was successfully expressed in MSCs and HEK 293 cells. In both cell types, the expression of YFP-EAAT2 was confirmed by immunological staining and flow cytometry. The functionality of the transporter was determined by [3H]glutamate uptake assays, and the blood glutamate-grabbing activ
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There are also data showing potential beneficial effects
2022-08-17
There are also data showing potential beneficial effects of SGLT2i on non-alcoholic fatty liver disease (NAFLD) [[14], [15], [16], [17]], a hepatic manifestation of the metabolic syndrome that has been linked to type 2 diabetes mellitus (T2DM) development and increased cardiovascular (CV) as well as
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br Conflict of interest statement br
2022-08-17
Conflict of interest statement Acknowledgments Introduction Hedgehog (Hh) signaling controls key steps of development in most tissues and organs of invertebrates and vertebrates (Briscoe and Therond, 2013, Ingham et al., 2011, Wilson and Chuang, 2010). The unique cellular composition and mo
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The first report about the activity of
2022-08-17
The first report about the activity of ANAM in CACs it is due to Garcia et al. [19] which treated 16 cancer patients with oral ANAM 50mg once daily vs placebo for 3days followed by a washout WM-8014 of 5–7days and then cross-over to the other group for 3 more days. It was described a weight gain of
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br Materials and methods br Results
2022-08-16
Materials and methods Results Discussion Induction of neuronal cell death is the main neurotoxic mechanism of arsenite (Vahidnia et al., 2007). Previous studies have demonstrated that arsenite may trigger neuronal cell death via apoptosis, autophagy as well as necrosis (Yen et al., 2012; La
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br Materials and methods br Results br
2022-08-16
Materials and methods Results Discussion ERK5 signaling and its regulation has gained focus in recent years specially in the subject of cardiovascular biology, where this kinase plays a key role in angiogenesis and maintenance of blood vessel integrity [18,20,34,35]. The signaling pathways
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br Introduction Ovarian cancer patients have the highest mor
2022-08-16
Introduction Ovarian cancer patients have the highest mortality rate amongst patients with gynecologic cancers. The 10-year survival rate of ovarian cancer patients is Fluorescein TSA with BRCA1/2 mutation [2]. Several studies have indicated the role of dysregulation of histone methylation in ca
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