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In this study we have explored
2019-08-13
In this study we have explored a functional role of the oxysterol/EBI2 system in this process. In 2011 we and others reported the discovery of oxysterols as ligands for EBI2 [6], [7]. Oxysterols are metabolites generated by hydroxylation of cholesterol and have been linked to a variety of fundamenta
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br Conflicts of interest br Financial support NZ is
2019-08-13
Conflicts of interest Financial support NZ is an Established Investigator of the Dutch Heart Foundation (2013T111) and is supported by an ERC Consolidator grant (617376) from the European Research Council and by a Vici grant from the Netherlands Organization for Scientific Research (NWO; 91818
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Metal ions are known not
2019-08-13
Metal ions are known not to be necessary for catalytic activity of serine proteinases. Nevertheless, Co2+ and Ca2+ ions were found to stabilize glutamyl endopeptidase molecule [1], [7], [19]. In our previous study, we have described significant stimulating effect of Ca2+, Mg2+, and Co2+ on biosynthe
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In the present study promoting bile acid synthesis by activa
2019-08-13
In the present study, promoting bile Dioscin manufacturer synthesis by activating EP4 receptors was shown to exert protection against hepatic steatosis. This finding may be relevant for treatment of non-alcoholic fatty liver disease, a major cause of liver disease and prominent indication for liver
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20187 The synthesis of tricyclic analogs is
2019-08-13
The synthesis of tricyclic analogs 28–33 is described in Scheme 3. Oxidative C–C bond cleavage of the terminal olefin of 39i afforded a tricyclic product 52 without isolation of an aldehyde expected as an intermediate. Aminolysis of the chloride 52 with optionally substituted anilines afforded 28–30
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br Menopausal hormone therapy from the beginning to
2019-08-12
Menopausal hormone therapy, from the beginning to WHI Estrogen products have been used since the 1940s, with increasing prescription through the 1960s. First concerns appeared in the 1970s when oral treatment was linked to uterine cancer. Oral estrogens have traditionally been coupled with proges
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br Conclusions br Acknowledgements This work was supported
2019-08-12
Conclusions Acknowledgements This work was supported by the Science and Technology Planning Projects of Guangdong Province (2014A020210027); the Major Scientific Research Projects of Universities in Guangdong Province (2016KZDXM042); the Natural Science Foundation of Guangdong Province (2015A0
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br Fragment based drug discovery FBDD
2019-08-12
Fragment-based drug discovery (FBDD) is a powerful method to discover drug leads and has been widely adopted in both academia and industry. FBDD can be used to explore chemical PR619 space with libraries which are smaller in size, producing drug leads with high ligand-binding efficiency. It also
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The sequence identity of CYP A with
2019-08-12
The sequence identity of CYP3A163 with CYP3A sequences from other species is maximum in reptiles ranging (75-91)%, gradually decreasing from Metabolism Compound Library manufacturer (63-71)% to mammals 62% to downwards based on evolutionary distances. The high level of homology with CYP3A77 in Alli
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BGB-324 A phenylacetic acid derivative discovered in a high
2019-08-12
A phenylacetic BGB-324 derivative (), discovered in a high throughput screen for CRTH2, inhibited the binding of H-PGD to CRTH2 receptors on 293 cells with an IC of 0.010μM, and inhibited the binding of H-PGD to DP receptors with an IC of only 8.3μM (). Compound also inhibited CRTH2 mediated cell mi
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The results of bisaryl ether linker
2019-08-12
The results of bisaryl ether linker study are shown in . It was found that the methylene linker () moderately improved the binding to the DP receptor. The increased binding potency was also diminished in the presence of plasma, possibly due to higher plasma protein binding. Other linkers, such as th
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The importance of mitochondria as site of aerobic oxidation
2019-08-12
The importance of mitochondria as site of aerobic oxidation of metabolic fuels, such as FA, has been recognized for a long time. It has been observed that the number of mitochondria may vary in response to cellular metabolic requirements and hormonal environment (Gao et al., 2014). In order to susta
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Introduction Robust evidence suggests that genetic factors i
2019-08-12
Introduction Robust evidence suggests that genetic factors influence an individual\'s susceptibility to BD (Craddock and Sklar, 2013). Yet, no single, high penetrance gene has been identified with direct causality (Craddock and Sklar, 2009). The largest GWAS to date for identifying genes conferring
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It should be noted that the long lifetime binding
2019-08-12
It should be noted that the long-lifetime binding-responsive luminescence of ARC-1528 and ARC-1530 becomes evident only upon illumination with radiation at near-UV range where the excitation of ATB or ASB moiety is possible. At higher wavelength range (visible light), the fluorophore (5-TAMRA) can b
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This paper proposes an acceptance process and
2019-08-12
This paper proposes an acceptance process and evaluation criteria, specialized for the dedication of indirect COTS SW as well as direct ones. (Step 1) It first recognizes an indirect COTS SW as a target of dedication, unlike EPRI NP-5652/TR-106439. (Step 2) It then determines the safety category of
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