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Thyroid Hormone Receptor Antagonist (1-850) br Results and d
2020-03-07
Results and discussion Conclusions In conclusion, we have developed rational strategies that allowed us to successfully identify a series of novel analogs structurally related to to modulate the activity of estrogen-related receptors (ERRγ and ERRβ), which are constitutively active. All of th
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Given the molecular pharmacology and in vitro metabolism dat
2020-03-07
Given the molecular pharmacology and in vitro metabolism data, we proceeded to evaluate the in vivo pharmacokinetics of . Mice (=3) were subsequently administered a subcutaneous dose (5mg/kg) with intermittent plasma collections to measure systemic levels of (). Compound achieved a maximum plasma
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To assess whether the described cooperation between the
2020-03-07
To assess whether the described cooperation between the EGFR and FGFR receptors was relevant at the clinical level, we determined the effect on progression-free survival of FGFR1 expression in patients with adenocarcinoma who were receiving erlotinib or gefitinib. As we had observed EGFR-FGFR1 coope
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The HEV vaccine developed based on
2020-03-07
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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amatoxin mg Hedamycin isolated from Streptomyces griseoruber
2020-03-07
Hedamycin, isolated from Streptomyces griseoruber, belongs to the highly cytotoxic pluramycin class of amatoxin mg (Figure 3(c)). It consists of a planar anthrapyrantrione chromophore attached to two amino sugar rings at one end and a bisepoxide-containing side-chain at the other end (Figure 3(c)).
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AS-703026 An increasing body of evidence demonstrates that M
2020-03-07
An increasing body of evidence demonstrates that MXC can cause neurobehavioral and neuropathological alterations [7]. In the brain, there are several steroidogenic enzymes, which are responsible for neurosteroid production. Neurosteroids are subsets of steroids that rapidly change neuronal excitabil
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br Results br Discussion Prostate cancer dissemination
2020-03-07
Results Discussion Prostate cancer dissemination and skeletal metastases represent major therapeutic challenges. Once the skeletal metastasis occurs, the incurable patient could just be symptomatically treated to alleviate the pain. Therefore it is of great necessity to disclose the molecular
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CysLTs trigger contractile and inflammatory processes
2020-03-07
CysLTs trigger contractile and inflammatory processes through the specific interaction with cell surface receptors belonging to the rhodopsin family of the G protein-coupled receptor (GPCR) genes. Until now, two receptor subtypes have been cloned, namely CysLT1 and CysLT2[8]. In particular, when the
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Crystal structures of various CRM complexes have provided in
2020-03-07
Crystal structures of various CRM1 complexes have provided insight into molecular details of the interactions between CRM1 and its interaction partners during the transport cycle. CRM1 cooperatively binds RanGTP and cargo in the nucleus (Paraskeva et al., 1999). In this ternary complex, RanGTP is lo
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Similarly LTD concentration dependently enhanced AQP express
2020-03-06
Similarly, LTD4 concentration-dependently enhanced AQP4 expression in astrocytes (Fig. 3). The LTD4-enhanced AQP4 expression was not affected by pranlukast but inhibited by Bay u9773, a non-selective CysLT1/CysLT2 receptor antagonist [33]. Because no selective CysLT2 receptor antagonists are current
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br Experimental procedures br Introduction Perfluorooctane s
2020-03-06
Experimental procedures Introduction Perfluorooctane sulfonate (PFOS) is an anthropogenic compound with high thermal, chemical and biological stability, which makes it a perfect ingredient for many industrial applications (Kissa, 2001). Nevertheless, these characteristics also mean that PFOS i
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Endothelial dysfunction has been associated with
2020-03-06
Endothelial dysfunction has been associated with most of the established cardiovascular risk factors, such as hypercholesterolemia, hypertension, smoking, diabetes mellitus, a positive history of premature CAD and elevated GFP Quantitation Kit homocysteine 4, 26, 27. Endothelial dysfunction is pres
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br Acknowledgements We would like
2020-03-06
Acknowledgements We would like to thank Dr Ron Mason (NIEHS, Research Triangle Park, NC) for helpful discussion regarding the analysis of CCl4 metabolism, to Dr Karla Thrall and Dr Rick Corley (Battelle) for helpful discussions regarding study design and data interpretation, and to Jim Merdink an
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The importance of EBI for B
2020-03-06
The importance of EBI2 for B cell function was first suggested by the dramatic upregulation of this receptor in EBV-transformed nitric oxide synthase inhibitor and further inferred from its regulation in activated and GC B cells (Birkenbach et al., 1993, Glynne et al., 2000, Shaffer et al., 2000).
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Lymphocyte mobility and homing is
2020-03-06
Lymphocyte mobility and homing is modulated by the chemoattractant receptor subfamily of G protein-coupled receptors (GPCRs) (Campbell et al., 2003, Rot and von Andrian, 2004). B cell migration and position are controlled to a large extent by the lymphoid chemokines CXCL13, CXCL12, CCL19, and CCL21
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