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Recently roflumilast has been approved
2019-07-09
Recently, roflumilast has been approved as the first selective PDE4 inhibitor for the treatment of chronic obstructive pulmonary disease (COPD) [2]. Roflumilast has been suggested to target several different pathogenetic mechanisms, including inflammation, fibrotic, emphysematous and vascular remode
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Enolases are among the most abundantly expressed
2019-07-09
Enolases are among the most abundantly expressed cytosolic proteins. They are metalloenzymes that catalyze the conversion of 2-phosphoglycerate to phosphoenolpyruvate [18]. Eubacteria and archaebacteria have a single enolase gene (reviewed in [19]). Despite the lack of signal peptides or cognate pr
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br Restenosis after angioplasty remains a remarkable
2019-07-09
Restenosis after angioplasty remains a remarkable challenge, although drug-eluting stents have reduced the incidence of restenosis considerably . Vascular smooth muscle M 1145 molecular (VSMCs) play a pivotal role in the development of intimal thickening and restenosis. VSMCs proliferate and migr
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In light of the overall loss
2019-07-09
In light of the overall loss of activity and selectivity observed with this series of arylchromenone-4-ones bearing small -alkoxy substituents, we were pleased to identify a potent and relatively selective inhibitor , exhibiting IC values of 0.008μM and 0.07μM for DNA-PK and PI3Kα, respectively. The
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For the SAR optimization of the right
2019-07-09
For the SAR optimization of the right hand side, it was decided to explore the inclusion of the key carboxylic BMS 193885 what moiety present in the original DGAT-1 inhibitors from . Analogs were constructed by the synthetic routes outlined in , . In , the methylene-oxy linker was introduced by cond
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In normal cells the apoptotic stimuli
2019-07-08
In normal cells, the apoptotic stimuli lower the expression level of antiapoptotic proteins by increasing turnover rate and preventing the constant degradation of proapoptotic proteins. Thus, the dysregulation of anti-/pro-apoptotic proteins will confer the survival of cancer Escitalopram Oxalate vi
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The IV chains of mature
2019-07-08
The α3/α4/α5(IV)-chains of mature GBM are built exclusively by podocytes (not by endothelial cells) (Abrahamson et al., 2009), placing the podocytes into the focus of GBM-diseases such as Alport syndrome. Alport syndrome (AS) is caused by mutations in the COL4A3, 4 or 5 genes coding for the α3/α4/α5
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One strategy which is different
2019-07-08
One strategy which is different from the above is to isolate a similar enzyme to the one under study which will not be recognized by the antibody of the original protein. This approach will lead to prolonging an enzyme’s activity. For example, a novel variant of Carboxypeptidase G2 (CPG2), which has
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Although it is well established that estrogen and
2019-07-08
Although it is well established that estrogen and ESR1 mediate numerous reproductive processes, increasing evidence suggests that ESR2 also lays an integral role in reproduction. ESR2 is a mediator in folliculogenesis and may also act by stimulating ovulation and regulating luteinization (Su et al.,
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br Materials and methods br Results br Discussion COX mediat
2019-07-08
Materials and methods Results Discussion COX-2-mediated production of PGE2 is involved in cell growth and metastasis of many cancers. Previous studies indicated that COX-2 was overexpressed in many cancer tissues and that PGE2 increased cancer cell growth, a process that could be suppressed
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br Inhibiting APC C during Interphase
2019-07-08
Inhibiting APC/C during Interphase and prior to Anaphase Because ubiquitylation by APC/C triggers cell division, it is essential that APC/C is restrained until cells are prepared for its substrates to be degraded. In addition to regulation by phosphorylation, an additional layer of control comes
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EBI remains an orphan GPCR and the
2019-07-05
EBI2 remains an orphan GPCR and the identity and source of its ligand are yet to be described. Molecular studies of EBI2 have suggested that this receptor has constitutive activity, similar to that observed for many herpesvirus-encoded 7TM receptors (Benned-Jensen and Rosenkilde, 2008, Rosenkilde et
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br Results br Discussion Many
2019-07-05
Results Discussion Many assays in the literature for DBH require the use of catalase to protect the active site from hydrogen peroxide, which is a by-product in the initial step of the reaction. For the non-immobilized enzyme there was a visible increase in the rate with increasing amounts of
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To further explore whether it is the bisulfite conversion or
2019-07-05
To further explore whether it Methylpiperidino pyrazole weight is the bisulfite conversion or the HRM amplification that limited the efficiency of amplification of DNA of DNA levels below 1 ng, we performed serial dilutions of bisulfite-modified samples prepared with 1 ng of input genomic DNA. Four
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Acknowledgements This work was supported in part by
2019-07-05
Acknowledgements This work was supported in part by a Scholarship Fund for Young Researchers by the Promotion and Mutual Aid Corporation for Private (2017 to S.K.), research grant from Japan Rett Syndrome Support Organization (2018 to S.K.), and MEXT-Supported Program for the Strategic Research Fou
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