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In normal tissues the expression patterns of GPR and
2022-06-02
In normal tissues, the expression patterns of GPR120 and GPR40 are not uniform. GPR120 is highly expressed in adipocytes, lung and intestinal tract, while GPR40 is shown to be expressed in pancreatic islet R406 and intestinal tract [7], [20]. It is considered that the distribution of the GPR120 and
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The activation of the ERK pathway participates in the transm
2022-06-02
The activation of the ERK pathway participates in the transmission of pain signaling by sensitizing primary afferents (Ji et al., 2009, Lai et al., 2011). Thus, the blockade of ERK activation in the primary sensory Disuflo Cy3 azide can reduce the mechanical hypersensitivity and the thermal hyperse
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In the present study we characterized the expression
2022-06-01
In the present study, we characterized the expression of glucose transporters in the developing and adult mouse lens and showed that GLUT1 is the primary transporter expressed in the lens epithelium. We found that mice with a homozygous deletion of Slc2a1 from the lens epithelium developed cataracts
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Pyrogallol is an organic gallic acid
2022-06-01
Pyrogallol is an organic gallic acid-converting compound that has three hydroxyl groups and belongs to the phenol family. Gallic MK-571 sodium salt hydrate is obtainable from the galls and barks of various trees, and a simple heating procedure can induce the decarboxylation of gallic acid to produc
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euk 134 mg Administration of a fructose rich diet to normal
2022-06-01
Administration of a fructose-rich diet to normal rats induces insulin resistance and impaired glucose tolerance or diabetes, depending on treatment duration [23]. We have shown that development of these abnormalities as well as fat deposit in liver, are effectively prevented by co-administration of
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LbGlcK and the HsHxKIV d
2022-06-01
LbGlcK and the HsHxKIV-d-glucose complex (PDB entry 3IDH) [17] were superimposed from individual subunits. The active site regions revealed the key clinical trial binding residues to be present for LbGlcK; also, the superposition showed that HsHxKIV had residues that were absent in LbGlcK, such as
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The effect of the selected
2022-06-01
The effect of the selected compounds on NF-kB transrepression was assessed using the well-studied HeLa B2 cell line that expresses endogenous GR and NF-kB family members and responds properly to glucocorticoids and pro-inflammatory cytokines (such as TNF). Our data revealed that the two hit compound
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Using data from a large population based cohort
2022-06-01
Using data from a large population-based cohort study in Finnish males and females, Suchankova et al. [97] looked at a subset of the aforementioned SNPs, namely one SNP on GHSR (rs2948694) and two SNPs on GHRL (rs4684677 and rs696217), in relation to alcohol use disorders identification test (AUDIT)
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By association a possible mechanism which may underlie the
2022-06-01
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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A way to identify what subunit interfaces contribute to
2022-06-01
A way to identify what subunit interfaces contribute to the pharmacology of agents is to utilise binary GABAARs as tool receptors to ascertain possible binding sites for particular ligands. These receptors can help identify subunits and subunit interfaces that contribute to receptor pharmacology. In
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Recently they reported an enyne chemotype
2022-06-01
Recently, they reported an enyne chemotype agonist (21, Fig. 13) with low lipophilicity, small polar surface area (PSA) and high potency (Clog P=3.8, tPSA=37 A2, EC50=20nM), further derived from TUG-424. The compound endowed fast oral IRAK-1-4 Inhibitor I (tmax=15min) and a decent pharmacokinetic pr
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The canonical tumor suppressor p
2022-06-01
The canonical tumor suppressor p53 has also been implicated as a transcriptional mediator of ferroptotic death (Jiang et al., 2015, Tarangelo et al., 2018, Wang et al., 2016, Xie et al., 2017). Specifically, p53 negatively regulates transcription of SLC7A11, the cystine-glutamate antiporter (Xc-) (J
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Sumoylation is involved in regulating protein protein
2022-06-01
Sumoylation is involved in regulating protein-protein interactions, subcellular protein localization, protein stability, and transcriptional factor activity (reviewed in [29]). The small ubiquitin-like modifier (SUMO) protein is covalently attached to a lysine residue in a Ψ-K-X-D/E consensus sequen
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When taken together data suggest
2022-06-01
When taken together, data suggest CRF plays a central role in linking the HPA axis, the eCB system, and the amygdala with anxiety (Hill et al., 2009, 2010a; Hillard et al., 2011). In elaborate studies in mice, Gray and colleagues (Gray et al., 2015) showed stress-associated increase in CRF concentra
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A new series of pyrimidones with
2022-06-01
A new series of pyrimidones (14) with C-7 and C-9 modifications were furnished consisting of a hydroxypyridinone and a thiazole ring and checked against raltegravir resistant HIV mutant strains to determine their in vitro anti-HIV IN potency. Compounds 14a–14a, 14b–14b and 14c–14c appeared with 6.4
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