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The underlying mechanisms of how progesterone prolongs pregn
2019-08-13

The underlying mechanisms of how progesterone prolongs pregnancy, although not completely understood, are thought to have to do with reduction in uterine contractility, antimicrobial protein up-regulation, immunosuppression, and inflammatory inhibition. Specific to preterm PROM, progesterone has bee
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br Effects of estrogens on bone Estrogens
2019-08-13

Effects of estrogens on bone Estrogens play an important role in bone remodeling, as demonstrated by studies in mice in which the ER genes were deleted [21], [22]. ERβ compensates for the (±)-CPSI 1306 of ERα, and vice versa, but when both ERs are deleted a profound decrease in trabecular bone v
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PGE exerts its functions by
2019-08-13

PGE2 exerts its functions by binding to different receptors. Four different subtypes of PGE2 receptors are found in mammals and are designated as EP1-4. These are G-protein coupled receptors that belong to a family of seven rhodopsin-like transmembrane spanning receptors. They are structurally diffe
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A range of inhibitors were therefore synthesized containing
2019-08-13

A range of inhibitors were therefore synthesized containing either carboxylic calcitonin receptor or ester functionality at the ‘tail’ group as well as variations in the ‘head.’ These were assayed in vitro using the DCIP assay for binding affinity against and human DHODH at 50μM, respectively ().
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Some pyrimidine analogs are substrate based
2019-08-13

Some pyrimidine analogs are substrate-based inhibitors that bind to the dihydroorotate binding site, but most reported inhibitors of DHODH bind to the site occupied by the ubiquinone co-factor., , , , , , , , , , , , , , , , , X-ray crystallographic studies of inhibitor complexes with DHODH and DHO
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For example nM MTX markedly stimulates
2019-08-13

For example, 200nM MTX markedly stimulates the differentiation of the monocytic U937 Piceatannol [39], but only 10nM MTX is sufficient for the inhibition of clonogenicity in the ALL and APL cell lines [22]. Furthermore, an even lower concentration of MTX (2nM) selectively induces the expression of
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sb chemical The synthetic route of R
2019-08-13

The synthetic route of R-changed derivatives is shown in . Compounds – were prepared from commercially available 4-nitro-1-indazole (). After same two steps with , the N-substituted indazole of was produced using the Suzuki reaction in a good yield (85%). Reduction of was performed using Pd/C, and
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Predictions of enzyme topology for
2019-08-12

Predictions of enzyme topology for DGAT2 are more difficult since the DGAT2 polypeptide sequences are more diverse across species than those of DGAT1. The length and function of the hydrophilic N-terminus preceding the first hydrophobic segment varies with species – for example, segments in fungi ar
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br MCADD review br Funding None br Introduction
2019-08-12

MCADD review Funding None. Introduction Bacteroides species are obligate anaerobes, Gram-negative, and non-spore-forming bacteria and 21 species of this genus are found particularly in the oral cavity and gastrointestinal tract in vertebrates [1,2]. B. fragilis is the most common phospholi
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eflornithine hydrochloride Here we examined whether Intracel
2019-08-12

Here, we examined whether Intracellular ER may mediate Cd-induced ovarian cancer proliferation. To determine this relationship, we used ICI 182,780 as a general inhibitor of ERα and ERβ. The results suggest a metalloestrogenic effect of Cd in ovarian cancer cell lines. Inconsistency with our results
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We continued to investigate the contribution of
2019-08-12

We continued to investigate the contribution of the EP1 prostanoid receptors to nociceptive sensitization by utilizing its natural ligand PGE and tested the effect of local subcutaneous injection of PGE (5nmol in 5μl) into one hindpaw on mechanical and heat pain thresholds. Wild-type mice displayed
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In this study we investigated whether the Ednra signaling
2019-08-12

In this study, we investigated whether the Ednra signaling is involved in Hoxa9/Meis1-mediated leukemogenesis. We found an upregulation of Ednra in leukemic murine bone marrow (BM) MC1568 overexpressing Hoxa9 and Meis1 compared to cells overexpressing Hoxa9 alone. We showed that overexpression of Ed
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Intriguingly one E residue may
2019-08-12

Intriguingly, one E2 residue may serve as a molecular ‘gate’ to allow the C-terminus of ubiquitin to access the closed E2~Ub conformations favorable for ubiquitin transfer. This residue, Asp87 in UbcH5 family members, resides on one side of the opening that leads to the active site Cys (Fig. 4D). In
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br Conformational Activation of APC C Enables Binding to the
2019-08-12

Conformational Activation of APC/C Enables Binding to the Coactivator CDC20 APC/C comes to life by binding a coactivator. This is controlled in part by phosphorylation and APC/C conformational changes that expose the STA9090 calculator for the C box and IR tail of the coactivator. In interphase
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Covalent inhibitors are well suited
2019-08-12

Covalent inhibitors are well suited for targeting the E1 selective serotonin reuptake inhibitor of Ubl modifications. Because the E1 enzymes in Ubl modifications, such as the SUMO E1 and Atg7, have a slow turnover rate (Boggio et al., 2004), prolonged inhibition can be achieved without requiring co
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