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The synthetic route chosen for the preparation of the
2019-10-14
The synthetic route chosen for the preparation of the substrates 18 is shown in Scheme 3. Commercially available 4-aminobenzyl alcohol 13 was found to be relatively unstable to storage and hence it was prepared immediately before use by reduction of the readily available and inexpensive 4-nitrobenzy
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roxadustat clinical A factor that complicates the use of hum
2019-10-14
A factor that complicates the use of human liver roxadustat clinical is one of variability, which arises in part because many of the human liver samples available for research show various stages of a variety of disease states (steatosis (fatty liver), cirrhosis, carcinogenesis in adjacent tissue),
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br Materials and methods br Results br Discussion Drug
2019-10-14
Materials and methods Results Discussion Drug of abuse induces widespread NVP 231 and changes in the molecular and cellular functions in circuits between VTA and its neighbored regions such as NAC, and amygdala. It is belived that these changes result behavioral phenotype that characterize
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Upstream Stimulatory Factor USF binding
2019-10-14
Upstream Stimulatory Factor (USF) binding to the −65 E-box is required for the regulation of FAS promoter activity in fasting/feeding [97], [98]. DNA-PK are identified as a USF-interacting protein [99]. In response to feeding/insulin, the transient double-stranded DNA breaks occurred during the tran
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br Introduction Coping with DNA damage is possible
2019-10-14
Introduction Coping with DNA damage is possible thanks to surveillance mechanisms (checkpoints), that detect the problem and promote its solution [1], [2], and to repair and tolerance pathways that remove the lesions or reduce the damage consequences [3], [4]. Failures in these processes have a h
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Three DDR binding sites have
2019-10-14
Three DDR2 binding sites have been mapped on the collagen triple helix by us for collagen type 1 and by others using the collagen toolkit for collagen type 2. All of the three reported binding sequences are conserved in the α1 chain of collagen types 1, 2 and 3. The central motif sequence GARGQAGVMG
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The purposes of this study is to develop an
2019-10-14
The purposes of this study is to develop an experimental model of CysLT2 receptor-mediated LTC4-induced lung air-trapping in guinea pigs using S-hexyl GSH, and to clarify the mechanism underlying response to such trapping using montelukast, a CysLT1 receptor antagonist, BayCysLT2RA, a CysLT2 recepto
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Dexamethasone DEX a potent synthetic glucocorticoid drug
2019-10-14
Dexamethasone (DEX), a potent synthetic glucocorticoid drug, is effective for treatment of a range of inflammatory and autoimmune conditions as well as the reduction of side effects associated with chemotherapy. On the Czech Republic pharmaceutical market, DEX is incorporated into eighteen drugs use
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br Material and methods br Results
2019-10-14
Material and methods Results Discussion Monomeric CDK5 shows no enzymatic activity and requires the association with a regulatory partner for activation (Dhavan and Tsai, 2001). Here, we found that CDK7 might be one of the partners required for activation of CDK5 in the skin tissue, based o
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Resveratrol is a phytoalexin that occurs in relatively
2019-10-14
Resveratrol is a phytoalexin that occurs in relatively large amounts in peanut, berries, grapes, and red wine (Soleas et al., 2001). A recent study showed that resveratrol prevents social deficit in an animal model of autism, indicating its potential for possible therapeutic use in children with aut
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Why are Tfh cell dynamics
2019-10-12
Why are Tfh cell dynamics so fundamentally different in naive and immune animals? Initially, GC BEC must pass stringent affinity and specificity checkpoints to ensure only high-affinity non-self-reactive cells are selected. Therefore, restricting primary Tfh cells with the greatest helper capacity
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The molecular docking data supported the potential interacti
2019-10-12
The molecular docking data supported the potential interaction of lapachol and the synthetic naphthoquinonolyl compounds with the PfDHODH enzyme as the putative mechanism of action and the inhibition of parasite growth in vitro. In general, compounds fit well into the binding pocket of PfDHODH, the
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Widely expressed mammalian adhesion receptors for fibrillar
2019-10-12
Widely expressed mammalian adhesion receptors for fibrillar collagens include the α2β1- and α11β1-integrins and the discoidin domain receptors (DDRs), DDR1 and DDR2 (Leitinger, 2011). Integrins and DDRs bind distinct and separate motifs in native fibrillar collagen (Curat et al., 2001, Vogel et al.,
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br Materials and methods br Results br Discussion The
2019-10-12
Materials and methods Results Discussion The studies reported here provide a more direct link between conformations of the glycine-rich region of DAPK and enzyme activity. As schematically illustrated in Fig. 3, the various conformations of DAPK with bound substrate or product can be consid
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Transduction of cellular signals by G protein
2019-10-12
Transduction of cellular signals by G protein-coupled receptors (GPCRs) is stringently regulated to prevent the deleterious effects of unrestrained GPCR signaling. The rapid termination of signaling mediated by agonist-occupied GPCRs is referred to as homologous desensitization and involves the foll
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