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To develop antagonists selective for the mouse EP
2021-03-16
To develop antagonists selective for the mouse EP1 receptor, we started with compound (), synthesized as previously described (). Diethyl dipicolinic PNU-120596 () was reduced with NaBH to . Parikh–Doering oxidation of with sulfur trioxide–pyridine complex and DMSO produced the unstable aldehyde
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Our approach including the characterization of
2021-03-16
Our approach, including the characterization of histone modifications in scarce NK subsets, allowed us to identify super-enhancers, which associate with genes endowing a given cell type with its unique identity (Hnisz et al., 2013). Especially intriguing were SEs with distinct activities in NK subse
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br DUBs in regulation of critical steps in tumor metastasis
2021-03-16
DUBs in regulation of critical steps in tumor metastasis Tumor metastasis comprises a complicated series of biological processes in terms of the invasion-metastasis cascade that requires cancer Decanoyl-RVKR-CMK to (1) migrate and invade from the origin sites through the extracellular matrix (EC
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In the present work we have investigated the
2021-03-16
In the present work, we have investigated the reactivity of N-aryl-N′-hydroxyguanidines 1a–d (see Scheme 1 for structures) with the water-soluble Cu(II) complex 8. Using EPR and UV–Visible spectroscopy, we have shown that the studied N-aryl-N′-hydroxyguanidines 1a–d can bind and transfer electrons t
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Our data also showed that D
2021-03-16
Our data also showed that D2 dopamine receptor was down-regulated in the hippocampus, NAc and striatum of F1-MEP animals, which was only significant in the hippocampus. Both agonists and antagonists of D2 dopamine receptor are able to decrease heroin self-administration (Hemby et al., 1996; Rowlett
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ASC was reported as a potent antiviral and antifungal
2021-03-16
ASC was reported as a potent antiviral and antifungal agent, and its derivatives could modulate a variety of physiological activities, such as anti-tumor, anti-metastatic, and anti-diabetic activities in animals. Mie Tsuruga et al. found that 4-o-methylascochlorin had immunosuppressive activity, but
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The p controls transcription of several genes that affect th
2021-03-16
The p53 controls transcription of several genes that affect the release of cytochrome c in the mitochondrial apoptotic pathway [44]. In addition, p53 can induce a transcription-independent apoptosis through a direct interaction with the Bcl-2 family proteins [45]. However, the role of mitochondrial
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Introduction Psoralea corylifolia L Leguminosae
2021-03-16
Introduction Psoralea corylifolia L. (Leguminosae) is a well-known traditional Chinese medicine, and it has been widely used for the treatment of various diseases like bronchial asthma, leucopenia, vitiligo and psoriasis in East Asian countries (Zhang et al., 1990). Previous studies have reported t
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br Subjects and methods br Results br Discussion In
2021-03-16
Subjects and methods Results Discussion In the present study, we found significantly increased CSF levels of IL-4, IL-5, IL-9, IL-10, TNF-α, CXCL8/IL-8, and VEGF-A together with significantly higher detection rates of IL-6, GM-CSF, PDGF-BB and IL-1ra in IHP patients compared with OND patien
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Concanamycin A synthesis br Materials and methods br Results
2021-03-16
Materials and methods Results and discussion Conclusions Clitocypin is another member of the mycocypin family of cysteine protease inhibitors that is unique to Concanamycin A synthesis shown to exhibit strong insecticidal activity against Colorado potato beetle larvae. This effect is conce
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Cell swelling stimulates the release of certain amino acids
2021-03-15
Cell swelling stimulates the release of certain amino acids, in particular the non-protein amino GSK2801 taurine, via a pathway which has the characteristics of a channel rather than a carrier [54], [69]. Indeed, on the basis of pharmacological inhibition, it was suggested that volume-activated taur
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Famprofazone FGF ERK signaling has been
2021-03-15
FGF/ERK signaling has been implicated in epithelial-mesenchymal interactions in a wide range of tissues (Huh et al., 2015, Klein et al., 2006, Rice et al., 2004, Zhang et al., 2006, El Ramy et al., 2005, Volckaert and Langhe, 2015). During embryonic organogenesis and in adult organs, we often observ
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br Halogenases Enzymatic C H activation leading to halogenat
2021-03-15
Halogenases Enzymatic C–H activation leading to halogenation is another emerging area in biocatalysis [55,56]. Incorporation of halogen atoms during medicinal chemistry eff ;orts is a well-established practice, presenting an effective means to control the molecule’s bioactivity and physicochemical
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Therefore HNE is an attractive therapeutic target and the
2021-03-15
Therefore, HNE is an attractive therapeutic target and the design of new HNE inhibitors is a demanding field that has been extensively investigated in order to provide inhibitors with new molecular architectures, including the potent oxo-β-lactam class [14]. In the present work, a coumarin-based oxo
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Cyclosporine NEORAL Oral Solution Novartis is an immunosuppr
2021-03-15
Cyclosporine (NEORAL® Oral Solution, Novartis) is an immunosuppressant widely used in organ transplantation and many other clinical conditions [12]. It undergoes extensive hepatic and intestinal biotransformation mainly via the metabolizing enzyme, CYP3A4 [[12], [13], [14], [15]]. Considering the na
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