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GSK2334470 To develop novel EPAC inhibitors Zhou and co work
2021-02-09
To develop novel EPAC inhibitors, Zhou and co-workers optimized the HTS hit as the chemical lead. After modifications of the substituents on the phenyl ring or C6-position of compound , compound () was identified to be the more potent compound in this series with an IC value of 4.0µM (EPAC2). Dockin
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Recent reports revealed that CSE
2021-02-09
Recent reports revealed that CSE affects the endothelial cells of various tissues like kidney, liver, heart including UNC 0646 [26,30]. The damage of brain endothelial cells enhances the progress of cognitive dysfunction due to the accumulation of toxic free bio-radicals and activation of inflammato
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During the entire life of individual articular chondrocyte a
2021-02-09
During the entire life of individual, articular chondrocyte as well as subchondral bone receives acute or chronic stress. Joints homeostasis is maintained by biomechanical stress, as rapid loss of proteoglycan in joints occurs due to immobilization or disuse. These osteophytes are fibrocartilage cap
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Despite the weak and transient nature
2021-02-09
Despite the weak and transient nature of E2–E3 interactions, this binding is required for the transfer of ubiquitin to the substrate. The low affinity characteristics of this interaction may be due to the fact that E2s use the same surface to interact with E1s and E3s, and hence while binding to an
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br A brief introduction to DUBs The reversal of ubiquitin
2021-02-09
A brief introduction to DUBs The reversal of ubiquitin conjugation of targeted proteins relies on deubiquitinating emca synthesis (DUBs), which catalytically cleave single Ub or poly-ubiquitin chains from proteins. The human genome encodes approximately 100 potential DUBs which can be classified
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Tumor cells exposed to the effect of these compounds
2021-02-09
Tumor DDD107498 exposed to the effect of these compounds were shown to become chemo and radio-sensitive. Based on that, it was possible to anticipate the selectivity requirement for DNA-PK inhibition and the best route for their development. Accordingly, prompted by the clinical significance and th
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The lungs dissected from week mice
2021-02-08
The lungs dissected from 4–5-week mice were cut into small pieces and then immersed in Dulbecco's modified Eagle's medium (Invitrogen, Carlsbad, CA) containing collagenase II (2 mg/ml), trypsin (2.5 mg/ml), Dnase I (2 mg/ml), penicillin (100 U/ml), and streptomycin (100 μg/ml) for 12 hours at 37 °C
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br Materials and methods br Results
2021-02-08
Materials and methods Results Discussion Although no increase in DAPK activity was detected at early time points associated with neuronal apoptosis, it is possible that the spread of apoptosis through the Fenoprofen Calcium sale following HI is not synchronized enough to yield a large, con
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Prednisolone br Materials and methods br Results As shown in
2021-02-08
Materials and methods Results As shown in Table 1, blood urea nitrogen and serum creatinine levels were significantly elevated at both 1st and 7th days of pyelonephritis, when compared with those of the control group (PPrednisolone formation or intratubular neutrophils, while tubules showed mi
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Today many strategies have been developed to enhance
2021-02-08
Today, many strategies have been developed to enhance CXCR-4 receptor Acetazolamide receptor on the cell surface, either by modifying the cell culture medium or by modifying the CXCR-4 gene in BMSCs to stimulate stem cell recruitment (Jiang et al., 2012, Liu et al., 2014b). For instance, the pre-co
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This review focuses on the atomic basis of CRM
2021-02-08
This review focuses on the atomic basis of CRM1-mediated nuclear export. There are now 27 crystal structures of CRM1 in the Protein Data Bank (PDB) (www.rcsb.org) [64]. Collectively, this large body of work explains various aspects of CRM1 function. Here we summarize the structure–function studies t
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Protein A/G Although the presence of at least one triple hel
2021-02-08
Although the presence of at least one triple helix domain is typically the collagen signature, collagens are modular proteins composed of a succession of collagenous (COL) and non-collagenous domains (NC) that are both involved in collagen functions and in receptor binding. COL domains are linked by
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br Acknowledgements br Introduction In Arabidopsis thaliana
2021-02-08
Acknowledgements Introduction In Arabidopsis thaliana (L.) Heynh, there are at least four copies of the caseine kinase-like gene Ck1, which is involved in peptide phosphorylation in mammals [1]. These genes are distributed on Celecoxib receptor 1, 2, 4, and 5. A similar number of copies for C
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The repeat sequence TTAGGG of telomere
2021-02-08
The repeat sequence “TTAGGG” of telomere could be directly recognized by TERF1. TERF1 is indispensable for the maintenance of telomere voltage gated sodium channel structure and integrity (Tan et al., 2017). Trf1 genetic depletion in vivo induces a persistent DNA damage response and telomere uncapp
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There is evidence that the response
2021-02-08
There is evidence that the response of CYP450 activity to DEX is species-specific. CYP1A and CYP3A expressions were strongly induced by DEX in porcine hepatocytes (Rasmussen et al., 2014) and in rat and human, but not minipig or beagle dog hepatocytes (Lu and Li, 2001). Within fish, there are also s
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