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Based upon these findings on portions A and
2021-02-27
Based upon these findings on portions A and B, novel scaffolds of EP4 antagonist, and (R & R=()-Me; =Cl; R=H), shown in , were identified. We next focused on optimizing portion C of these scaffolds. We utilized for an alternative synthesis of nicotinamide scaffold , which is quite effective for
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Our study provides proof of principle for dimerizing two dif
2021-02-27
Our study provides proof of principle for dimerizing two different E3 ligases as a novel approach to inducing one ligase to degrade the other one. The outcome of ‘ligase versus ligase’ PROTAC-mediated activity might be unpredictable a priori, but could reveal a new mechanism for proximity-mediated h
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In general cellular senescence is considered a programmed
2021-02-27
In general, cellular senescence is considered a programmed response to stress that can be activated by oxidative stress, irradiation or action of substances or drugs. These stressors cause DNA damage and, through the action of specific proteins (p53 and p21), lead to cell senescence (di Fagagna, 200
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br Compliance with ethical standards
2021-02-26
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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br Materials and methods br Results br Discussion The first
2021-02-26
Materials and methods Results Discussion The first DGAT1 gene was described in the mouse in 1998 [28], and a few years later DGAT2 was identified from the oleaginous fungus Mortierella ramanniana[29]. Although both of them are known as the primary enzymes for de novo TAG biosynthesis, they
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In humans CYP A major isoforms of CYP As in
2021-02-26
In humans, CYP3A4/5, major isoforms of CYP3As in the liver, have variants that reduce the enzyme activities [33], [34]. In addition, Werk et al. recently reported the first case of a complete failure of CYP3A enzyme activity due to homozygous loss-of-function mutation of CYP3A4 combined with nonfunc
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Studies have shown that the cultivation of BMSCs under hypox
2021-02-26
Studies have shown that the cultivation of BMSCs under hypoxic conditions, treating with cytokines (such as HGF, IGF-1 and IL-6) and viral-mediated CXCR-4 gene delivery have been shown to re-establish CXCR-4 expression on the surface of stem Liquidambaric acid (Liu et al., 2010, Liu et al., 2014a,
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br Amygdala microcircuitry and fear
2021-02-26
Amygdala microcircuitry and fear learning Recent work has begun to dissect functional amygdala circuits that are responsible for the acquisition and expression of fear learning. Ciocchi et al. (2010) identified separable populations of ARCA EGFP within the CeAL that have opposite responses to CS
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In summary our data demonstrated a biological
2021-02-26
In summary, our data demonstrated a biological function of cpt1a gene from large yellow croaker. In particular, we indicated the effects of fasting on free carnitine status, CPT1 kinetics, and cpt1a mRNA expression in liver of large yellow croaker. During short-term fasting, the fish liver may have
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br Limitations of the study br Possible
2021-02-26
Limitations of the study Possible conflicts of interest Dr. Fayemiwo or SAF has received full financial support from Europe Gilead Sciences Ltd. for his M.Sc. degree programme in Medical Mycology and has been paid for talks on behalf of AstraZeneca and GSK. Caroline Moore or CBM has received
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Stable carbon and nitrogen isotope ratios in bone collagen
2021-02-26
Stable carbon and nitrogen isotope ratios in bone collagen and carbon isotope ratios in bone apatite data were obtained by the means of the techniques described in supplementary data (SD1). For collagen, standard indicators have been used to assess its preservation, such as collagen yield, carbon an
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Based on the above we hypothesized that
2021-02-26
Based on the above, we hypothesized that a PROTAC strategy would be effective to induce CK2 protein degradation. Herein reported is an approach for the preparation of novel PROTACs via “click reaction” for degradation of CK2 protein (Fig. 2). Importantly, “click reaction” is a very facile, selective
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In the present study cells were exposed to a
2021-02-26
In the present study, cells were exposed to a low level of arsenite and a low cytotoxic concentration of BaP. Thus, γ-H2AX loss correlated with repair of DNA damage in cells co-exposed to arsenite and BaP. These results show that arsenite inhibits repair of BaP-induced DNA damage. In a previous stud
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br Effects of estrogens on bone Estrogens play an
2021-02-26
Effects of estrogens on bone Estrogens play an important role in bone remodeling, as demonstrated by studies in mice in which the ER genes were deleted [21], [22]. ERβ compensates for the LCL161 of ERα, and vice versa, but when both ERs are deleted a profound decrease in trabecular bone volume i
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br The orphan estrogen related receptor
2021-02-26
The orphan estrogen-related receptor exists as three subtypes (ERRα, ERRβ, and ERRγ) in the human genome. ERRα is expressed in metabolically active tissues such as muscle and adipose. ERRγ is expressed in the spinal cord and CNS. ERRβ appears to play a role in development, as postnatal expression
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