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The in vivo IC M in the adipose tissue
2019-07-03
The in vivo IC (0.0003μM) in the adipose tissue assay is in very good agreement with the in vitro IC (0.0005μM), and it is larger than the one measured in the OLTT assay (0.00005μM) for this compound. These differences in in vivo IC between OLTT and TAG synthesis are expected as we used free CX-4945
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With a favorable spectrum of CRTh dependent
2019-07-03
With a favorable spectrum of CRTh2 dependent in vitro and in vivo efficacy demonstrated, the off-target activity of compound 18 was investigated, first against a panel of prostanoid receptors and related eicosanoid targets (Table 8), where no significant activities at 10μM concentration were found i
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br Results br Discussion GPCRs recognize
2019-07-03
Results Discussion GPCRs recognize a broad range of molecules with a vast chemical Sweroside through different mechanisms. Our understanding of the recognition of lipid mediators by GPCRs primarily comes from the structural studies of receptors for lysophospholipids and endocannabinoids inclu
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The most important cytotoxic lesion formed by the nitrogen
2019-07-03
The most important cytotoxic lesion formed by the nitrogen mustards is generally considered to be the DNA–DNA interstrand cross-link 12, 13. DNA–DNA interstrand cross-links are thought to exert their cytotoxic effects by inhibiting DNA duplex strand separation, progression of the Sitagliptin phospha
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br Experimental section br Results br Discussion In our
2019-07-03
Experimental section Results Discussion In our previous work (Rashidi et al., 2018) we isolated a novel glucarpidase whose raised Gastrodin did not cross-react with the one in clinical use. In principle, therefore, it would be possible to delay the production of antibodies in a patient by
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Several TERRA binding proteins have also been discovered esp
2019-07-03
Several TERRA-binding proteins have also been discovered, especially telomeric duplex DNA binding proteins TRF1 and TRF2, pointing to a significant role of TERRA in more general chromosome biology [14], [20], [21]. TRF2 is a key component of Shelterin that protect chromosome termini [22]. Telomeres
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br Roles of TLS polymerases outside DNA
2019-07-02
Roles of TLS polymerases outside DNA damage tolerance Preparing the ground for more DNA damage: adaptive responses through gene induction Conclusions and perspectives Although known for many decades, the relevance of TLS in genome stability is normally considered secondary to mechanisms tha
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JTP-74057 In this review we first
2019-07-02
In this review, we first introduce the in vivo metabolism profile of VD3, and the mediation of Cyp3a gene transcription by PXR and CAR in humans, mice and rats. We then focus on the species-specific VDR-dependent regulation of human (CYP3A4, CYP3A5 and CYP3A7), mouse (mainly CYP3A11 and CYP3A13), a
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In the phase I AURA trial
2019-07-02
In the phase I AURA trial, patients with EGFR activating mutations and centrally confirmed tumor and/or plasma genotyping (BEAMing) T790M result were enrolled. Among 216 patients with both plasma and tissue genotyping results, the concordance rate was 82% for d-biotin 19 deletions, 86% for L858R an
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Today many strategies have been developed to
2019-07-02
Today, many strategies have been developed to enhance CXCR-4 receptor KP372-1 on the cell surface, either by modifying the cell culture medium or by modifying the CXCR-4 gene in BMSCs to stimulate stem cell recruitment (Jiang et al., 2012, Liu et al., 2014b). For instance, the pre-conditioning of su
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In the original ELF study patients were considered eligible
2019-07-02
In the original ELF study [7], patients were considered eligible if they were due to undergo liver biopsy for the investigation of chronic liver disease, defined as abnormal biochemical liver function tests persisting for more than 6 months, ability to provide informed consent and age between 18 and
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Initially studies of GPCRs predominantly assessed
2019-07-02
Initially, studies of GPCRs predominantly assessed the signalling pathways downstream of receptors on the cell surface. There is now an understanding that GPCRs can localize to and signal from various intracellular compartments, such as the nucleus (reviewed in [40]). These intracellular pools of re
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Tibolone is also efficacious on bone in elderly women
2019-07-02
Tibolone is also efficacious on bone in elderly women and induces a clear reduction in bone turnover markers [50], [51]. Rymer et al. showed that, after 10 years of treatment with tibolone, the difference in bone mineral density compared with a placebo group was more than 12% for both lumbar spine a
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Our previous studies have shown that in a
2019-07-02
Our previous studies have shown that in a preimplantation mouse embryo the proportion of inner to outer cells (i.e. precursors of ICM and TE, respectively) is regulated by a different frequency of differentiative cell divisions at the 8- and 16-cell stages. Low number of inner blastomeres generated
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The genetic asymmetries between parental
2019-07-02
The genetic asymmetries between parental genomes are also the subject of genetic conflict theory. This concept proposes that paternally inherited imprinted genes “extract” nutrients from the mother during gestation. By contrast, maternally inherited genes counteract the effect of paternal genes (Con
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