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This structure guided the variation
2019-07-12
This structure guided the variation of the compounds aiming either at enhanced interaction with CK1 or to exclude interaction with CK1 (R=Me, 15). We chose the 5-cloro substituted oxoindole as backbone as it is supposed to show enhanced metabolic stability, which is commonly used in medicinal chemis
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No orthologs could be found in our B oleracea
2019-07-11
No orthologs could be found in our B. oleracea BAC library for AtCk1/2, which could mean that it is unique to Arabidopsis, or that we failed to detect it in our library. However, the second possibility is unlikely considering that Southern blotting analysis with four restriction enzymes disclosed fr
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The intricate roles and neural
2019-07-11
The intricate roles and neural systems and mechanisms involved in the CRF1 and CRF2 mediation of spontaneous and stress-induced anxiety behavior remain to be defined. Of particular relevance are studies evaluating the behavioral actions of CRF1 and CRF2 receptors separately as well as together. For
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In addition to the ESIs
2019-07-11
In addition to the ESIs identified that target both EPAC1 and EPAC2, ESI-05 and ESI-07 were identified as compounds that selectively antagonise EPAC2, displaying almost no inhibition of EPAC1 at concentrations up to 100μM [99]. Both compounds were effective inhibitors EPAC2 GEF activity towards Rap1
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There has recently been some interest in Uba which
2019-07-11
There has recently been some interest in Uba6, which is most similar to slime mold, with BLAST identities of 59% and positives 73% in the 400–600 ADD range. The 400–600 ADD correlation of the two profiles is a striking 87%, so functional differences probably arise outside the ADD binding domain. Hu
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br DGAT protein interactions Although DGAT
2019-07-11
DGAT-protein interactions Although DGAT1 and DGAT2 are membrane proteins of the ER, the ER contains within its extensive three-dimensional network different, unique structural and functional protein domains that arise from the non-uniformity imposed on it by the intracellular structures it intera
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br Menopausal hormone therapy from the
2019-07-11
Menopausal hormone therapy, from the beginning to WHI Estrogen products have been used since the 1940s, with increasing prescription through the 1960s. First concerns appeared in the 1970s when oral treatment was linked to uterine cancer. Oral estrogens have traditionally been coupled with proges
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Fujimoto et al pointed out that RPN knockout alleviated
2019-07-11
Fujimoto et al. pointed out that RPN2 knockout alleviated the resistance of GC SB 242084 (MKN74 and KATO III) to docetaxel and DDP [23]. Yuan et al. demonstrated that the depletion of RPN2 resulted in the reduction in resistance of GC cells to drugs such as irinotecan, docetaxel, doxorubicin, oxali
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Co operation or synergy between
2019-07-11
Co-operation or synergy between PKA and Epac has been recently reported in PCCL3 thyroid cell line in which cAMP is pro-mitogenic, in C-type natriuretic peptide (1-22) (human, rat, swine) weight to VSMC [19]. Our study demonstrates for the first time that PKA and Epac also synergise to inhibit cell
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br Roles of DDR in
2019-07-11
Roles of DDR1 in epithelial cell differentiation Roles of DDR1 in cell migration, and invasion Dichotomous functions of DDR1 in disease progression Conclusions and perspectives The switch in Deoxynivalenol molecular from DDR1 to DDR2 during EMT is another important issue. The DDRs may e
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love herself There is a large interindividual difference in
2019-07-10
There is a large interindividual difference in intestinal cholesterol love herself of cholesterol that is mainly due to genetic variation [15], [19]. Single nucleotide variation (SNV) in NPC1L1 and, ABCG5 and ABCG8 key modulators of cholesterol influx and efflux into intestinal mucosal cells, respe
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ITE weight The HEV vaccine developed based
2019-07-10
The HEV vaccine, developed based on p239 particles, is of good efficacy, immunogenicity and safety, and was licensed in China in 2012. p239 (aa 368–606) and E2 (aa 394–606) share a common region of ORF2, referred to as E2s (aa 459–606), which harbors the major antigenic determinants of the HEV vacci
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The unique property of mutant IDH in producing an
2019-07-10
The unique property of mutant IDH1/2 in producing an oncometabolite that has no known physiological function makes mutant IDH enzymes as obvious potential therapeutic targets for the treatment of IDH-mutated tumors (Rohle et al., 2013, Wang et al., 2013). Clinical studies have also suggested the pr
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Next the BE obtained for the
2019-07-10
Next, the BE obtained for the different complexes were evaluated. From the BE obtained from our MD simulations, a very good binder can be differentiated from a very weak binder (−11.85 kcal/mol for MTX vs. −6.74 and −3.61 kcal/mol for compounds 14b and 15c, respectively) but ligands with similar bin
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Recent pharmacological and clinical studies suggested that
2019-07-10
Recent pharmacological and clinical studies suggested that estetrol (E4) should also be considered as an interesting candidate for MHT (Abot et al., 2014; Mawet et al., 2015). E4 is naturally produced from E2 and estriol (E3) via 15α- and 16α-hydroxylase by the human fetal liver during pregnancy and
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