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Azaserine Although historically the two ROCK isoforms
2021-12-04

Although historically, the two ROCK isoforms have been viewed as redundant, recent observations show that the two isoforms of ROCK might have different functions (Newell-Litwa et al., 2015). Knockdown of ROCK1 was found to result in cell rounding and a decrease in cell size while cells with knockdow
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br Learning from our ancestors As mentioned earlier
2021-12-03

Learning from our ancestors As mentioned earlier, homologues of all γ-secretase components have been identified in plants and protozoans, some of which have emerged as model systems for the study of γ-secretase independent functions of the presenilins [27]. The moss P. patens was the first plant
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br Biologically active non peptide galanin
2021-12-03

Biologically active non-peptide galanin receptor ligands The first successful attempt in overcoming these weaknesses was undertaken by Saar et al. (2002). Screening of galanin sequence established that Trp-2, Asn-5, Tyr-9 were pharmacophores, responsible for biochemical action of the peptide. Bas
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Many neutral and acidophilic galactosidases have been
2021-12-03

Many neutral and acidophilic β-galactosidases have been purified from microorganisms [14], while only a few alkalophilic β-galactosidases have been reported [19]. An alkalophilic β-galactosidase, BGal_375, was obtained and researched for the characterization of its hydrolytic activity. BGal_375 show
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C prevents the glutamate and erastin induced
2021-12-03

C16 prevents the glutamate- and erastin-induced ROS accumulation but does not affect the decrease in GSH, indicating that prevention of ROS accumulation by C16 is not due to the restoration of GSH levels. Instead, C16 itself possessed superoxide anion scavenging activity in vitro at similar concentr
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br Rationale The present study
2021-12-03

Rationale The present study was motivated to get further insight into the molecular recognition processes of 2-alkyl(amino)ethyl-1,1-bisphosphonates taking compounds 12–14 as reference structures. We have recently demonstrated that TcFPPS inhibitors 12 and 13 bind to the allylic site of the enzym
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br Formation of secretory vesicles and trafficking
2021-12-03

Formation of secretory vesicles and trafficking toward plasma membrane Insulin and other components of the secretory granules are sorting and providing certain cues for Methylpiperidino pyrazole off the adjacent TGN membrane, forming immature secretory clathrin coated vesicles (Gehart and Ricci,
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Several layers of regulation for this canonical activation o
2021-12-03

Several layers of regulation for this canonical activation of the HH pathway exist. First, the protein kinase A (PKA), the casein kinase 1α (CK1α) and GSK3β can phosphorylate and mark for proteosomal degradation the GLI transcription factors. [36] Second, Suppressor of Fused (SUFU) binds to GLI and
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In an attempt to further optimize
2021-12-03

In an attempt to further optimize interactions in the lipophilic P4 pocket, we next prepared compounds – () which possessed the preferred stereochemistry at P4, but with R-groups of varying size and shape. In addition to providing important structural information for maximizing potency, these compo
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The mode of action of
2021-12-03

The mode of action of m-Tyr has not been fully recognized. The primary/basic mechanism of action of m-Tyr is thought to be associated with the incorporation of this NPAA into the structure of proteins resulting in formation of dysfunctional proteins [11], [12]. m-Tyr is incorporated into proteins in
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br Potential endogenous agonists of GPR The first endogenous
2021-12-02

Potential endogenous agonists of GPR35 The first endogenously produced chemical that was shown to be able to activate GPR35 was the tryptophan metabolite kynurenic luteolin [8]. When human GPR35 was expressed along with a mixture of promiscuous and chimeric G proteins 9, 10 (Box 1) in CHO cells,
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pi3k inhibitors br Materials and methods br Results br Discu
2021-12-02

Materials and methods Results Discussion In this study, the supF forward mutation assay showed that 5OHU induced mutations in human cells and that a C→T mutation was the predominant mutation among 5OHU-induced mutations. In addition, the DNA cleavage activity assay revealed that 5OHU was ex
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In response to oxidative stress in DM antioxidant
2021-12-02

In response to oxidative stress in DM, antioxidant defence systems are activated in β-cells. Glutathione (GSH) is one of the most abundant antioxidants and has been shown to be expressed at lower concentrations in patients with DM [12], [13]. Furthermore, plasma levels of glycine, which is a synthet
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br Introduction Prostate cancer is
2021-12-02

Introduction Prostate cancer is the most commonly diagnosed cancer and the second leading cause of cancer deaths in men in the United States, accounting for about 30,000 cancer deaths annually [1]. Epidemiological studies that show geographical variations in prostate cancer incidence and mortalit
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ICH induced striatal lesion produced a
2021-12-02

ICH-induced striatal lesion produced a reduction of EAAT1 expression analogous to the decreased glutamate uptake at 6 h. The combined reduction of excitatory amino MK2206 mg transporters and of glutamate uptake activity might explain the well-known glutamate excitotoxicity following brain ischemia
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