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In summary we have identified a
2021-08-11

In summary, we have identified a series of amides as ERRγ agonists with suitable potency for further development. Our SAR studies of this chemotype identified SR19881 as the most potent full agonist of ERRγ with an EC=0.39 μM in a binding assay and an EC=4.7 μM in a cell-based assay. SR19881 was als
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Enhanced responses to varying concentrations of bronchoconst
2021-08-11

Enhanced responses to varying concentrations of bronchoconstrictors, such as MCh, and airway obstruction are characteristic of ONX-0912 and common to other clinical states, including chronic obstructive pulmonary disease, lung transplantation, and infection- or chemical agent-induced airway inflamm
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br Experimental Procedures br Author Contributions br Acknow
2021-08-11

Experimental Procedures Author Contributions Acknowledgments Introduction The intestinal mucosal barrier surface is constantly exposed to food antigens, beneficial microbes, pathogens, and a multitude of other environmental stimuli (Turner, 2009). Innate lymphoid WZB117 (ILCs) are known
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br Conclusion br Introduction br CRL E ligases
2021-08-11

Conclusion Introduction CRL4 E3 ligases in tumorigenesis Small molecule-based PROTACs PROTAC: Major biological impacts Acknowledgements The authors sincerely apologize to all those colleagues whose important work was not cited in this paper owing to space limitations. They thank th
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While a number of studies have helped elucidate
2021-08-11

While a number of studies have helped elucidate the principles of target amino group specificity, UBL selectivity, and Ub TH-302 australia specificity [3], [4], [9], [10], [14], [19], [20], [23], [24], [33], [34], [37], [38], [39], [40], [41], the role of the canonical E2-RING interface in governing
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The best characterized APC C substrates are recruited
2021-08-11

The best-characterized APC/C substrates are recruited via various linear motifs (e.g., D boxes, KEN boxes, and ABBA motifs) that serve as degrons, binding to distinct regions of the β-propeller domain of a coactivator (Figure 1, Figure 3B) (reviewed in [44]). In addition, D boxes also simultaneously
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br Materials and methods br Discussion To date
2021-08-11

Materials and methods Discussion To date, only a fraction of studies pertaining to analysis of avian semen have focused on the study of DNA, with the vast majority being associated with the effects of cryopreservation on sperm DNA integrity (Kotłowska et al., 2007, Madeddu et al., 2009, Partyk
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br Acknowledgments We thank Jon
2021-08-11

Acknowledgments We thank Jon Clardy, Juan Manuel Domínguez, José Francisco García Bustos, and the GlaxoSmithKline (GSK) Plasmodium falciparum dihydroorotate dehydrogenase project team for their contributions, helpful advice, and discussions. Introduction Dihydroorotate dehydrogenase (DHODH) i
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Traditionally serum triglycerides have been measured in the
2021-08-11

Traditionally, serum triglycerides have been measured in the clinic in the fasted state in order to reduce variability and also to facilitate the calculation of LDL-cholesterol via the Friedewald equation, which was derived using fasted samples (Warnick and Nakajima, 2008). We have previously report
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Proteolysis by CPs is crucially
2021-08-10

Proteolysis by CPs is crucially important for cereal seed development and germination. However, these enzymes must be tightly controlled. Pre-harvest sprouting is a phenomenon in which the control of CPs is disrupted. This disruption manifests in the premature synthesis and activation of CPs, leadin
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reference 4 Cell lines which possess microglial or neuronal
2021-08-10

Cell lines which possess microglial or neuronal properties are uncomplicated and convenient in vitro models for studying reference 4 injury at the cellular and molecular levels. Microglial BV-2 cells are derived from the immortalized mouse microglia and exhibit many of the morphological, phenotypic
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The distorted geography on the number
2021-08-10

The distorted geography on the number lines of many pre-service primary teachers in this study also highlights the need to provide them with strong visual models of negative numbers and their ordering. The evidence from Indri's interview is that some standard models of negative numbers (e.g., lendin
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From the results of previous experiments with the
2021-08-10

From the results of previous experiments with the purvalanol B affinity matrix, it is not clear whether the selective capture of parasite CK1 enzymes is a reflection of their high abundance or rather their affinity for the ligand compared with other kinases present in the lysates. Based on compariso
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The intestinal cholesterol absorption markers sitosterol and
2021-08-10

The intestinal cholesterol Chymostatin markers sitosterol and campesterol to cholesterol levels were significantly lower in Villin-Tgif1 mice compared to wild type mice, irrespective of diet. However, the decrease was less pronounced in Villin-Tgif1 mice fed a chow diet (∼20–30%) compared to mice f
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TL32711 br Materials and methods br
2021-08-10

Materials and methods Results Discussion The oestrogen agonist properties and androgen antagonist activities of parabens have been well documented by a variety of in vitro and in vivo assay systems over the past decade (Chen et al., 2007, Darbre and Harvey, 2008, Golden et al., 2005). To th
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