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While previously reported optimizations on compound
2021-03-29
While previously reported optimizations on TCS 2002 focused on the phenyl ring A () and substituents on isoxazole ring, other alternatives to replace isoxazole ring were never explored. Herein, we propose to replace the isoxazole with its bioisosteric substituted phenyl ring B () to explore new ch
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Endothelin appears to have direct effects on neoplastic cell
2021-03-29
Endothelin 1 appears to have direct effects on neoplastic GDC-0994 receptor by inducing cellular proliferation, angiogenesis, migration, invasion, and inhibition of apoptosis [10]. Endothelin 1 mediates mitogenic effects in some epithelial tumors such as colorectal, ovarian, and prostate cancers [1
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How does APC C recognize its substrates and catalyze their
2021-03-27
How does APC/C recognize its substrates and catalyze their ubiquitylation? How are the outcomes and timing of these activities regulated? These questions have driven a decade of structural studies that begin to explain how APC/C interacts with coactivators, substrates, and E2s, and how these interac
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br Prospect of DDR antagonist DDR a
2021-03-27
Prospect of DDR2 antagonist DDR2, a receptor of tyrosine kinase has been found now to be reported to play a significant role in onset of osteoarthritis at the early stage of diseases progression. The DDR2 are the receptor for extracellular collagen and activated upon the binding of collagen resul
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Common to all models for nuclear transport is
2021-03-27
Common to all models for nuclear transport is the binding of importins/exportins to FG repeats found in about a third of the ∼30 nucleoporins, the so-called FG-Nups (Iovine et al., 1995, Rexach and Blobel, 1995); for review, see Grossman et al. (2012), Stewart (2007), and Terry and Wente (2009). FG-
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br Experimental procedures br Introduction Perfluorooctane s
2021-03-27
Experimental procedures Introduction Perfluorooctane sulfonate (PFOS) is an anthropogenic compound with high thermal, chemical and biological stability, which makes it a perfect ingredient for many industrial applications (Kissa, 2001). Nevertheless, these characteristics also mean that PFOS i
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From our array results Supplemental Fig S we found that
2021-03-27
From our array results (Supplemental Fig. S2), we found that differential lncRNA profiling exhibited much greater disparity compared to differential gene profiling in CD28nullCD8+ T cells, indicating that differentially expressed lncRNA(s) would serve as ideal hallmarks. Moreover, we were fortunate
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Located on the fore tarsals of
2021-03-27
Located on the fore-tarsals of the front pair of legs, the Haller’s organ is presumed central to tick chemosensation. Recent genomic, transcriptomic and proteomic investigations have identified several families of transmembrane proteins in the forelegs of ticks that are likely involved in olfactory
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br Methods Ventricular cardiomyocytes from
2021-03-27
Methods Ventricular cardiomyocytes from adult male Wistar rats were isolated using a standard enzymatic digestion [11]. Cells were incubated at 37°C for 4 to 6h with Tyrode solution (in mM: 140 NaCl, 4 KCl, 1.1 MgCl2, 10 HEPES, 10 glucose, 1.8 CaCl2; pH7.4, with NaOH) supplemented or not with 10μ
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br Methods br Results br Discussion I R induces
2021-03-26
Methods Results Discussion I/R induces oxidative stress and increases the intracellular levels of ROS, resulting in tissue damage [31]. ROS is generated by mitochondrial electron transport chain, nicotinamide (+)- Corydaline dinucleotide phosphate (NADPH) oxidase complex, xanthine oxidase
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Results from experiments in model systems have suggested
2021-03-26
Results from experiments in model systems have suggested that the DPRs translated from the HRE of C9ORF72 are toxic and play a role in disease pathogenesis (reviewed in Taylor et al. (2016)). Although the DPRs are present in neurons and glia in various regions of the central nervous system (CNS) ear
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Another mechanism underlying on the toxicity
2021-03-26
Another mechanism underlying on the toxicity of dopaminergic neurons might be related to dopamine-dependent initial oxidative stress [60]. Dopamine Enalapril Maleate synthesis mediated by monoamine oxidase (MAO) can produce hydrogen peroxide as a by-product, and excess dopamine can undergo auto-oxid
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SB 290157 trifluoroacetate salt br Experimental section br R
2021-03-26
Experimental section Results and discussion Conclusions In conclusion, we have presented an autocatalytic recycling amplification electrochemical biosensing platform for simple, rapid and ultrasensitive detection of MTase activity by combining methylation-sensitive restriction endonuclease
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Previous synthetic lethal screening efforts Cox et al have m
2021-03-26
Previous synthetic lethal screening efforts (Cox et al., 2014) have mainly used RNAi as a means of identifying potential targets (Barbie et al., 2009, Kim et al., 2016, Luo et al., 2009, Scholl et al., 2009), although a few screens (Shaw et al., 2011, Steckel et al., 2012) have been performed with s
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br Acknowledgements br Introduction Lung cancer treatment st
2021-03-26
Acknowledgements Introduction Lung cancer treatment strategies, especially molecular targeted therapy, have progressed rapidly. However, most established treatments are for adenocarcinoma of the lung, not for squamous cell carcinoma (SQCC). SQCC constitutes approximately 30% of lung cancers, w
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