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Determination of relative potency EC by dose response
2021-02-25

Determination of relative potency (EC50) by dose response assays in vitro is subject to the same sources of variability as determination of affinity, since the EC50 and Hill slope of the dose response curve are highly dependent on the binding of ligand to a competing receptor that may be present, an
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br Significance Ubl post translational
2021-02-25

Significance Ubl post-translational modifications are potential targets for developing novel therapeutics for life-threatening diseases, such as c-Myc- and KRas-driven cancers that lack targeted therapy. However, only a few drugs are available to target these modifications. This lack of drugs hig
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Introduction Glucose is the major carbon source in
2021-02-25

Introduction Glucose is the major carbon source in most organisms. Cancer FTY720 Phosphate in particular require a steady source of energy to maintain growth and proliferation, and preferentially use glycolysis for their energy supply even under aerobic conditions. Glucose uptake in mammals is mai
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Following DEX exposure the levels of CYP A protein
2021-02-25

Following DEX exposure, the levels of CYP1A1 protein and activity remained unchanged, as seen in our previous in vitro study (Burkina et al., 2013). Dasmahapatra and Lee (1993) reported that 3.9μgL−1 DEX, similar to our highest tested concentration, did not change CYP1A1 protein content. An increase
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br Methods An ongoing prospective study at the
2021-02-25

Methods An ongoing prospective study at the Princess Margaret Cancer Centre is enrolling consenting patients with stage IV EGFRm NSCLC for longitudinal blood collection. Patients may enrol at any point in their treatment. In this study, we performed a cross-sectional analysis of 72 patient liquid
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br The ubiquitin proteasome system The ubiquitin
2021-02-25

The ubiquitin proteasome system The ubiquitin proteasome system (UPS) plays a significant role in the regulation of cell growth and survival, in addition to maintaining cellular homeostasis. By means of the UPS, fda approved can precisely and temporally degrade approximately 80% of the entire pr
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One of the critical functions
2021-02-25

One of the critical functions of the product of the AR gene is to activate the expression of target genes. This transactivation activity resides in the N-terminal domain of the protein encoded in exon 1, which contains polymorphic repeats. These trinucleotide repeats, (CAG) and (GGC), encode polyglu
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br Four active site residues of KSTD
2021-02-24

Four active site residues of Δ1-KSTD1 are fully conserved in Δ1-KSTDs from different species (Supplementary Figure S2). These residues are Tyr-119, Tyr-487, and Gly-491 from the FAD-binding domain and Tyr-318 from the catalytic domain. The structure of the Δ1-KSTD1•ADD complex revealed that the hy
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br Acknowledgements This work was
2021-02-24

Acknowledgements This work was supported by grants from Agence Nationale de la Recherche (ANR CAPHE) and from Ligue contre le Cancer. We acknowledge the continuous support of CNRS and the University of Strasbourg. We thank the technical assistance of the “Plateforme de Chimie Intégrative de Stras
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Dexamethasone DEX a potent synthetic
2021-02-24

Dexamethasone (DEX), a potent synthetic glucocorticoid drug, is effective for treatment of a range of inflammatory and autoimmune conditions as well as the reduction of side effects associated with chemotherapy. On the Czech Republic pharmaceutical market, DEX is incorporated into eighteen drugs use
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Nucleocytoplasmic transport systems play a
2021-02-24

Nucleocytoplasmic transport systems play a critical role in intracellular localization and regulation of proteins in each cell. This balance is quite important and is typically uncontrolled in cancer cells. Specific localization of tumor suppressor and oncoproteins is quite important because any abn
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While several C terminal peptides have been
2021-02-24

While several C-terminal peptides have been reported to have modest (astressin) or substantial (astressin2-B, antisauvagine-30) subtype selectivity for the CRF2 receptor (), [125I]YP20 is the first reported small analog of the C-terminus of CRF exhibiting subtype selectivity for the CRF1 receptor vs
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Other mutations in the SYNE region exons have been
2021-02-24

Other mutations in the SYNE1 3′ region (exons 81–85) have been implicated in an upper motor neuron disease, ARCA1 (Gros-Louis et al., 2007). The disease is characterized by progressive movement, coordination, and balance problems caused by disrupted Purkinje cell function and their impaired signalin
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Pahlavanzadeh and Fakouri Baygi employed PC SAFT EoS to pred
2021-02-24

Pahlavanzadeh and Fakouri-Baygi [6] employed PC-SAFT EoS to predict the Cefepime Dihydrochloride Monohydrate of carbon dioxide by aqueous MEA solutions. They used the ideal form of Smith–Missen algorithm to calculate liquid phase concentrations. The results illustrate acceptable accuracies so that
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Two nutrient sensing pathways the cAMP protein kinase A PKA
2021-02-24

Two nutrient-sensing pathways, the cAMP-protein kinase A (PKA) pathway and the target of rapamycin complex 1 (TORC1) pathway, are implicated in Msn2/4 regulation. Under non-stress conditions, Msn2 localizes in the cytoplasm and is inactivated by both PKA-dependent phosphorylation of the nuclear loca
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