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Utilization of fascinating properties such as
2021-12-22

Utilization of fascinating properties, such as localized surface plasmon resonance (LSPR), high fluorescent quantum yield, biocompatible nature, chromogenic and electrocatalytic functionality of several nanomaterials for histamine sensing is also quite evident where the nanomaterials have served as
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this content As disclosed in our preceding paper medicinal c
2021-12-22

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, this content lacks an
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Finally we investigated increasing basicity as a way
2021-12-22

Finally, we investigated increasing basicity as a way to improve solubility. We expected that conversion of the ether linkage of to an -methyl group could improve solubility. More than expected, ABH australia demonstrated significant improvement of values of solubility for the two media, especial
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The differential tissue and ligand dependent
2021-12-22

The differential tissue- and ligand-dependent signaling described here has important implications for the therapeutic potential of synthetic GPR109A agonists for the treatment of atherosclerosis. The failure of MK-0354, a biased, partial GPR109A agonist, to activate signaling pathways upstream of va
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br Materials and methods br Results br Discussion
2021-12-22

Materials and methods Results Discussion Heart hypertrophy is initially physiological to compensate for the loss of heart functions. However, sustained stresses lead to a pathological status, in which myocardium becomes stiffened by interstitial fibrosis and thereby diastolic dysfunction in
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HSOR belonging to the aldoketo reductase superfamily is
2021-12-22

3α-HSOR, belonging to the aldoketo reductase superfamily, is a rate-limiting enzyme for the synthesis of 3α-reduced steroids, such as allopregnanolone and tetrahydrodeoxycorticosterone. 3α-HSOR was extensively expressed in the spinal dorsal horn and was upregulated following peripheral nerve injury,
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br GR Is a Transcriptional Activator How GR activates
2021-12-22

GR Is a Transcriptional Activator How GR activates some genes while repressing others remains unsettled after decades of study. While significant controversy exists regarding GR-mediated repression, a consensus model for transcriptional activation has emerged: GR activates transcription through s
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To identify inhibitors of the Hh GLI
2021-12-22

To identify inhibitors of the Hh/GLI signaling pathway from natural resources, we have recently reported the successful construction of a cell-based screening assay system for the Hh/GLI signaling pathway (Fig. 1). This is an assay using a GLI-dependent luciferase reporter in human keratinocyte cell
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The HH Gli pathway has been demonstrated to
2021-12-22

The HH-Gli pathway has been demonstrated to play an extensive role in skeletal development. India Hedgehog, derived from hypertrophic chondrocytes, and Parathyroid Hormone-like related Protein (PTHrP), derived from peri-articular chondrocytes, form a negative feedback loop to inhibit chondrocyte hyp
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By association a possible mechanism
2021-12-22

By association, a possible mechanism which may underlie the progression of seizures is long-term potentiation (LTP). Indeed, LTP shares many common mechanisms with seizures activity both anatomically and physiologically, and has been implicated as a mechanism of acute epileptogenesis (Wasterlain et
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We hypothesize that HBO increases
2021-12-22

We hypothesize that HBO2 increases GABA activity at the GABAA receptor via a nitric oxide dependent mechanism. Blotting for the phosphorylated β3 subunit of the GABAA receptor should theoretically be increased when there is more GABA activity at the receptor (McDonald et al., 1998). We expected that
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GLP is released in response to ingestion of nutrients includ
2021-12-22

GLP-1 is released in response to ingestion of nutrients including carbohydrates, protein, and fat. Recent studies aimed at identifying the receptors involved in nutrient stimulated GLP-1 secretion have identified free fatty Ro 3306 receptor 4 (FFA4/GPR120) as a potential 7TM receptor involved in lon
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br Materials and methods br Results br Discussion The distri
2021-12-22

Materials and methods Results Discussion The distribution of FFA1 and FFA4 expressed in normal tissues is distinguishable. FFA1 is expressed in the restricted organ, such as pancreatic beta Neratinib [18]. In contrast, FFA4 is highly expressed in the lung, gastrointestinal tract, adipocyte
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Reports described a range of
2021-12-22

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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br Importance of iron and lipoxygenase
2021-12-22

Importance of iron and lipoxygenase in ferroptosis What remains to be somewhat controversial is the role of iron and lipoxygenases (LOX) in the death process, specifically in lipid peroxidation. So far, iron chelators have been repeatedly shown to halt ferroptosis (hence its name) induced by chem
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