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Enlarging the ligand binding pocket by reduction
2020-01-22
Enlarging the ligand-binding pocket by reduction of the size of the residue F435 switched DES to an agonist indicating that F435 is involved in mediating the antagonistic effect of DES (Fig. 7E) [13]. The conformation of the smaller side chain of L435 was either not altered by DES or was too small t
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One possible pitfall of using EPAC activators in
2020-01-22
One possible pitfall of using EPAC2 activators in the treatment of T2DM is their potential to increase glucagon levels. As discussed previously, although the ability of EPAC2 to increase glucagon expression and production is controversial, several studies show that this protein increases Gcg mRNA le
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Accordingly we prepared three compounds and as shown
2020-01-22
Accordingly, we prepared three compounds (, , and ) as shown in . Condensation of commercially available bruton\'s tyrosine kinase with glycine methyl ester gave amide . A Friedel–Crafts reaction between compound and 4-methyl valeryl chloride in the presence of aluminum chloride mainly produced
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Preliminary studies suggest that dimerization of the AT
2020-01-22
Preliminary studies suggest that dimerization of the AT1 receptor occurred during the biosynthesis in the endoplasmic reticulum before surface expression [27,40], which may explain the presenece of these gaba receptor antagonist before the addition of any ligand. Our results showed that the presenc
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Our finding that activating DDR variants are a cause
2020-01-22
Our finding that activating DDR2 variants are a cause of this disease suggested that the ABL inhibitor dasatinib, a leukemia drug that also inhibits DDR2, could be used for treatment of affected individuals.10, 11 To examine the effect of dasatinib on p.Leu610Pro- and p.Tyr740Cys-induced autophospho
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br Introduction The protein Epidermal Growth Factor Receptor
2020-01-22
Introduction The protein Epidermal Growth Factor Receptor Tyrosine Kinase (EGFR-TK) play important role in non small-cell lung carcinoma (NSCLC) and vital therapeutic progress withinin the treatment of this ailment has revamped the past ten years through the exploitation of this insight (Mok et a
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This pre GC B cell differentiation
2020-01-22
This pre-GC B cell differentiation deficiency caused by RD2 loss of function was explained at least in part by the finding that the BCL6 RD2 domain is required to repress expression of the key migration factors GRP183 and S1PR1. Downregulation of GRP183 is critically important for B cell migration i
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E protein expressed in a plasmid encoding codon optimized
2020-01-22
E1 protein expressed in a plasmid encoding codon-optimized canine oral papillomavirus (COPV) led to therapeutic immunization of COPV-infected Beagle dogs [25], [26], which was better than that achieved with plasmids encoding E2 or E7 COPV. Moreover, E1 and E2 from cottontail rabbit papillomavirus (C
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br Materials and methods br Results In
2020-01-22
Materials and methods Results In the leaves of the studied varieties, one to three nucleoli per nucleus were observed (Fig. 1a), except for the variety Bastardo were a maximum of two nucleoli per nucleus were detected. In the root-tip cells, most of the varieties presented one to three nucleo
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br DGKs inhibition and signaling Local DAG levels are strict
2020-01-22
DGKs inhibition and signaling Local DAG levels are strictly controlled by a balance between synthesis and degradation rates. Both receptor controlled PLC-mediated production and DGK-mediated degradation are classically implicated in the control of “signaling” DAG. However, this dogma is starting
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In the last and the most
2020-01-22
In the last and the most challenging part, three mixtures were selected to evaluate the reliability of the presented correlation and the CPA model. For Athabasca bitumen, Amani et al. [25] measured the experimental data at very high temperatures compared to the thermal recovery range up to 644 K (ne
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br Acknowledgments This work was funded by the EU ERDF
2020-01-22
Acknowledgments This work was funded by the EU ERDF and the Spanish Ministry of Economy and Competitiveness (MINECO) under Project TIN2013-41576-R, and the Spanish Ministry of Education, Culture and Sport (MECD) under a FPU grant (AP2010-3259), and the Andalusian Regional Government (Spain) under
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br Results and discussion br
2020-01-22
Results and discussion Conclusions In this work, we have conjugated two thermophilic enzymes (i.e., AMY and LASPO) to iron oxide NPs through different conjugation strategies obtaining efficient biocatalysts. We have demonstrated that these NP-enzyme systems can be successfully activated by an
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Imatinib STI is a first line tyrosine kinase inhibitor TKI
2020-01-22
Imatinib (STI-571) is a first-line tyrosine kinase inhibitor (TKI) targeted at breakpoint cluster region-Abelson kinase (ABL) for the treatment of chronic myeloid leukemia (CML) [26]. As a type II inhibitor, imatinib achieves significant selectivity by binding to an inactive DFG-out conformation (DF
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exendin 4 In our xenograft study Fig
2020-01-22
In our xenograft study (Fig. 7, Fig. 8), we observed that DYD acts very similarly to progesterone; the initial faster tumor growth in the PGRMC1-transfected MCF7 tumor was not significant compared with that with progesterone, in exendin 4 to the greater tumor growth observed with norethisterone. Th
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