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Additional derivatives were synthesised using a modified app
2021-02-08
Additional derivatives were synthesised using a modified approach (). Commercially available 4-bromo-2-methoxyaniline () was converted into the boronic ester , followed by a Suzuki–Miyaura cross-coupling with chromenone triflate to afford the corresponding arylamine . Acylation of with chloroacetyl
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The importance of G S phase progression to the formation
2021-02-07
The importance of G1–S phase progression to the formation of malignant tumors has been highlighted by the high incidence of aberrations in the genes involved in this progression in a wide variety of tumors. p27Kip1 is a member of the Cip/Kip family of cyclin-dependent kinase inhibitors (CKI). Its ro
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Since we found that the
2021-02-07
Since we found that the pharmacokinetic properties of KPT-185 were unsuitable when given subcutaneously or orally, it is not a candidate for in vivo therapy for NHL. However, the pharmacokinetic properties of KPT-276, a CRM1-inhibiting SINE structurally related to and with functional activities simi
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Recently several Pt IV complexes as
2021-02-07
Recently, several Pt(IV) complexes as prodrugs have been designed and studied to enhance anti-tumor efficacy of traditional Pt(II) drugs, improving their cellular uptake and blood-circulation time [26], [27], [28], [29]. Compared with their Pt(II) counterparts, six-coordinated Pt(IV) complexes with
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br Conclusions In conclusion the substrates c e all produced
2021-02-07
Conclusions In conclusion, the substrates 18c–18e all produced highly fluorescent colonies with the panel of Gram-negative microorganisms. This has been attributed to the combination of two synergistic effects; the wide distribution of l-alanylaminopeptidase in Gram-negative microorganisms and th
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With respect to bone metabolism and ossification related gen
2021-02-07
With respect to ‘bone metabolism and ossification’-related genes, treatment of SaOS-2 osteoblast-like leukotriene receptor antagonists with MS-10 up-regulated IGFBP-4, TG2, and SOST. Up-regulation of IGFBP-4 in SaOS-2 cells inhibits DNA and protein synthesis induced by IGF-1 (Kudo et al., 1995, Kud
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br Anti inflammatory effects of MTX In addition to
2021-02-07
Anti-inflammatory effects of MTX In addition to cytotoxic and cytostatic effects, the anti-inflammatory activity of MTX was also described by several studies. Inhibition of ATIC by MTX has been found to result in the accumulation of 5-aminoimidazole-4-carboxamide-1-β-d-ribofuranosyl 5′-monophosph
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Dgat mice however had less adipose
2021-02-07
Dgat−/− mice, however, had less adipose tissue, as reflected by lower total fat pad weights and body triglyceride content. Because of these findings, we hypothesized that, although Dgat−/− mice could make triglycerides through non-DGAT pathway(s), their triglyceride synthesis capacity might not be e
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As a basis for the DDR substrate
2021-02-07
As a basis for the DDR1 substrate identification approach detailed below, we first set out to perform 2D-gel electrophoresis with lysates isolated from collagen-stimulated human breast cancer MDA-MB-231 GDC-0994 australia overexpressing DDR1 (b-isoform). This allowed us to determine whether DDR1 is
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Some studies have demonstrated that BMSCs can provide severa
2021-02-05
Some studies have demonstrated that BMSCs can provide several trophic and growth factors that play important roles in cell survival, angiogenesis, and BMSC differentiation, but not cell replacement (Peled et al., 1999, Shen et al., 2007, Ji et al., 2004). This paracrine effect of BMSCs is a potentia
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Immunofluorescence Cells were fixed with paraformaldehyde PF
2021-02-05
Immunofluorescence. Cells were fixed with 4% paraformaldehyde (PFA) in PBS and extracted by 0.5% Triton X-100-PBS, or fixed in cold methanol. The cells were immunostained with mouse monoclonal yutopar against α-tubulin (Sigma), γ-tubulin (Sigma), Ran (Upstate), rabbit polyclonal antibodies against
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Data presented herein suggest that
2021-02-05
Data presented herein suggest that competent IL-18BP production in epithelial PYR-41 is implemented by epigenetic means based on demethylation of a single CpG site at −45 bp/−44 bp (CpG2) of the human IL18BP promoter. In contrast, retarded IL-18BP production in monocytic cells associates with CpG2
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br Conflict of interest br Acknowledgements This work
2021-02-05
Conflict of interest Acknowledgements This work was supported in part by JSPS KAKENHI Grant Number 26292031. We thank Nissan Chemical Industries, Ltd. for the gift of the sample of fluralaner. Introduction As one of the most common cancers in southern China and southeast Asia, nasopharynge
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Interestingly increased level of both circulating ET and uri
2021-02-05
Interestingly, increased level of both circulating ET-1 and urinary excretion of ET-1 have been observed in patients treated with nephrotoxic immunosuppressive agents as cyclosporine A and tacrolimus (Slowinski et al., 2002). Other nephrotoxic agents, such as cisplatin, also increase urinary excreti
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In contrast irinotecan has shown
2021-02-05
In contrast, irinotecan has shown much less myelosuppression and may be more active in Ewing sarcoma both alone and in combination with temozolamide. One phase II study of 13 heavily pretreated Ewing sarcoma patients demonstrated a response rate of 38% including 2 complete responses (Bisogno et al.,
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