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A novel series of DHODH inhibitors was developed by us
2021-01-04
A novel series of DHODH inhibitors was developed by us based on a lead that was discovered during a docking procedure and medicinal chemistry exploration. The activity of the initial lead was improved by a QSAR method and yielded low nanomolar inhibitors. Introduction The most common metabolic h
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br Materials and methods br Results br Discussion CDK
2021-01-04
Materials and methods Results Discussion CDK4 has been identified recently as a potential therapeutic target in human breast cancer, liposarcoma, melanoma, and glioblastoma [[37], [38], [39]]. Due to the importance of CDK4 activity in cancer cells, CDK4 inhibitors have emerged as promising
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br Conclusions CK inhibition protects young
2021-01-04
Conclusions CK2 inhibition protects young and aging WM function against an ischemic episode by preserving oligodendrocytes and axonal structure by maintaining mitochondrial integrity. CK2 recruits CDK5 and AKT/GSK3ß signaling to mediate WM ischemic injury in a differential spatiotemporal manner s
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Targeting the MAPK pathway has
2021-01-04
Targeting the MAPK pathway has attracted significant interest in cancer therapy. Efforts directly targeting RAS protein are believed to be very challenging in spite of the promise shown by a few RAS inhibitors in the early development stage. Clinical benefits achieved by BRAF and MEK inhibitors have
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An Ubl modification requires several steps that are catalyze
2021-01-04
An Ubl modification requires several steps that are catalyzed by three enzymes, referred to as E1 (activating enzyme), E2 (conjugation enzyme), and E3 (ligase). The SUMO E1 is a heterodimer of SAE1 and Uba2 (also known as SAE2). In brief, an Ubl is first activated by E1 through ATP hydrolysis and fo
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Lonafarnib In accordance with its original
2021-01-04
In accordance with its original discovery, EBI2 may play its major role in response to viral infections or in a pathological context such as in autoimmunity. Although we found a significant delay of onset in the Th17 transfer EAE model, active EAE was unchanged in absence of EBI2. At the moment, we
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In contrast to inflammatory cytokines TGF has
2020-12-31
In contrast to inflammatory cytokines, TGF-β has immunosuppressive properties yet is also important for tissue imprinting immune cell function during development [23]. Salivary gland (SG) ILCs, in addition to liver and intestinal intraepithelial ILC1, express markers denoting tissue residency and TG
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In humans several different small ubiquitin related
2020-12-31
In humans, several different small ubiquitin-related modifier (SUMO) paralogs can be conjugated to cellular proteins. The human genome codes for five SUMO paralogs (SUMO1–5); of these, SUMO1 and the almost identical SUMO2 and SUMO3 are ubiquitously expressed. Sumoylation is executed by an enzymatic
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br Discussion Although DNA has a limited chemical
2020-12-31
Discussion Although DNA has a limited chemical stability it has long been known that DNA in blood stains may remain relative stable for weeks, months, or even years at ambient temperature,1, 2, 3, 4, 5, 6 and samples (e.g., reference samples) that have been transferred to a matrix, e.g., FTA® pap
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In this study we characterized the metabolic
2020-12-31
In this study, we characterized the metabolic function of tra2 in the Drosophila fat body. Similar to the 9G8 phenotype, decreasing tra2 levels in the Drosophila fat body using RNAi resulted in increased starvation resistance and a large increase in triglycerides. This increased storage of triglycer
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While we are taking full
2020-12-31
While we are taking full responsibility for any remaining errors and shortcomings of the paper, we would like to thank Dr. Jong-Hyeon Jeong, Department of Biostatistics, Graduate School of Public Health, University of Pittsburgh, for offering us insight and literature pointers useful in our quest to
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System Analysis and Modeling In this work
2020-12-31
System Analysis and Modeling - In this work, a three-level hierarchical modeling – composed by combinatorial and state-space models – is used: (1) First, failure rates () of TMS servers subsystem units are estimated through continuous Markov chains; (2) Then, the single server Piperlongumine failur
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Furthermore in silico physicochemical characters and pharmac
2020-12-31
Furthermore, in silico physicochemical characters and pharmacokinetic parameters for the synthesized compounds were predicted using dedicated computer software [34], [35], [36] to ensure successful in vivo therapeutic activity. Practical logP testing was performed and compared to the theoretical val
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PET CT static images of F
2020-12-31
PET/CT static images of F-CJ-042794 acquired at 1h p.i. from LNCaP tumour-bearing mice with/without co-injection of non-radioactive CJ-042794 (50μg) are shown in . The LNCaP tumours were clearly visualized in PET images with a moderate tumour-to-background contrast. High radioactivity accumulation w
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Neurons in the striatum unlike those
2020-12-30
Neurons in the striatum, unlike those in the T0901317 and cerebellum, do not form a layered or columnar structure. Although they appear to be randomly distributed, they are actually scattered in two embryologically different compartments called striosomes (often referred to as “patches” in rodents)
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