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The optimization of the lead compound was initiated and
2021-06-17
The optimization of the lead compound () was initiated and the initial key SAR and the results of the structural modifications of lead compound are summarized in . Replacement of the carboxylic Lithocholic Acid moiety with other functional groups led to loss of functional activity against EP4 rece
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br Materials and methods br Results br Discussion COX mediat
2021-06-17
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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The importance of AAE in
2021-06-17
The importance of AAE3 in enhancing the survival of plants and yeast when confronted with certain environmental stresses has been documented in recent reports. In response to biotic stress such as oxalate-secreting micro-organisms, AAE3 was found to reduce the inhibitory growth effects of the secret
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Our study revealed elevated basal Akt phosphorylation in die
2021-06-17
Our study revealed elevated basal Akt phosphorylation in diet-induced obesity, the effect of which was reversed by ETAKO. Activation of Akt promotes cardiac hypertrophy via a number of cellular mechanisms including activation of its downstream targets such as mTOR and GSK3β [45, 46]. Short-term acti
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br Material and methods br Results br Discussion
2021-06-17
Material and methods Results Discussion The results show for the first time that DDRs may be involved in the pathogenic mechanisms of neurodegenerative diseases. We found that DDR1 and DDR2 levels are up-regulated in post-mortem AD and PD brains, suggesting that these receptors play a role
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In this study we implicate SCFFBXO E ligase
2021-06-16
In this study, we implicate SCFFBXO3 E3 ligase as a critical modulator of inflammation in atherosclerosis and demonstrate the efficacy of a small molecule FBXO3 inhibitor in suppressing inflammatory responses important in atherosclerosis. Specifically, individuals carrying a hypofunctioning genetic
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We also note that though the deletion of
2021-06-16
We also note that though the Shikonin of the N-terminus in Ube2E1∆N46 or the mutations in Ube2E16KtoR enhanced their activity compared to the wild type, it failed to match Ube2D2 (Fig. 1). We concluded this difference to be multi-factorial as none of the Ube2E1∆N46 point mutants involving “Ub back-b
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DNA hypomethylation has been found in
2021-06-16
DNA hypomethylation has been found in liver tumor and other tumors of humans, such as laryngeal cancer, lactacystin tumors, tongue squamous cell carcinoma and uterine leiomyomas [[20], [21], [22], [23], [24]]. Then, we mainly sought to confirm whether TCA could induce DNA hypomethylation in vitro an
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LPA is known to regulate the peroxisome proliferator
2021-06-16
LPA is known to regulate the peroxisome proliferator-activated receptor γ and the reorganization of actin cytoskeleton [58]. However, the physiological functions of LPA in cells are still poorly understood. The simultaneous production of PA with/without 1-LPA or 2-LPA may be important to maximize a
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The use of SP in IPTp
2021-06-16
The use of SP in IPTp may not be the only driver of parasite polymorphisms in this population, because Senegal has used sulfadoxine and/or pyrimethamine in the national antimalarial treatment plan for many years, and furthermore these drugs are still being used in antibacterial combination therapy.
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The co occurrence of the AA and the AA
2021-06-16
The co-occurrence of the AA12 and the AA8 domains in CcPDH would allow for electron transfer between these domains. Such electron transfer is known to occur in CDH, and the AA8 family in CAZy is in fact largely comprised of cytochrome domains of multi-domain CDHs. One notable exception concerns the
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We used two different VSMCs cell lines KSB and
2021-06-16
We used two different VSMCs cell lines, KSB and CSD (isolated from two different thoracic aortas). Rat aortic VSMCs were isolated from medial segments from thoracic rate Fenofibrate from Wistar-Kyoto rats (six to eight weeks old, Charles River Wiga GmbH) and cultured over several passages as descri
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The isolation of a proteinaceous
2021-06-16
The isolation of a proteinaceous putative inhibitor of cysteine proteases from the extracts of Y. enterocolitica and E. coli was performed by affinity chromatography on immobilized and inactivated papain (Fig. 7A). Instead of the column variant of this technique (Tsushima et al., 1992), we used a ba
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apelin receptor In conclusion we developed a
2021-06-16
In conclusion, we developed a new CysLT1 and CysLT2 receptors-mediated anaphylaxis guinea pig model that can be useful for screening both CysLT2 receptor and CysLT1/2 receptor antagonists. In addition, we have shown that the dual CysLT1/2 receptor antagonist ONO-6950 can exert protective effect agai
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Based on both the observational and theoretical
2021-06-16
Based on both the observational and theoretical data generated in this study, it appears that the mechanism(s) underlying lower IFM CPT1 activity is complex. Modeling enzyme activity versus alterations in catalytic efficiency (Fig. 3A) suggests that the observed age-associated changes in Km and Vmax
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