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Tacrine amino tetrahydroacridine I Fig was the first AChEI t
2019-11-16

Tacrine (9-amino-1,2,3,4-tetrahydroacridine) (I, Fig. 1) was the first AChEI to be approved by the Food and Drug Administration (FDA) for the treatment of AD [25], [26], [27], [28]. However, despite its good AChE inhibitory activity, tacrine was far from ideal due to its low bioavailability and shor
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Although MMP might be a downstream target of Src kinase
2019-11-16

Although MMP-9 might be a downstream target of Src kinase signaling (Liu and Sharp, 2011), a direct connection has not been established. We showed for the first time that, in the collagenase-induced ICH model, Src kinase signaling regulates MMP-9 activity and mediates EP1R toxicity. Consistent with
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A number of chemical strategies have been developed to
2019-11-16

A number of chemical strategies have been developed to design activatable optical imaging probes and have been summarized in several excellent reviews 11., 12., 13., 14., 15.. Fluorogenic enzyme substrates are one of the most explored activatable probe types for enzyme detection. These probes contai
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The EGFR belongs to the ErbB
2019-11-15

The EGFR belongs to the ErbB family of receptor tyrosine kinases (RTKs), comprised of four members: EGFR (ErbB1, HER1), HER2 (ErbB2), HER3 (ErbB3) and HER4 (ErbB4) [24]. HER receptors are activated by a group of epidermal growth factor (EGF) ligands and undergo homo- or hetero-dimerization during th
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br Materials and methods br Results br Discussion CHIKV
2019-11-15

Materials and methods Results Discussion CHIKV is an important arthropod borne virus with substantial impact on global health and cause a major viral disease that requires the development of antiviral drug to combat chikungunya disease. Virus specific proteases have particularly become an a
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Taking into account that Gr dysfunction
2019-11-15

Taking into account that Gr dysfunction is involved in the molecular mechanisms underlying HPA axis disorder (Li et al., 2017b) and Gr activity has been reported to be lowered in patients with severe mood disorders (Rush et al. 1996) and in adult rats (Green et al. 2016), PFOS could alter HPA axis a
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The availabilities of serotonin and
2019-11-15

The availabilities of serotonin and dopamine are modulated by the serotonin transporter and catechol-O-methyltransferase enzyme. The serotonin transporter (5-HTT) is a key protein that reuptakes serotonin from the synaptic cleft back into synaptic boutons (Coleman et al., 2016; Talvenheimo et al., 1
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Resistance to avermectins has been associated with point
2019-11-15

Resistance to avermectins has been associated with point mutations of GluCls in C. elegans, D. melanogaster, T. urticae and P. xylostella (Dent et al., 2000; Dermauw et al., 2012; Kane et al., 2000; Kwon et al., 2010; Wang et al., 2016a, 2017). Our electrophysiological study found a 8.2-fold reducti
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prostaglandin receptor br Materials and methods br Results b
2019-11-15

Materials and methods Results Discussion We confirmed the published cDNA and protein sequence of feline CSF-1R and stably cloned the cat receptor into the Ba/F3 cell line. Activation of feline CSF-1R by recombinant human CSF-1 was previously tested by Woolford et al. [14]. Expression of onc
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The GH family includes also
2019-11-15

The GH30 family includes also xylanases which are not MeGlcA-dependent. Most of them are grouped to GH30_7 subfamily that includes XynIV from Trichoderma reesei showing exo- and endo-xylanase activity [11] and XYLD from Bispora sp. MEY-1 [12] having activity towards glucuronoxylan and arabinoxylan,
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br Conclusions and future directions
2019-11-15

Conclusions and future directions In recent years we saw major advances in our knowledge of H2A-DUB biology, with discovery of novel mammalian H2A-DUBs, better understanding of their biochemical properties, and development of several animal models to address their in vivo functions. However at pr
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A novel series of DHODH inhibitors was developed by us
2019-11-15

A novel series of DHODH inhibitors was developed by us based on a lead that was discovered during a docking procedure and medicinal chemistry exploration. The activity of the initial lead was improved by a QSAR method and yielded low nanomolar inhibitors. Introduction The most common metabolic h
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br Introduction Benzanthrone BNZ is a dye intermediate used
2019-11-15

Introduction Benzanthrone (BNZ) is a dye intermediate used in the synthesis of number of polycyclic vat and disperse dyes. It has been detected as an environmental pollutant in urban ambient air particulates, originating from furnace effluents, municipal refuge, wood and coal combustion and autom
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To elucidate the potential mechanism underlying osteosarcoma
2019-11-15

To elucidate the potential mechanism underlying osteosarcoma cell growth decrease by CDK4 inhibition, flow cytometry analysis was used to determine WAY 208466 dihydrochloride and apoptosis in human osteosarcoma cells after palbociclib treatment. The results showed that osteosarcoma cells were arres
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The collagen field undoubtedly regains attractiveness with t
2019-11-15

The collagen field undoubtedly regains attractiveness with the emergence of new concepts (cell niche, regulation of growth factor bioavailability, mechanotransduction, cell microenvironment sensing) and new tools to investigate their in vivo functions (atomic force microscopy (AFM), second harmonic
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