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We propose the following model for how
2021-04-20

We propose the following model for how B cell-guiding EBI2 ligand gradients are established in lymphoid tissues. CH25H and CYP7B1 are needed in radiation-resistant stromal cells, are abundantly expressed and active in CXCL13+ and CCL21+ FRCs, but not lymphocytes, and are poorly expressed in the inne
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A growing number of other post translational modifications
2021-04-20

A growing number of other post-translational modifications are implicated in regulation of the ubiquitin system, including substrate modification by hydroxylation, glycosylation, acetylation, methylation, modification by poly(ADP-ribose) (PAR), and attachment of ubiquitin-like modifiers. The HIF1-α
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In the context of E ligase drug discovery it
2021-04-20

In the context of E3 ligase drug discovery, it is critical to identify the appropriate E2/E3 substrate pairing to ensure the development and use of the most physiologically relevant screening assay. There have been many reports of limited E2/E3 activity profiling with a small number of E2 and E3 Gef
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br Conclusion From the series of synthesized N methylated an
2021-04-20

Conclusion From the series of synthesized N-methylated and N-benzylated pyrimidinediones, it may be concluded that the presence of electron rich species with pyrimidinediones is vital for enhancing binding with target, although, incorporation of steric bulky group must be taken into consideration
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With regard to the DGATs we have found that
2021-04-20

With regard to the DGATs, we have found that the majority of algal species encode at least one DGAT1, although it appears to be absent from Ostreococcus and Micromonas, as is the case for yeast, S. cerevisiae. More surprising is the presence of multiple DGAT2 genes in algae, with the exception of C.
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For human health risk assessment of chemicals a
2021-04-20

For human health risk assessment of chemicals, a default uncertainty factor (UF) of 3.16 is used to capture inter individual variation in toxicokinetics (Dorne and Renwick, 2005). However, the scientific background for this default UF remains unsatisfactory., Several studies have reported that a fac
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In conclusion our work provides the preclinical evidence sho
2021-04-20

In conclusion, our work provides the preclinical evidence showing the potent in vivo efficacy of AT7519 on chemoresistant cancer T0070907 and its underlying mechanisms of action. Our work supports the biological rationale behind the clinical trials initiated with AT7519, particularly for the treatme
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The synthesis of tricyclic analogs is described in
2021-04-19

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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Employing distinct genetic and pharmacological approaches Di
2021-04-19

Employing distinct genetic and pharmacological approaches, Divakaruni et al. now demonstrate that macrophages still acquire their IL-4-elicited phenotype in the absence of CPT1a (considered the main isoform in leukocytes) or CPT2, and highlight that the increased LC-FAO in M(IL-4) cells is less cruc
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The substitution of serine by an
2021-04-19

The substitution of serine 185 by an alanine led to an increase of EGF-R stabilization along with a better binding of PRK1, a RhoB effector described to be involved in EGF-R intracellular traffic. Overall these data indicated that the phosphate group on serine 185 impaired its binding to the effecto
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It has previously been shown that human melanocytes are resp
2021-04-19

It has previously been shown that human melanocytes are responsive to a multiplicity of hormonal triggers [10], particularly to pituitary or ovarian hormones [11]. Studies concerning the effects of BS-181 on human melanocytes led to inconsistent data [12], [13]. Im et al. [14] reported that the res
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ERR is present early in the developing placenta
2021-04-19

ERRβ is present early in the developing placenta in a subset of Zanamivir in extra-embryonic ectoderm destined to make up the chorion.19, 20 ERRβ is likely essential for reproduction. ERRβ expression is essential for the maintenance of pluripotency and self-renewal potential in mouse embryonic stem
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The compounds listed in Table Table
2021-04-19

The compounds listed in Table 1, Table 2, Table 3, Table 4, Table 5 were biologically evaluated for their inhibition of the specific binding of a radiolabeled ligand [3H]PGE2 to membrane fractions prepared from cells stably expressing each mouse prostanoid receptor. The EP1 antagonist activity of th
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The elastase induced injury model
2021-04-19

The elastase-induced injury model has been shown to produce airspace enlargement, and increases in lung volume and compliance that are similar to those observed in human patients (Hantos et al., 2008, Hamakawa et al., 2011). Thus, this model, which has been used to study emphysema, should be adequat
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br Introduction The ubiquitination status of a target
2021-04-19

Introduction The ubiquitination status of a target protein is achieved via a delicate balance between two opposing forces: ubiquitin E3 ligases and DUBs. It has been postulated that the majority of proteins in a cell are regulated and modified by ubiquitin at some point (Hershko and Ciechanover,
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