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Herein in consider of the high similarity
2021-10-08
Herein, in consider of the high similarity between GR HBP site and AR HBP site, we applied rational drug design strategy to develop AR/GR antagonists based on the chemical structures of antiandrogens and crystal structure of GR. The following bioassay identified Z19 as a dual AR/GR antagonist. Z19 i
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In total strains with relatively
2021-10-07
In total, 5 strains with relatively rapid acid-producing ability (MA14, 15M2, DQHXNQ38–12, 5G2, and 6G5) were selected for further analysis. Compared with the strains ATCC19435, ZN8, and D-XJ4–12, which were used as controls, these 5 strains exhibited significantly different growth and titratable ac
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Compared to a large database of
2021-10-07
Compared to a large database of NSCLC samples matched for disease type, many of the frequently altered genes were similar to those seen in this series of FGFR fusion-positive samples; however, there were notable exceptions. As expected, alterations in known NSCLC drivers (KRAS and EGFR) were signifi
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br Molecular aberrations in the FGFR signaling pathway
2021-10-07
Molecular aberrations in the FGFR signaling pathway Non–small cell lung cancer Small cell lung cancer Integrated Neochlorogenic acid analysis revealed focal amplification of FGFR1 in 6% of SCLC cases. In another study with PD173074, Pardo et al. used two human SCLC xenograft models, H-510 a
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Reducing the molecular weight According to a thorough analys
2021-10-07
Reducing the molecular weight: According to a thorough analysis of a large, structurally diverse Caco-2 permeability dataset using a variety of statistical techniques by AstraZeneca researchers, logD and molecular weight are suggested the most important factors in determining the permeability of dru
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br Conclusions Histone acetylation deacetylation
2021-10-07
Conclusions Histone acetylation/deacetylation is a major epigenetic mechanism implicated in the regulation of transcription and various biological processes such as development and gametogenesis from plants to vertebrates. However, despite being well characterized in zebrafish, acetyltransferase
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Distribution of histamine receptors in the
2021-10-07
Distribution of histamine receptors in the intestines varies among species, but our findings are similar to those previously reported in humans and guinea pigs (Thurmond, 2010, Thurmond, 2015). H1 receptors were located mainly in the gastric mucosa, smooth muscle, and lymphoid tissue, corresponding
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aromatase inhibitors br Materials and methods br Results br
2021-10-07
Materials and methods Results Discussion Reduced glutathione is considered to be one of the important regulators of REDOX balance in the biological system. The cellular concentration of 4-HNE under physiological conditions ranges from 0.1 to 3μM and has no detrimental effect in the biologic
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br Introduction Chronic rhinosinusitis with
2021-10-07
Introduction Chronic rhinosinusitis with nasal polyps (CRSwNP), a subgroup of chronic rhinosinusitis (CRS), is a chronic inflammatory condition of the nasal and paranasal sinuses. CRSwNP is characterized by grape-like structures with dense inflammatory infiltrates, loose fibrous Disulfiram and t
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A subsequent modeling study by a different
2021-10-07
A subsequent modeling study by a different group was based on the bovine rhodopsin homology model using the 1L9H construct [38]. However, the site-directed mutagenesis data and docking suggested that the niacin-binding pocket is different to that described in the aforementioned report, but similar t
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In conclusion the present study demonstrated that peripheral
2021-10-07
In conclusion, the present study demonstrated that peripheral nerve exposure to HIV gp120 increased the expression levels of the P2Y12 receptor in DRG SGCs and enhanced mechanical and thermal hyperalgesia in rat models. Up-regulation of the P2Y12 receptor in DRG SGCs further promoted the release of
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The amino hydroxy methyl isoxazolepropionic acid AMPA
2021-10-06
The α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic Dexmedetomidine HCl receptor (AMPA) receptors are related ionotropic glutamate receptors (iGluRs) that mediate fast excitatory neurotransmission, and are also typically heteromeric ion channels, composed of GluA2 subunits in conjugation with GluA1
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Acknowledgements br Introduction Alzheimer s disease AD
2021-10-06
Acknowledgements Introduction Alzheimer's disease (AD) is a devastating neurodegenerative disorder and the leading cause of dementia. There is currently no treatment available to slow or halt disease progression. The underlying mechanisms of AD on the cell and molecular levels are still not comp
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Lenvatinib is an orally available multi targeted tyrosine ki
2021-10-04
Lenvatinib is an orally available, multi-targeted tyrosine kinase inhibitor against VEGFR1–3, FGFR1–4, PDGFRα, RET, and KIT [11,12]. In a recent phase III trial for patients with previously untreated uHCC (REFLECT study), lenvatinib showed statistical non-inferiority of overall survival compared to
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For our test subjects we used established high fat
2021-10-04
For our test subjects, we used established high fat diet–induced obese (eDIO) male mices T2DM models. The establishment of eDIO mice was accomplished with a 60% high fat diet ad libitum over a 14 week period (initiated at 6 weeks of age). Compared with regularly-dieted mice, the eDIO ones weigh sign
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