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While previously reported optimizations on compound focused
2019-10-12
While previously reported optimizations on aldehyde dehydrogenase inhibitor focused on the phenyl ring A () and substituents on isoxazole ring, other alternatives to replace isoxazole ring were never explored. Herein, we propose to replace the isoxazole with its bioisosteric substituted phenyl rin
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We further analyzed the transcriptional mechanisms
2019-10-12
We further analyzed the transcriptional mechanisms underlying the synergistic action of IL-23 and PGE2 and found that this action is mediated by not only STAT3 but also CREB1 and NF-κB. Involvement of CREB1 is analogous to that in the PGE2-EP2/EP4–mediated Il12rb2 induction during TH1 cell different
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Regardless of its effect on
2019-10-12
Regardless of its effect on EBV infection, the chemokine system has been found to be regulated in both nasopharyngeal cancer and Hodgkin lymphoma. As such, Hodgkin and Reed–Sternberg (HRS) cells from Hodgkin lymphoma and nasopharyngeal carcinoma cells have been shown to express CXCL8 and CCL17. Furt
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In another study Nutlin a mediated p
2019-10-12
In another study, Nutlin-3a-mediated p53 activation induced strong negative impact on NF-κB signaling in LPS-stimulated neutrophils and macrophages [34]. Nutlin-3a limited cellular immune response to LPS, partly by attenuating DNA binding activity of NF-κB and impairing transcription of its target c
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Pyridostatin br Results br Discussion In this
2019-10-12
Results Discussion In this paper we present insights into the observed specificities of inhibitors targeting the ubiquitin-activating and related E1 Pyridostatin via crystal structures of the specific NEDD8-E1 inhibitor MLN4924, the dual NEDD8/Ub E1 inhibitor ABPA3, and the selective Ub-E1 in
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We have compared the potency
2019-10-12
We have compared the potency of a series of DNA-directed alkylating agents, including N-mustard-acridine, N-mustard-quinoline, and N-mustard-quinazoline conjugates previously synthesized in our laboratory [7], [13], and currently used drugs (oxaliplatin, cisplatin, or 5-FU) for the treatment of CRC
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br Conclusions This report describes the discovery of
2019-10-12
Conclusions This report describes the discovery of a new class of host-directed antiviral agents characterized by a 1-aryl-4,6-diamino-1,2-dihydrotriazine scaffold, responsible for a host (human) DHFR inhibition mechanism. Host-targeting antivirals represent an alternative and emerging strategy t
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Fujimoto et al pointed out
2019-10-11
Fujimoto et al. pointed out that RPN2 knockout alleviated the resistance of GC bud (MKN74 and KATO III) to docetaxel and DDP [23]. Yuan et al. demonstrated that the depletion of RPN2 resulted in the reduction in resistance of GC cells to drugs such as irinotecan, docetaxel, doxorubicin, oxaliplatin
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ERK and p MAPK signaling pathways play critical role
2019-10-11
ERK and p38 MAPK signaling pathways play critical role in genesis and metastasis of melanoma (Tang et al., 2018). >50% of melanoma 6780 (Abildgaard and Guldberg, 2015) show abnormal activity of BRAF-RAS-RAF to activate MEK signal that drives the growth-promoting extracellular signal-regulated kinase
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This pre GC B cell differentiation deficiency caused
2019-10-11
This pre-GC B cell differentiation deficiency caused by RD2 loss of function was explained at least in part by the finding that the BCL6 RD2 domain is required to repress expression of the key migration factors GRP183 and S1PR1. Downregulation of GRP183 is critically important for B cell migration i
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MPI-0479605 mass br Introduction Acinetobacter baumannii is
2019-10-11
Introduction Acinetobacter baumannii is a gram-negative opportunistic pathogen that causes nosocomial infections including pneumonia and bloodstream infections which is associated with an increased mortality and multi-drug resistance [[1], [2], [3]]. A. baumannii was rated as one of the critical
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γ-Linolenic Acid methyl ester br Compliance with ethical sta
2019-10-11
Compliance with ethical standards This work was conducted in compliance with ethical standards. Conflict of interest Funding The work was funded by extra mural research grant (EMR/2016/005135) from Science and Engineering Research Board, Government of India. Acknowledgements Introduc
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CXC chemokines are primarily expressed
2019-10-11
CXC chemokines are primarily expressed in immune organs and the central nervous system: the mouse thymus and spleen (Heesen et al., 1996), chicken bursa (Liang et al., 2001), primate (Macaca mulatta) BVT 2733 (Federsppiel et al., 1993) and cattle locus coeruleus, cerebellum and pons (Rimland et al.,
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IL is not expressed in tissues constitutively
2019-10-11
IL-8 is not expressed in tissues constitutively because of its strong chemoattractant, proinflammatory, and angiogenic activities. Rather, it is an inducible factor, produced by a variety of cell types, including leukocytes, fibroblasts, endothelial and epithelial cells, in response to proinflammat
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The significant CRF increase in the DS and
2019-10-11
The significant CRF increase in the DS and the overall changes in the CRF system observed in the VM and DS during the development of sensitization suggest that this neuropeptide (and possibly urocortin) contributes to the specific molecular alterations occurring in the mesolimbic pathway that suppor
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