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Protein structures determined in high resolution by X
2022-08-04
Protein structures determined in high resolution by X-ray crystallography and NMR techniques provide wealth of structural information on intra-domain and inter-domain protein interactions of small sized proteins. In addition, cryo-EM often provides low resolution structures of multi-component protei
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PFK-015 Glutathione transferases GST have been discovered in
2022-08-04
Glutathione transferases (GST) have been discovered in many tissues including the cornea of humans and several other mammals (Awasthi et al., 1980, Bilgihan et al., 2003; Gondhowiardjo and van Haeringen, 1993; Saneto et al., 1982, Sastry et al., 1995, Singh et al., 1985, Watkins et al., 1991). To d
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By combining the results of the melting
2022-08-04
By combining the results of the melting curve analysis of exon 5 and exon 6, the allelic setup of our 250 subjects was determined; the four allelic variants are shown in Table 1. However, GSTP1-1 *A/*C and GSTP1-1 *B/*D could not be distinguished from one another because both genotypes are character
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br Positive regulation of gene expression by Nrf br Repressi
2022-08-04
Positive regulation of gene LDN-212854 by Nrf2 Repression of Nrf2 by Keap1 Because many xenobiotic inducers of NQO1 and GST enzyme activities contain a thiol-reactive electrophilic moiety (i.e. are soft electrophiles), Paul Talalay and colleagues predicted in 1988 that they would be recognize
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Apart from the different assays used biased
2022-08-04
Apart from the different assays used, biased agonism could also explain the inconsistent pharmacology of GPR55. Indeed, one study compared the effect of LPIs and Virodhamine in HEK293 endothelin receptor antagonist stably transfected with human GPR55. They found that the effect of both ligands on i
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The synthesis of nitropyrimidine analogs was
2022-08-04
The synthesis of 5-nitropyrimidine analogs – was outlined in . 4,6-Dichloro-5-nitropyrimidine, 4-methylsulfonylaniline and 2-fluoro-4-methylsulfonylaniline were prepared according to previously reported procedures., , Reaction of 4,6-dichloro-5-nitropyrimidine and substituted aniline in DMF yielded
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The top concern for the clinical use of
2022-08-04
The top concern for the clinical use of CRISPR-Cas9 technology is safety. Off-target alterations must be avoided to ensure genome integrity and proper cellular function. WGS found no off-target effects among the top 49 predicted off-target sites. WGS did find 4,658 indels and 1,891 SNVs in sgRNA1/2-
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br Regulation of gonadotropins by
2022-08-04
Regulation of gonadotropins by GnRH GnRH is released from the hypothalamus, and its release pattern is known to be pulsatile. That is, the pulse frequency and amplitude of GnRH release vary physiologically during reproductive cycles in females, and differentially stimulate the production and rele
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br Introduction Glucokinase GCK hexokinase IV
2022-08-03
Introduction Glucokinase (GCK, hexokinase IV) is a monomeric enzyme that catalyzes the ATP-dependent conversion of glucose to glucose 6-phosphate, the first and rate-limiting step of glycolysis in the liver and pancreas [1,2]. GCK was first discovered in the early 1960's, and shortly thereafter i
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Consistent with recent independent studies we confirm that t
2022-08-03
Consistent with recent independent studies, we confirm that the GCG-induced increase in oxygen consumption is only partially blunted in Fgf21−/− mice [32], implicating additional GCGR-dependent mechanisms contributing to the acute GCG-dependent enhancement of energy expenditure. Notably, glucagon ad
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Growing evidence supporting the anti inflammatory and tissue
2022-08-03
Growing evidence supporting the anti-inflammatory and tissue-protective effects of FPR antagonists led to the screening of commercial libraries for novel small-molecule FPR antagonists. As result of these screening efforts and/or structure–activity relationship (SAR)-directed design and synthesis, a
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Next we conducted subgroup analyses with stratification alon
2022-08-03
Next, we conducted subgroup analyses with stratification along interaction variables, namely the PPARG SNP and fasting NEFA. The study population was thus stratified into high and low NEFA (along the median NEFA, 561 μmol/L), and PPARG minor allele (Ala) carriers. This stratification resulted in 4 s
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Accordingly and in animal models a
2022-08-03
Accordingly and in animal models, a high-fat diet rich in CO (CO-HFD) impeded ventricular function and induced cardiac cell death and remodeling, at least, by down-regulating cell antioxidant defense systems and induction of oxidative stress [28], [29], [30], [31]. Interestingly, long chain fatty ac
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br Factor Xa an enzyme in the
2022-08-03
Factor Xa, an enzyme in the coagulation cascade, has recently been identified as having a role in inflammation, generating interest in factor Xa inhibitors as anti-inflammatory agents beyond their established use as anticoagulants [, , , ]. We report sustained clinical and electrophysiologic impro
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H O induced astrocyte ATP release through
2022-08-03
H2O2 induced astrocyte ATP release through lysosome exocytosis. The LDH assay and electric microscope results indicated that the increase of extracellular ATP concentration was not due to the cell rupture, but the alternations in cell activities. In addition, when lysosome exocytosis was blocked by
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