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br Conclusion In conclusion we discovered a pair of
2022-03-24

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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Primarily because secretase was a therapeutic target in
2022-03-23

Primarily because γ-secretase was a therapeutic target in AD, a plethora of γ-secretase inhibitors (GSIs) have been developed that effectively inhibit γ-secretase cleavage in humans [16]. Indeed, “druggability” of γ-secretase has not been an issue even when the identity of the target was unknown in
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To enhance the impact of GD as an immune target
2022-03-23

To enhance the impact of GD2 as an immune target in this cancer, we investigated a novel strategy to upregulate expression on the cell surface of EwS cells by an epigenetic agent, based on the following rationale. Biosynthesis of GD2 and other gangliosides during organ development is driven by stage
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Aberrant activity of PRC as a
2022-03-23

Aberrant activity of PRC2 as a result of over expressed EZH2, has been frequently seen in a wide range of human cancers including breast and prostate tumors [10]. However, leukemia-associated epigenetic aberrations are not fully understood [7]. Herein, we will overview the current knowledge of epige
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NeuroHIV is initiated by HIV crossing the blood brain barrie
2022-03-23

NeuroHIV is initiated by HIV crossing the blood–brain barrier (BBB) to enter the CNS. This is thought to occur primarily via the transmigration of infected CD14+CD16+ monocytes (Williams, 2014), using the monocytes as “Trojan Horses” (Peluso, 1985), although some studies suggest alternate routes of
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nor-NOHA acetate synthesis In Kdm c germline and forebrain
2022-03-23

In Kdm5c germline and forebrain conditional knockout mice, RNA sequencing showed the upregulation of a large set of genes, suggesting that Kdm5c functions primarily as a transcriptional repressor [,]. While no changes in global H3K4me3 levels were observed in the knockout neurons, there were thousan
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Sometime ago we have described diamino triazines as histamin
2022-03-23

Sometime ago we have described diamino-1,3,5-triazines as histamine H4R ligands,12, 13 and aryl derivatives of the 1,3,5-triazine, which attenuated inflammatory and nociceptive response in vivo in the rodent models of inflammation induced by lpl receptor and zymosan. In this work we describe new de
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Diabetes and atherosclerosis are paralleled by impaired
2022-03-23

Diabetes and atherosclerosis are paralleled by impaired wound healing and endothelial angiogenesis in the periphery, which cause severe complications and mainly occur as a result of the elevated circulating levels of glucose and free fatty acids. Yuan et al. recently showed that palmitic histamine r
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Hippo signaling is unique in that it
2022-03-23

Hippo signaling is unique in that it does not possess a cognate ligand and receptor system. Instead, numerous upstream sensors that monitor cell morphology, cell polarity, cell-cell contact, and mechanical stress impinge onto the Hippo pathway core kinases, MST, and LATS. This in turn indicates the
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br Conclusions br Acknowledgements This
2022-03-23

Conclusions Acknowledgements This work was supported by grants from the Polish National Science Center: 2014/14/E/NZ1/00139 (to A. Jazwa-Kusior) and 2015/17/N/NZ1/00041 (to M. Tomczyk) and National Centre for Research and Development (STRATEGMED2/269415/11/NCBR/2015) (to J. Dulak). Faculty of
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Hh signaling pathway plays an essential
2022-03-23

Hh signaling pathway plays an essential role in the regulation of invertebrate and vertebrate tissue development and metabolic homeostasis. Components of Hh signaling pathway have been identified in succession, including Hh ligands, membrane protein receptors, cytoplasmic components and transcriptio
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G protein coupled receptor kinases
2022-03-23

G protein-coupled receptor kinases (GRKs) are another group of kinases whose limited substrate repertoire is associated with an extensive binding interface. GRKs phosphorylate activated G protein-coupled receptors (GPCRs) at multiple sites, promoting binding of arrestin proteins to mediate receptor
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An interesting question is why
2022-03-23

An interesting question is why RhoF has such the slow rate of GDP dissociation. The amino 84 9 mutations in a presumable GDP-binding site of RhoF had only moderate effects on the GDP dissociation (Fig. 3C), which suggests a mechanism involving the global amino acid sequence of RhoF, rather than the
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Notably we observed that GPR activation induced by
2022-03-22

Notably, we observed that GPR35 activation induced by PA, an in vivo GPR35 agonist [6], significantly decreased DAI, colon weight, and histological score, while increasing colon length in mice with DSS-induced colitis. Furthermore, fibronectin and integrin α5 were co-localized with GPR35 on the colo
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br Discussion Naloxone and CTAP were
2022-03-22

Discussion Naloxone and CTAP were able to alter the febrile response induced by gp120. This effect was particularly evident during the initial hours following gp120 administration (90–210min). We also investigated the potential role of the delta-2 opioid receptor in gp120-induced fever. The delta
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