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Remarkably most of these molecules are
2021-09-30

Remarkably, most of these molecules are also quite effective in interfering with the proliferation of the drug-resistant cancer cell lines, with IC50 values ranging from 0.59 to 2.93 μM against MCF-7/ADR cells, and from 0.160 to 1.17 μM against NSCLC-resistant H1975 cells. Among these molecules, com
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Cell stiffness is determined by
2021-09-30

Cell stiffness is determined by the cytoskeleton, an intracellular polymeric network consisting of chemical informative post filaments, microtubules, intermediate filaments, and crosslinking proteins [38]. Low cell stiffness has been correlated with reduced formation of well-defined F-actin filamen
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br Acknowledgments I thank Takeshi Sakaba for critical readi
2021-09-30

Acknowledgments I thank Takeshi Sakaba for critical reading of the manuscript and helpful comments. This work was supported by JSPS/MEXT KAKENHI Grant Numbers 17K19466, 17H03548. Introduction The oral route of drug application is the main route in pharmacology since it is easy to handle and o
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A biochemical characterisation of this functionally crucial
2021-09-30

A biochemical characterisation of this functionally crucial LSD1-p53 interaction is the focus of this study. Using several complementary assays [29], [30], [31], [32], we find that a well-defined segment of p53-CTD is capable of binding to LSD1 active site, thereby inhibiting the enzymatic activity
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br Conclusions br Acknowledgments This
2021-09-30

Conclusions Acknowledgments This work was financially supported partly by Shanghai Pujiang Talent Project (No.: 08PJ14017), the National Natural Science Foundation of China (Nos.: 20771029 and 91013001) and Shanghai Leading Academic Discipline Project (No. B108). Soluble guanylate cyclase (
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Main Text There are over small GTPases that
2021-09-30

Main Text There are over 200 small GTPases that play critical roles in diverse fundamental cellular processes such as signal transduction, simvastatin zocor dynamics, and intracellular trafficking. Most of the GTPases act as switch-like molecules by cycling between the guanosine triphosphate (GTP)
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KYNA has been shown to regulate iNKT cytokine release Fallar
2021-09-30

KYNA has been shown to regulate iNKT cytokine release (Fallarini et al., 2010) and at high concentrations to reduce LPS-induced TNFα release from cultured peripheral blood mononuclear Meropenem trihydrate receptor (Wang et al., 2006). Our results show that elevating KYNA to “exercised” levels is su
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Thus synthesized thienopyrimidine derivatives were evaluated
2021-09-30

Thus synthesized thienopyrimidine derivatives were evaluated in vitro for GPR119 agonistic activity, and the results are summarized in , , . First, we fixed the 4-methylsulfonylphenyl substituent at the R position on the thienopyrimidine ring, and derivatized at the R position. As shown in , and s
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br Several reports have shown an anti proliferative effect
2021-09-30

Several reports have shown an anti-proliferative effect of type I IFNs on CD4+ T Phenformin activated in vitro either upon anti-CD3 antibody treatment [28,29] or upon cognate antigen stimulation [29]. However, the in vivo setting is a lot more complex, since the final outcome is the net effect of
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br Materials and methods br Results In
2021-09-30

Materials and methods Results In order to address the role played by the catalytic and the anticodon-binding domains of E. coli GluRS in cognate and non-cognate aminoacylation, the two domains (NGluRS: 1–314; CGluRS: 318–471) of E. coli were expressed and purified (Fig. 1b). Prior to assessing
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With rare exceptions the biological role of secretase cleava
2021-09-30

With rare exceptions, the biological role of γ-secretase cleavage of substrates other than Notch 1 has been ignored during proof of concept preclinical repurposing studies. For example, in the GSI AD trial, many individuals noted changes in hair color, apparently due to inhibition of tyrosinase, ano
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br Experimental section br Results and discussion br
2021-09-30

Experimental section Results and discussion Conclusions To summarize, the act of conjugating a ASC ligands to a Ru(II) polypyridyl subunits resulted in a class of excellent DNA binders. A comparison of the DNA binding abilities of the free ASC ligand and the complexes, has revealed that the
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N1-Methylpseudo-UTP All data were analyzed using SAS softwar
2021-09-29

All data were analyzed using SAS software (version 9.3, SAS Institute Inc., Cary, NC). Because of very low FFAR1 protein detection (at the detection limit or no signal) in 3 H-BHB cows, quantification was not possible within a linear range and therefore these animals were omitted from the statistica
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The main consequence of glucose catabolism is the elevation
2021-09-29

The main consequence of glucose catabolism is the elevation of ATP concentration, which in turn suppresses the ATP sensitive potassium (KATP) channels gating function. The KATP channels are octamers composed of the tetrameric inward-rectifying potassium channels (with Kir6.1 and Kir6.2 subunits), th
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Aspartame l aspartyl l phenylalanine methylester
2021-09-29

Aspartame (l-aspartyl l-phenylalanine methylester) is a dipeptide artificial sweetener that is widely used as a non-nutritive sweetener in various food products [1]. The increased market of dietary products and the development of new synthetic sweetening compounds have not been sufficiently explored
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