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br Conclusions Present work comprehensively characterizes th
2019-07-25
Conclusions Present work comprehensively characterizes the inhibitory activity of Yersinia enterocolitica against cysteine proteases. All tested strains, regardless of their bioserotype, genotype and the presence of virulence markers, synthesized the high-molecular-weight inhibitors of papain and
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In humans CYP A major
2019-07-25
In humans, CYP3A4/5, major isoforms of CYP3As in the liver, have variants that reduce the enzyme activities [33], [34]. In addition, Werk et al. recently reported the first case of a complete failure of CYP3A enzyme activity due to homozygous loss-of-function mutation of CYP3A4 combined with nonfunc
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br Results br Discussion GPCRs
2019-07-25
Results Discussion GPCRs recognize a broad range of molecules with a vast chemical D-erythro-Sphingosine (synthetic) is through different mechanisms. Our understanding of the recognition of lipid mediators by GPCRs primarily comes from the structural studies of receptors for lysophospholipids
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Building applications by selecting and integrating component
2019-07-25
Building applications by selecting and integrating components is known in software engineering as COTS-based development. Nowadays, this approach is recognized as a crucial success factor for the software industry (Ahuja, 2014). The advantages of using COTS components include minimizing the overall
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Previous work examining the link between
2019-07-25
Previous work examining the link between the COMT gene and ISV is limited and has produced contradicting results. The Val allele was linked with higher ISV of RTs following target trials in a continuous performance task (Stefanis et al., 2005) and with higher ISV of RT and P3b latencies of unfamilia
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Our study demonstrates that the duration of storage under
2019-07-25
Our study demonstrates that the duration of storage under the conditions analysed did not have a major effect on the recovery efficiency for any of the swabs (Fig. 1). However, up to 4-fold differences in the recovery efficiencies were observed between the different swabs tested (Fig. 2). Using the
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br Materials and methods br Results br Discussion
2019-07-25
Materials and methods Results Discussion In this study, the N&B analysis showed new evidence regarding the proportion and the oligomerization state of the AT1 and the ETA receptors near or on the plasma membrane. Althought, preliminary studies suggest that the AT1 and the ETA receptors occu
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FGF ERK signaling has been implicated in
2019-07-25
FGF/ERK signaling has been implicated in epithelial-mesenchymal interactions in a wide range of tissues (Huh et al., 2015, Klein et al., 2006, Rice et al., 2004, Zhang et al., 2006, El Ramy et al., 2005, Volckaert and Langhe, 2015). During embryonic organogenesis and in adult organs, we often observ
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Acknowledgments br Introduction Steroidogenesis the process
2019-07-25
Acknowledgments Introduction Steroidogenesis, the process of testosterone synthesis, occurs in the adrenal cortex, testis and ovary, and it is controlled by luteinizing hormone (LH), which is synthesized and secreted from the pituitary (Hanukoglu, 1992, Payne and Youngblood, 1995). In the testis
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Here we describe a novel series of arylazoderivatives develo
2019-07-24
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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br Results br Discussion br
2019-07-24
Results Discussion Experimental Procedures Acknowledgments In the preceding paper, we reported 3-amido-4-anilinoquinolines as highly selective inhibitors of CSF-1R kinase, along with our initial efforts to optimize the series. Examples from the 6,7-dimethoxyquinoline series were very p
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Two are the sigma receptors identified
2019-07-24
Two are the sigma receptors identified to date: the non-opioid receptor, σ1R, and σ2R, whose identity with the Progesterone Receptor Membrane Component 1 (PGRMC-1) protein is in doubt (Chu et al., 2015). Despite endogenous ligands have not been yet identified, drugs of abuse may interact with these
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Herein the interactions of etamicastat nepicastat and zamica
2019-07-24
Herein, the interactions of etamicastat, nepicastat and zamicastat with P-gp and BCRP were evaluated. Although recent investigations have been performed to assess the involvement of P-gp in the gsk-3 exposure of nepicastat and etamicastat (Loureiro et al., 2015), the contribution of BCRP remains un
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Disodium (R)-2-Hydroxyglutarate where We recently employed a
2019-07-24
We recently employed a functional drug screening approach to identify mithramycin as an inhibitor of EWS–FLI1. In our study, we employed a stepwise approach involving a luciferase primary screen and a novel multiplex PCR screen to evaluate over 50,000 compounds to identify mithramycin as an inhibito
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br Materials and methods br Results br
2019-07-24
Materials and methods Results Discussion GOS potently inhibited SRD5A1 in COS-1 cells (Fig. 4A) and rat Leydig cells (Fig. 4B), possibly attenuating testosterone activation into DHT. It has been reported that gossypol inhibited human SRD5A1 with IC50 of 7 × 10−6 M [28]. Interestingly, gossy
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