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br Introduction The cervix is
2021-03-10
Introduction The hcv protease inhibitor is a poorly studied component of the mare’s reproductive tract. It has anatomical and biological defense mechanisms involved in the delicate balance between immunological tolerance, sperm transport and biological defense. Anatomically, the cervix is compose
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To develop novel EPAC inhibitors Zhou and co
2021-03-10
To develop novel EPAC inhibitors, Zhou and co-workers optimized the HTS hit as the chemical lead. After modifications of the substituents on the phenyl ring or C6-position of compound , compound () was identified to be the more potent compound in this series with an IC value of 4.0µM (EPAC2). Dockin
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Our observation that nuclear but not cytoplasmic EP expressi
2021-03-10
Our observation that nuclear, but not cytoplasmic EP4 expression is associated with different outcomes is interesting. In breast cancer, using the same methods, we did not detect EP4 in the nucleus of malignant dna alkylating agents whereas cytoplasmic EP4 was commonly observed [13]. While G protein
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Kinetic isotope effects KIEs inform on bond vibrational chan
2021-03-10
Kinetic isotope effects (KIEs) inform on bond vibrational changes between the ground state (GS) and TS of a chemical reaction and remain one of the most powerful experimental techniques for interrogating TS structure. KIEs on enzyme reactions measured by the internal Heme Colorimetric Assay Kit aus
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Introduction Pain is frequently the first clinical symptom o
2021-03-10
Introduction Pain is frequently the first clinical symptom of head and neck carcinoma. Indeed, pain is the initial reason leading ∼70% of cancer patients to seek professional assistance (Lam & Schmidt, 2011; Rettig & D’Souza, 2015; Schmidt, 2014). Clinically, cancer-induced facial pain can be evoke
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br Oxysterols as Key Players in Metabolic Syndrome
2021-03-10
Oxysterols as Key Players in Metabolic Syndrome? Obesity and sedentary lifestyle are on the rise and pose serious threats to people's health and wellbeing. Obesity is often associated with other pathologies and is one of the criteria included in the definition of metabolic syndrome (MetS) (see Gl
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br Materials and methods br Results br Discussion We
2021-03-10
Materials and methods Results Discussion We recently detected phosphorylation of tyrosine Y102 in BPV-1 E2 and reported that FGFR3 binds to E2 and limits E1 dependent viral DNA replication (Culleton et al., 2017, Xie et al., 2017). In the current study, we addressed the potential role of ot
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br Materials and methods br Results br Discussion
2021-03-09
Materials and methods Results Discussion UPP components including the proteasome, E1s, E2s, E3s and DUBs may become one the most important Imeglimin hydrochloride of therapeutic targets for the pharmaceutical industry in the near future and supersede those which are involved in the phospho
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Herein the interactions of etamicastat nepicastat and
2021-03-09
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 meclozine exposure of nepicastat and etamicastat (Loureiro et al., 2015), the contribution of BCRP remain
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Methylation of histone tails is important in
2021-03-09
Methylation of histone tails is important in regulating salubrinal structure and transcription. Methylation occurs at arginine and at mono-, di- or tri-methylated lysine residues. The reversibility of histone methylation was recently revealed by the identification of two histone demethylases, LSD1
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Cyclin D inhibits the transcriptional
2021-03-09
Cyclin D1 inhibits the transcriptional activity of the transcription factors myogenin and MEF2 [39,40]. In addition, myogenin activates MEF2 expression, which feeds back to amplify the myogenin promoter [38]. In this study, DGKδ suppression, in addition to the increase of cyclin D1, inhibited myogen
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br Acknowledgments We thank Jon Clardy Juan Manuel Dom
2021-03-09
Acknowledgments We thank Jon Clardy, Juan Manuel Domínguez, José Francisco García Bustos, and the GlaxoSmithKline (GSK) Plasmodium falciparum dihydroorotate dehydrogenase project team for their contributions, helpful advice, and discussions. Introduction Dihydroorotate dehydrogenase (DHODH) i
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The present study found a significant negative correlation b
2021-03-09
The present study found a significant negative correlation between miR-152-3p and CDK8 expression in human HCC tissues. We also validated that CDK8 was a direct target of miR-152-3p, and overexpression of miR-152-3p inhibited proliferation and induced apoptosis in HCC Trigonelline sale by suppressin
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Nucleophosmin NPM which also plays
2021-03-09
Nucleophosmin (NPM1), which also plays a role on the nuclear export of ribosomal proteins and subunits (Maggi et al., 2008), is also a relevant MYC target, presumably through an interaction with CRM1. Conversely, it has been recently reported that specific SINE compounds reduce the levels of MYC in
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CRF binds to CRF and CRF receptor subtypes triggering downst
2021-03-09
CRF binds to CRF1 and CRF2 receptor subtypes, triggering downstream cascades and leading to stimulatory G protein (GsP) activation. Once activated, GsP undergoes a structural change provoking the separation of the subunits Gα and Gβγ. The Gα subunit induces the production of the second messenger cAM
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