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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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Not only does G a GLP complex appear
2021-12-21

Not only does G9a/GLP complex appear to play a role (albeit a seemingly conflicting one) in LTP maintenance, it may also be involved in long-term depression (LTD) (). At hippocampal CA1 synapses, LTD can be induced by pharmacological or synaptic stimulation of Group 1 metabotropic glutamate receptor
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Among the HER mutations reported in this
2021-12-21

Among the HER2 mutations reported in this study, the JMD mutant R678Q is the third most recurrent HER2 mutation. Basic residues (such as arginine) play an important role in anchoring TMD helices of single transmembrane proteins to the bilayer (Gleason et al., 2013, Hristova and Wimley, 2011, Kim et
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po1 The Y H D A variant
2021-12-21

The Y56H/D168A variant was resistant to all tested PIs, and the inhibitor binding mode determined the molecular mechanism of resistance. Prior to the development of grazoprevir, PIs typically contained large heterocyclic P2 moieties that strongly interacted with S2-subsite residues (Ali et al., 2013
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br Introduction Although effective hepatitis B virus HBV vac
2021-12-21

Introduction Although effective hepatitis B virus (HBV) vaccines are in use worldwide, HBV-related liver diseases are still a major public health concern, causing considerable morbidity and mortality. Approximately 257 million people are currently suffering from chronic hepatitis B and 887,000 de
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The synthesis of is shown in The Boc diaminopropanoic acid
2021-12-21

The synthesis of is shown in . The ---Boc--diaminopropanoic acid--butyl ester () fragment was synthesized in four steps from Boc--asparagine (). The key step in this synthesis was a Hofmann rearrangement of the terminal carboxamide, which was performed according to the elegant protocol of Zhang tha
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br Materials and methods E coli strains Strains of E
2021-12-21

Materials and methods E. coli strains. Strains of E. coli with mutations in the lacZ gene for β-galactosidase [5] and a derivative with a knock-out mutation of the chromosomal gene for FPG produced with P1vir [6] were obtained from H. Schellhorn (McMaster Univ., Hamilton, Ontario, Canada). Growth
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Pertussis Toxin The genes for the receptors for peptides sim
2021-12-21

The genes for the receptors for peptides similar to glucagon are dispersed on three human chromosomes, with two on chromosome 17 (GCGR and GLP2R) and one each on chromosomes 6 (GLP1R) and 19 (GIPR) (see Table S1). The exon–intron gene structures of these genes are similar, as are the genes for other
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