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br Fragment based drug discovery FBDD
2021-04-30
Fragment-based drug discovery (FBDD) is a powerful method to discover drug leads and has been widely adopted in both academia and industry. FBDD can be used to explore chemical Cy5 carboxylic acid (non-sulfonated) space with libraries which are smaller in size, producing drug leads with high liga
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Steady state mRNA levels of CYP A isoforms were not
2021-04-30
Steady-state mRNA levels of CYP3A isoforms were not changed during liver insufficiency. Suppression of these isoforms was observed only at the protein and activity levels, suggesting a nongenomic mechanism of CYP3A isoform downregulation during liver insufficiency. Nonetheless, transcriptional acti
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DDI is one of the main
2021-04-30
DDI is one of the main problems with serious clinical consequences in clinical settings. Several reports have highlighted the role of modulation of drug-metabolizing enzymes, especially CYP450 s, as a major mechanism involved in clinical DDIs [3,4,7]. The present study aimed to investigate the effec
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Cancer has been linked to both genetic and
2021-04-30
Cancer has been linked to both genetic and epigenetic changes. Epigenetic modifications, mainly DNA methylation at CpG dinucleotides, affect the regulation of gene transcription without altering the gene's sequence. Short sequences rich in CpG dinucleotides (i.e., CpG islands) are often found in the
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PD-1/PD-L1 Inhibitor 3 To characterize Ea and S DC AC electr
2021-04-30
To characterize Ea and γ·S, DC/AC electrical parameters will be determined from MIL standard measurements in a temperature range of −55 to +200°C. It is therefore necessary also to characterize the junction temperatures and hot points by infra-red or electrical method. The accelerated aging, represe
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br Patients and methods br Results Table shows relevant demo
2021-04-29
Patients and methods Results Table 1 shows relevant demographic and clinical characteristics of the 123 patients in the cohort. BAL fluid samples were obtained at a median of 172.5 days after allo-HSCT (range 3 days to five years). Discussion The definitive abandonment of traditional cultu
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br Acknowledgements This work was
2021-04-29
Acknowledgements This work was supported in part by JSPS KAKENHI Grant Number 26292031. Introduction The Cys-loop receptors constitute an important superfamily of ligand-gated ion ANP (1-11), rat (LGICs) and mediate synaptic transmission in both invertebrate and vertebrate nervous systems (J
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br Acknowledgements br Introduction Ischemic retinopathy is
2021-04-29
Acknowledgements Introduction Ischemic retinopathy is common to the major causes of blindness, including proliferative diabetic retinopathy, venous occlusion, and retinopathy of prematurity. The hypoxia that follows retinal capillary obliteration drives deregulated growth of new blood vessels
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Prostanoids typically act in an autocrine and paracrine
2021-04-29
Prostanoids typically act in an autocrine and paracrine fashion by binding to specific receptors in target Doxorubicin and there is evidence that both PGE2 and prostacyclin may be required for the optimal activation of angiogenesis (Hata and Breyer, 2004). PGE2 and prostacyclin bind to their specif
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High concentrations of kC may also
2021-04-29
High concentrations of 7kC may also arise from dietary intake of processed cholesterol-rich food, likely favoring or worsening inflammatory bowel disease (IBD) [5,13]. Furthermore, IBD has been associated with a dysregulation of colonic 11β-HSD expression, exhibiting increased 11β-HSD1 and decreased
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phospholipase a2 inhibitor Dysfunction of the ubiquitin prot
2021-04-29
Dysfunction of the ubiquitin-proteasome system causes abnormal organelle morphology and impairs sperm formation and maturation steps resulting in male infertility [[7], [8], [9]]; this indicates that ubiquitination is essential for spermatogenesis and sperm function during fertilization. β-catenin i
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Why then is leading strand DNA synthesis reduced relative to
2021-04-29
Why then is leading-strand DNA synthesis reduced relative to lagging-strand synthesis in rad53-1 mutant thiostrepton under replication stress? To gain insight into this question, we first determined whether the firing of late origins in rad53-1 mutant cells contributes to compromised leading-strand
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Cdc which is involved in filopodium formation
2021-04-29
Cdc42, which is involved in filopodium formation, and Rac1, which is involved in lamellipodium formation, engage in cross-talk with one another [25,26,30,31]. In general, filopodium formation precedes lamellipodium formation, and filopodium formation (Cdc42 activity) suppresses lamellipodium formati
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To compare glucose metabolism via oxidative phosphorylation
2021-04-29
To compare glucose metabolism via oxidative phosphorylation to that via glycolysis, a bioenergetics plot was constructed (Fig. 3A). In most cells, a decrease in one bioenergetics pathway is compensated by an increase in the other. However, following NAT1 deletion, there was a decrease in both oxidat
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NMR was employed for the
2021-04-29
NMR was employed for the determination of un-ligated domain 1 structure of DDR2 receptor. The collagen-binding site on the same was identified by cross saturation experiment and mutagenesis [40]. Birgit leitinger identified the binding site of collagen with DDR2 receptor, which was three spatially a
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