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br Acknowledgements br Introduction Protein tyrosine phospho
2021-01-28
Acknowledgements Introduction Protein–tyrosine phosphorylation, catalyzed by protein–tyrosine kinases and protein–tyrosine phosphatases, has a pivotal role in the regulation of a wide variety of cellular processes. Similar numbers of tyrosine kinases and tyrosine phosphatases are encoded by th
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Lonidamine Compounds were synthesized as illustrated
2021-01-28
Compounds – were synthesized as illustrated in , , , , . 3-(1-tetrazole-5-yl)benzaldehyde was obtained in 95% yield via [2+3] cycloaddition of sodium azide to commercially available 3-cyanobenzaldehyde in presence of triethylamine as reported in the literature. Nitration of 3-hydroxyacetophenone wit
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From an industrial perspective the low turnover numbers and
2021-01-28
From an industrial perspective, the low turnover numbers and limited substrate scope of α-KG halogenases still represents a significant challenge. However, in light of the fact that currently no chemical processes are available for the selective halogenation of aliphatic carbon centers in complex mo
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Schizandrin A br Materials and methods br Results
2021-01-28
Materials and methods Results Discussion Chronic inflammation is central to COPD and plays a critical role in the disease pathogenesis and progression. Among the various inflammatory cells, neutrophils are the key players in COPD pathogenesis. Their numbers are raised in airspaces and lung
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Among the Ub interactions observed in
2021-01-28
Among the ~Ub interactions observed in the HOIP structure is one that involves a RING2 domain (from the non-cognate HOIP) [47]. A similar binding interaction was defined between HHARI RING2 and the hydrophobic patch on Ub by NMR [54]. HHARI RING2 mutations that ablate the interaction inhibit formati
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A prominent example of such enzyme is the proteasome a
2021-01-28
A prominent example of such enzyme is the proteasome, a highly promising target not only in cancer, but also in inflammatory and autoimmune diseases. Circulating proteasomes and respective anti-proteasome autoantibodies were detected in serum samples from patients with autoimmune diseases such as mu
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Based on the similar activities of
2021-01-28
Based on the similar activities of Rad6p and Cdc34p (i.e., both are E2 ub-conjugating enzymes) on ubiquitinylation of p33 replication protein, we propose that Rad6p and the plant Ubc2p mono- and bi-ubiquitinate the viral replication proteins in order to facilitate the recruitment of the cellular ESC
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br Introduction Diacylglycerol kinase DGK is a
2021-01-28
Introduction Diacylglycerol kinase (DGK) is a lipid-metabolizing enzyme that phosphorylates diacylglycerol (DG) to produce phosphatidic teva 3026 (PA) [[1], [2], [3], [4]]. DG and PA act as lipid second messengers in a wide variety of biological processes. Ten DGK isozymes (α, β, γ, δ, η, κ, ε,
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br Sphingosine kinase One of the enzymes closely related to
2021-01-28
Sphingosine kinase One of the enzymes closely related to DGKs are the sphingosine kinases (SKs). These enzymes catalyze the conversion of sphingosine (Sph) to sphingosine-1-phosphate (S1P). SKs and DGKs are closely related lipid kinase in term of basic enzymology and the mechanism of regulation a
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Introduction Quassinoids are natural products
2021-01-28
Introduction Quassinoids are natural products formed through the oxidative degradation of triterpene derivatives with anti-inflammatory, antimicrobial, antineoplastic, and antiplasmodial effects (Chakraborty and Pal, 2013; Houël et al., 2013). They are characteristic ingredients of the family Simar
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br Conclusion In vivo pharmacokinetic
2021-01-28
Conclusion In vivo pharmacokinetic studies showed that dasatinib monohydrate pretreatment significantly decreased the blood level of CsA in rats, which was most probably due to the induction of CYP3A2 isoenzymes. The nilotinib pre-treatment had no significant effects on cyclosporine pharmacokinet
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To elucidate the potential mechanism underlying osteosarcoma
2021-01-28
To elucidate the potential mechanism underlying osteosarcoma cell growth decrease by CDK4 inhibition, flow cytometry analysis was used to determine MK-8745 and apoptosis in human osteosarcoma cells after palbociclib treatment. The results showed that osteosarcoma cells were arrested in G1 phase of
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Currently multiple clinical trials of CSF
2021-01-28
Currently, multiple clinical trials of CSF-1/CSF-1R-targeting agents in combination with standard treatment modalities and immunotherapies are underway (Table 1). In particular, results for combinations with checkpoint blockade inhibitors and other immunotherapeutic approaches are eagerly awaited.
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The small molecule d mannuronic
2021-01-27
The small molecule β-d-mannuronic kisspeptin (M2000), patented (DE-102016113018.4), has been tested as an anti-inflammatory and a novel immunosuppressive agent in various experimental models such as animal models of immune complex glomerulonephritis, nephrotic syndrome, multiple sclerosis and rheum
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Toremifene ApoE is secreted from astrocytes glia into
2021-01-27
ApoE is secreted from astrocytes/glia into the interstitial fluid and is important for metabolizing Aβ because of its propensity for binding Aβ as a cholesterol and phospholipid acceptor in reverse cholesterol transport [8]. Aβ oligomers show a direct toxicity to neurons, and ApoE inhibits oligomer
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