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GSK 650394 Recently a receptor for nicotinic
2021-11-17
Recently, a receptor for nicotinic acid, named GPR109A (also known as HM74a in man or PUMA-G in the mouse) has been identified (Lorenzen et al., 2001, Lorenzen et al., 2002, Soga et al., 2003, Tunaru et al., 2003, Wise et al., 2003). This receptor, a member of the 7 transmembrane G-protein coupled f
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A considerable body of evidence suggests
2021-11-17
A considerable body of evidence suggests that alcohols, volatile anesthetics and inhaled drugs of abuse act at discrete sites on glycine and GABAA receptors, specifically within circumscribed protein pockets (Mascia et al., 2000, Mihic et al., 1997, Beckstead et al., 2000). An amino hydrocort resid
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To help resolve the question of simple binding versus
2021-11-17
To help resolve the question of simple binding versus transport, we reasoned that if quercetin is transported by GLUT1, we should be able to block its uptake by other GLUT1 inhibitors. We initially investigated the effects of two newly identified GLUT1 inhibitors, BAY-876 and WZB-117. WZB-117 was fi
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Another consistent observation in our studies was the lower
2021-11-17
Another consistent observation in our studies was the lower plasma catecholamine concentrations in the exercised GHSR-null mice, suggesting a diminished sympathoadrenal response. A proper sympathoadrenal response is essential for increasing substrate utilization during exercise [81]. Thus, the reduc
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Recently several studies addressed cytological and biochemic
2021-11-17
Recently, several studies addressed cytological and biochemical features of oocyte aging. It was reported that cytological changes associated with the mammalian post-ovulatory oocyte aging include chromatin disorganization, abnormal meiotic spindle location or its disruption, partial exocytosis of c
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The present study showed that the FPR
2021-11-17
The present study showed that the FPR2 antagonists PBP10 and BOC2 are potent antiviral molecules in vitro against a broad range of IAV and B viruses. Consistently, our previous report showed that FPR2 plays a deleterious role during IAV infections and that another FPR2 antagonist WRW4 inhibits IAV r
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These observations are of particular interest in
2021-11-17
These observations are of particular interest in the context of recent conceptual changes regarding the mechanisms by which different types of leukocytes contribute to atherogenesis. Over the last decade, the paradigm of the predominant circulatory origin of lesional macrophages has been challenged
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The ability of GPX and other selenoproteins
2021-11-17
The ability of GPX4 and other selenoproteins to be selectively induced by ferroptotic stimuli suggests that the stress-induced increase in the transcription of a number of putative, “antioxidant” selenoproteins is an adaptive homeostatic, but insufficient response to prevent cell death in the face o
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However at variance with the well studied
2021-11-17
However, at variance with the well-studied R form of FBP1 which is flat, the R state of FBP2 is diametrically different, with a perpendicular orientation of the upper and lower dimers (Barciszewski et al., 2016). The cruciform-like R state of FBP2 is stabilized by a unique hydrophobic motif called ‘
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NeuroHIV is initiated by HIV crossing the blood brain barrie
2021-11-17
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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There are many histone H K demethylases
2021-11-17
There are many histone H3K9 demethylases, including JMJD1 A, JMJD2 A, JMJD2B, and JMJD2C (Kooistra and Helin, 2012). Considering that EPO ion channel is regulated by hypoxia, we further analyzed several hypoxia-induced H3K9 demethylases, such as JMJD1 A, JMJD2B and JMJD2C (Beyer et al., 2018; Polla
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The components of the SAGA complex including
2021-11-17
The components of the SAGA complex including Gcn5 have recently been found to be involved in regulating pathways that are required for development and virulence in different species under the environmental stresses, around 10% of S. cerevisiae genes are activated by the transcriptional coactivator S
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In conclusion the most salient observation
2021-11-17
In conclusion, the most salient observation from this study was that PAE reduced the expression of HDC protein expression in dentate gyrus, cerebral cortex, and cerebellum, but not in the caudate nucleus or ventral hypothalamus. The regional basis for this heightened sensitivity is not known, but it
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Other N substituted carboxamide oxy pyridine derivatives a h
2021-11-17
Other N-substituted-6-carboxamide-3-oxy-pyridine derivatives 52a, 52h, 52i, and 53h were synthesized using an alternative route. The Pd-catalyzed Heck aminocarbonylation of 44 or 45 with (PPh3)2PdCl2 catalyst in the presence of Et3N under CO atmosphere successfully provided various N-substituted-6-c
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Acknowledgments The authors thank Partners Healthcare for
2021-11-17
Acknowledgments The authors thank Partners Healthcare for financial support. This work was also supported in part by NIH Grant R01CA122608 to J.M.G.H. Introduction The phosphorylation of histone H3 is recognized as a hallmark of mitosis. Histone H3 phosphorylation at Thr3 (H3T3ph) acts as a mit
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