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Sequences of hexokinases were initially
2022-01-29

Sequences of hexokinases were initially deduced and predicted based on cDNA clones (Andreone et al., 1989, Schwab and Wilson, 1989, Schwab and Wilson, 1991, Griffin et al., 1991, Thelen and Wilson, 1991). Analysis of genome sequence data identified, in NCT-502 to the 4 expected known hexokinase enz
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Human Glucocorticoid Receptor hGR was first cloned in Hollen
2022-01-29

Human Glucocorticoid Receptor (hGR) was first cloned in 1985 (Hollenburg et al., 1985). It is a modular protein comprised of an N-terminal trans-activating domain (NTD), a C-terminal ligand-binding domain (LBD) and a central DNA- binding domain (DBD). The DBD is highly conserved and has two zinc fin
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A group of small molecule with a more promising
2022-01-29

A group of small molecule with a more promising therapeutic mechanism are known as γ-secretase modulators (GSMs), which modulate the cleavage activity of γ-secretase (and likely a host of other substrates) and specifically reduce the levels of the fibrillogenic Aβ42 peptide without altering the ε-si
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Seizures in turn selectively modulate
2022-01-29

Seizures, in turn, selectively modulate the brucine receptor of GalR in the hippocampus. Thus, pilocarpine-induced SE led to a 30% downregulation of GalR2 without affecting GalR1 (personal communication with T. Bartfai, Scripps Research Institute). Therefore, despite the fact that GalR2 could have b
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Prior models suggest that the
2022-01-28

Prior models suggest that the terminal ends of the endocrine FGFs individually determine FGFR and KLB recognition, with little or no cross-talk. Our results confirm that short C-terminal sequences are necessary and sufficient to bind KLB and, supportive of a common mechanism, the underlying structur
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We have expanded these studies by doing EEG recording
2022-01-28

We have expanded these studies by doing EEG recording in the ET-1 model. Using this technique, we demonstrated that activation of either the ETA A-803467 or the ETB receptor induces electrical seizures. ET-1 induced electrical seizures occurred in the presence of either the ETA receptor antagonist o
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The present study was therefore conducted with three
2022-01-28

The present study was therefore conducted with three aims; (1) we tested the effect of IRL-1620, a selective ETB receptor agonist, on the analgesic tolerance to morphine and oxycodone in mice; (2) we determined the expression of ETA receptors and ETB receptors in the Pirfenidone of morphine and oxyc
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Wolf et al then proceed to interrogate the mechanism by
2022-01-28

Wolf et al. (2016) then proceed to interrogate the mechanism by which NAG activates the NLRP3 inflammasome. When examining potential triggers previously implicated in NLRP3 activation, they found that both PGN and NAG trigger appearance of mitochondrial DNA (mtDNA) in the cytosol, which led them to
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Epidermal Growth Factor (EGF), human recombinant mg G protei
2022-01-28

G protein-coupled receptor kinases (GRKs) are another group of kinases whose limited substrate repertoire is associated with an extensive binding interface. GRKs phosphorylate activated G protein-coupled receptors (GPCRs) at multiple sites, promoting binding of arrestin proteins to mediate receptor
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Suz is required for methyltransferase activity silencing fun
2022-01-28

Suz12 is required for methyltransferase activity, silencing function, and PRC2 protein stabilization in somatic and human ESCs (Cao and Zhang, 2004, Pasini et al., 2004, Collinson et al., 2016). Our experiments indicate that, in addition to associating with the H3K27 demethylases KDM6A (UTX) (Wang e
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Interestingly the rabbit cornea exhibited a more than
2022-01-28

Interestingly, the rabbit cornea exhibited a more than two-fold higher level of total GST activity compared with that of the porcine cornea, whereas their levels of GSTO1‐1 and GSTP1‐1 activity were similar (Fig. 4). Because members of the GST Alpha, Mu, Pi and Omega XAP044 primarily utilize CDNB as
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The urinary levels of OHP
2022-01-28

The urinary levels of 1-OHP among the exposed workers were higher than those reported for a Brazilian group of charcoal workers (0.07 μmol mol creatinine) exposed to wood smoke (Kato et al., 2004), and for nonsmoking bus drivers (0.19 μmol mol creatinine) and nonsmoking mail carriers (0.11 μmol mol
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As disclosed in our preceding paper medicinal chemistry SAR
2022-01-28

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, RepSox synthesis l
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The activation of the ERK pathway participates
2022-01-28

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 AUY922 sale can reduce the mechanical hypersensitivity and the thermal hypersensitiv
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Petrat et al could show
2022-01-28

Petrat et al. could show, that even a low dosage of 10-mg/kg glycine (133 μmol/kg) has a beneficial effect on the small intestine after I/R. In regard to glycine, β-alanine has a clearly higher EC50 to the GlyR and activates the receptor with an efficiency of only 34.6%.16, 17 Therefore, it can be c
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