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DGK is not the only DGK
2021-01-13

DGKε is not the only DGK isoform that has been associated with p53. It has been shown that DGKζ binds to p53 and modulates its activity in both the cytoplasm and the nucleus [39]. In the cytosol DGKζ promotes the degradation of p53 through the ubiquitin-proteosome system [39], also a likely mechanis
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We also discovered important clues to domain
2021-01-13

We also discovered important clues to domain cucurbitacin of DGKs and how to exploit these regions for development of DGKα-selective inhibitors. The identification of a probe-modified site at the C1 domain provided the first evidence of a ligand binding site remote from the ATP binding region of DG
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Cryptosporidium is a protist causing serious diarrhea in
2021-01-13

Cryptosporidium is a protist causing serious diarrhea in humans and other animals (Bouzid et al. 2013). In its mitosomes, the most reduced forms of mitochondria, it is assumed that the membrane potential is generated by a simple respiratory chain consisting of transhydrogenase, type II NADH dehydrog
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Materials and methods Cell culture and receptor gene transfe
2021-01-13

Materials and methods Cell culture and receptor gene transfection. PC12 tcs products were purchased from the Institute of Cell Biology, Chinese Academy of Sciences, Shanghai, China. The cDNA for mouse CysLT1 or CysLT2 receptor (mCysLT1 and mCysLT2, subcloned into pcDNA3.0) was kindly gifted by Pro
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As previously reported azole class antifungal drugs inhibit
2021-01-13

As previously reported, azole class antifungal drugs inhibit fungal CYP450 14α-demethylase, as this interrupts the conversion of lanosterol to ergosterol, a component of the fungal cell membrane (Hof, 2006). Furthermore, correlation between fluconazole dose, the extent of hepatic hypertrophy, the le
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Recent studies investigating the effects of
2021-01-13

Recent studies investigating the effects of mesenchymal stem cell (MSC) therapy in rodent models including chronic renal failure and glomerulonephritis have demonstrated that MSC therapy can result in beneficial effects [57], [58]. In cats, autologous intra-renal injections of either adipose tissue-
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Models and theories The CPA
2021-01-13

Models and theories The CPA equation of state is composed predominantly of two parts: physical item and the association item based on the thermodynamic perturbation theory [21], [22], [26], [27]. The physical item is used to represent intermolecular physical interaction, usually representing the SR
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Two nutrient sensing pathways the
2021-01-13

Two nutrient-sensing pathways, the cAMP-protein kinase A (PKA) pathway and the target of rapamycin complex 1 (TORC1) pathway, are implicated in Msn2/4 regulation. Under non-stress conditions, Msn2 localizes in the cytoplasm and is inactivated by both PKA-dependent phosphorylation of the nuclear loca
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Next to organophosphates carbamates and metals
2021-01-13

Next to organophosphates, carbamates and metals, cholinesterase activity can also be affected by other pesticides, such as newer generation neonicotinoid insecticides (NN). NNs do not inhibit AChE activity via the organophosphate-sensitive binding site of the enzyme, but rather, by acting as a struc
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br Conclusions and future perspectives It
2021-01-13

Conclusions and future perspectives It is now evident that selective ETA or nonselective endothelin receptor antagonism provides therapeutic potentials against a variety of cardiovascular diseases such as hypertension, PAH, and diabetic microvascular dysfunction (Fig. 1). However, PAH is currentl
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WZ3146 synthesis br Conclusions ERK and its
2021-01-13

Conclusions ERK 1/2 and its phosphorylation plays an essential role in the hippocampus and can be triggered by both ROS accumulation and excessive Ca2+. DBP exposure can also affect the production of ROS and Ca2+ in the hippocampus. The question therefore arises as to whether the cell injury or a
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br Target enzyme attributes and substrate
2021-01-12

Target enzyme attributes and substrate peptide selection Protein kinases catalyze the phosphorylation of serine, threonine, and tyrosine residues in both proteins and peptides using ATP as the phosphoryl donor. The human kinome is comprised of 518 protein kinases and 40 lipid kinases. The vast ma
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br Results and discussion br Conclusion We have
2021-01-12

Results and discussion Conclusion We have constructed a series of potent and greatly selective DPP-4 inhibitors with pyrazolo[1,5-a]pyrimidin-7(4H)-one core surrogates. The modification of the core led us to b2 which has IC50 of 80 nM and > 1000 fold selectivity over DPP-8 and DPP-9. We utiliz
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One of the critical functions of
2021-01-12

One of the critical functions of the product of the AR gene is to activate the expression of target genes. This transactivation activity resides in the N-terminal domain of the protein encoded in exon 1, which contains polymorphic repeats. These trinucleotide repeats, (CAG) and (GGC), encode polyglu
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There are numerous theories of schizophrenia etiopathology
2021-01-12

There are numerous theories of schizophrenia etiopathology and genetics is often taken into consideration [25]. The dopamine D2 receptor is important since it is blocked by typical antipsychotic drugs with high affinity which is correlated with the ability to control psychotic symptoms in schizophre
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