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Estrogen related receptors ERRs are orphan nuclear receptors
2020-04-10
Estrogen-related receptors (ERRs) are orphan nuclear receptors and have three members including ERRα, ERRβ, and ERRγ (Yasumoto et al., 2007). Though they are termed as ERRs due to the sequence homology with estrogen receptors, they don’t need to bind estrogens to exert action. Generally, ERRs bind t
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In SLO permeabilized human sperm
2020-04-10
In SLO-permeabilized human sperm, the AR elicited by calcium, persistently active Arf6 [41] and Rab3A, 8-pCPT-2′-O-Me-cAMP [8], diacylglycerol and a non-hydrolyzable analog [35], is sensitive to the PLC blocker U73122. Furthermore, 8-pCPT-2′-O-Me-cAMP elicits a calcium signal in non-permeabilized sp
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Herein we designed a strategy utilizing
2020-04-10
Herein, we designed a strategy utilizing the target-protection method to produce a signal in a system involving fluorescence CuNPs stabilized by dumbbell template DNA (DT DNA) through a locked circle consisting of two poly T loops and a poly (ATTA) stem. In the presence of MTase, DT DNA was modified
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This hydrophobic biphenyl tail gave good
2020-04-09
This hydrophobic biphenyl tail gave good binding affinity for human DHODH enzyme (IC LJH685 was found to be the main metabolite in human microsomes and it was 100-fold less active against hDHODH than the ester. In an attempt to identify the specific non-covalent binding interactions which were res
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Collectively the results presented here provide new insights
2020-04-09
Collectively, the results presented here provide new insights into ligand binding, clustering, spatial distribution, and phosphorylation of DDR1b and DDR2 in response to soluble collagen I. As depicted in the cartoon of Scheme 1, we postulate a model in which the spatial distribution and assembly o
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Here we describe a novel series of arylazoderivatives develo
2020-04-09
Here, we describe a novel series of arylazoderivatives developed from CAN508, one of the first known selective CDK9 inhibitors. We focused on modification of both ends of parental molecule, CAN508, in order to improve cytotoxicity and CDK activity. We therefore analyzed how changes in molecules will
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Analysis of Table shows that compound b
2020-04-09
Analysis of Table 1 shows that compound 7b, in which the biphenyl scaffold does not bear any substituent, displays its inhibitory potency in the micromolar range (IC50 = 11 μM). If the amide bridge is moved from position 1 to 3 of the biphenyl system, product 7c is yielded, whose potency is about 4
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br Conclusions br Declaration of interest
2020-04-09
Conclusions Declaration of interest Acknowledgment This work was supported by an AIRC (Associazione Italiana Ricerca Cancro-Milan) Grant KFR062-2 to A.G.L, by Ricerca Funds by Fondazione IRCCS Ca’ Granda Ospedale Maggiore Policlinico (Grant No. 180/01) and by the ERA-NET “ERare” (Grant GO
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br Introduction The innate immune system stands the
2020-04-09
Introduction The innate immune system stands the first line of the defense that protects the host from viral intrusion, depending on pattern recognition receptors (PRRs) and the corresponding pathways [[1], [2], [3], [4]]. The pathogen-associated molecular patterns (PAMPs) of the invading viruses
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The transcriptome analysis of barley seeds in two
2020-04-09
The transcriptome analysis of barley seeds in two tissue fractions: starchy endosperm/aleurone and embryo/scutellum, during maturation, desiccation and germination, revealed the large group of GA-responsive genes (Sreenivasulu et al., 2008). These transcripts have been divided into two groups. Nearl
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Table summarizes the literature data available on the occurr
2020-04-09
Table 4 summarizes the literature data available on the occurrence of these two pitavastatin of steroidal compounds in sludge and sediments. In activated and digested sewage sludge, the concentrations of ethynyl estradiol (17 ng/g), estrone (37 ng/g ), and estradiol (49 ng/g) found in one of the ve
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The role of activation of xenosensor
2020-04-09
The role of activation of xenosensor nuclear receptors such as PPARα, CAR, and PXR in producing hepatomegaly and liver tumors in rodents has been well-established (Klaunig et al., 2003, Lake, 2009). In the case of PPARα, the increase in liver weight results from increased peroxisomal mass and expans
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br Results br Discussion In this paper
2020-04-09
Results Discussion In this paper we present insights into the observed specificities of inhibitors targeting the ubiquitin-activating and related E1 G-15 via crystal structures of the specific NEDD8-E1 inhibitor MLN4924, the dual NEDD8/Ub E1 inhibitor ABPA3, and the selective Ub-E1 inhibitor
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Fludarabine Phosphate Materials and methods Cell culture and
2020-04-08
Materials and methods Cell culture and receptor gene transfection. PC12 Fludarabine Phosphate were purchased from the Institute of Cell Biology, Chinese Academy of Sciences, Shanghai, China. The cDNA for mouse CysLT1 or CysLT2 receptor (mCysLT1 and mCysLT2, subcloned into pcDNA3.0) was kindly gift
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BRCC is the catalytic subunit
2020-04-08
BRCC36 is the catalytic subunit responsible for the majority of K63-Ub-specific DUB activity in the cytoplasm and in the nucleus as part of two distinct macromolecular assemblies characterized by the presence of either of the MPN– pseudo DUB proteins KIAA0157 or Abraxas (Cooper et al., 2009, Dong et
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