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Much evidence has demonstrated that the
2022-02-17

Much evidence has demonstrated that the differential HER2 level between normal tissue and a tumor helps to define HER2 as an ideal diagnostic and treatment target. Thus, HER2 status can be incorporated into a clinical decision, along with other prognostic factors, such as the CC-223 mg receptor (ER
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br Disp Mediated Hh Membrane Recycling Due to its
2022-02-17

Disp-Mediated Hh Membrane Recycling Due to its cholesterol modification, Drosophila Hh enriches on sphingolipid-rich apical membranes of polarized epithelial PF 1022A 33., 38., 39.. Genetic studies examining Hh release from wing imaginal disc epithelia suggest that Hh must be endocytosed from th
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br AURK Functions br Concluding
2022-02-17

AURK Functions Concluding Remarks The AURKs are crucial regulators of cell division; however, little is known about the mechanisms by which these kinases function in meiosis. Recent work has begun to chip away at the specific roles that each of the kinases play; however, as more is uncovered,
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The balance and composition of the
2022-02-17

The balance and composition of the gut microflora can be altered by the use of antibiotics or by colonization of the intestine by pathogens. This change may also induce, or be induced by, modifications in the body’s immune response, ultimately leading to disease. Thus, when intestinal homeostasis is
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In addition to understanding the GEF
2022-02-17

In addition to understanding the GEF-GAP cycle regulating Rho-family GTPases, studies have continued to address the role of the Rho-GDIs, which binds to the geranylgeranyl tail to sequester Rho-family GTPases from interacting with lipid membranes, preventing their activation. Whilst it would be tem
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Introduction Epigenetic alterations play an important
2022-02-17

Introduction Epigenetic alterations play an important role in carcinogenesis. Aberrant promoter CpG island hypermethylation causes transcriptional gene silencing [1], and has been documented for a number of genes in prostate cancer (PCA) [2]. Histone modifications are also important regulators of t
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br Materials and methods br
2022-02-17

Materials and methods Results Discussion To understand the molecular basis for how ghrelin secretion is regulated at the cellular level, we identified the full repertoire of 7TM receptors and G proteins in gastric ghrelin Golgicide A and functionally characterized the majority of the recept
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As disclosed in our preceding paper medicinal
2022-02-17

As disclosed in our preceding paper, medicinal chemistry SAR optimization of an HTS hit led to the discovery of , a potent and selective GPR119 agonist. This scaffold differs significantly from the ‘classical’ GPR119 pharmacophore, exemplified by the examples and (). Notably, rora lacks an essentia
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The neuronal glycine receptor HSOR allopregnanolone pathway
2022-02-17

The neuronal glycine receptor/3α-HSOR/allopregnanolone pathway may also be extended to the central nervous effects of gelsemine and koumine in brain. 3α-HSOR is expressed in certain brain regions in rats and humans, such as the limbic system including hypothalamus, hippocampus and amygdala, in addit
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For molecules with potential for
2022-02-17

For molecules with potential for therapeutic use, high potency is desired, preferably in the nM or lower concentration range. However, the glycine receptor specific peptides identified with the New England Biolabs Ph.D. libraries, both in this study (Fig. 3) and by Tipps et al. (2010), acted at low
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PBI is an agonist of GPR and acts as an
2022-02-17

PBI-4050 is an agonist of GPR40 and acts as an antagonist or inverse agonist of GPR84. It cannot be excluded that other targets besides GPR40 and GPR84 could be implicated in the mechanism of action of PBI-4050 and could be explored in future studies. However, the present study, and in particular th
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We observed the reduced expression of the GluN
2022-02-17

We observed the reduced expression of the GluN2a subunit in the temporal and entorhinal cortexes and ventral hippocampus, which may result in the predominance of GluN2b-containing NMDA receptors during the latent period. Previously, using the same model, we revealed the reduction of the GluN2a/GluN2
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br Origin of the vertebrate hexokinase gene family
2022-02-17

Origin of the vertebrate hexokinase gene family Multiple hexokinases have been found in vertebrates, plants and yeast (Wilson, 1995, Cárdenas et al., 1998). A hexokinase in both vertebrates and yeast has, unfortunately, been named glucokinase. The sharing of the name glucokinase has suggested to
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br Conclusion In conclusion we discovered a pair
2022-02-17

Conclusion In conclusion, we discovered a pair of novel epimers CBC and CBD from plant C. bungei. These two natural compounds inhibit Hh pathway by blocking signaling at the level of Gli. They are effective in suppressing Hh pathway-dependent medulloblastoma growth in vitro and in vivo. Furthermo
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br Acknowledgments This work was supported by
2022-02-17

Acknowledgments This work was supported by the NIH (R01DK103884 to JMZ, R01DK100659 to JKE, and F32DK104659 and K01DK111644 to CMC), the Diana and Richard C. Strauss Professorship in Biomedical Research, the Mr. and Mrs. Bruce G. Brookshire Professorship in Medicine, the Kent and Jodi Foster Dist
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