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All experiments in this study were performed
2021-09-15

All experiments in this study were performed at pD 6.1 for reasons described above. This leaves a question about the implications of stereochemistry in vivo. At physiological pH the GSTP1-1 catalyzed rate of EASG formation is only 1.1-fold higher than the non-enzymatic rate [26]. However, when human
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T L cells can be induced to differentiate
2021-09-15

3T3-L1 cells can be induced to differentiate into adipocytes by the appropriate hormonal treatment and they offer a useful in vitro model system for adipogenesis. GPR120 mRNA was detected in differentiated mature adipocytes but not in confluent preadipocytes (Fig. 3A). The level of GPR120 mRNA incre
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br Methods br Results br
2021-09-14

Methods Results Discussion Conclusion The in vivo pEC50 for NEFA release in the rat was derived for 12 GPR81/GPR109A agonists, including the historically well-known nicotinic acid. By integrating in vitro cell assay potency data for both receptors, these in vivo pEC50 values could be rea
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Adenosine triphosphatase ATP is a signaling molecule in
2021-09-14

Adenosine triphosphatase (ATP) is a signaling molecule in acute pain and chronic pain(Burnstock, 2009, Burnstock, 2013, Burnstock, 2014, Chizh and Illes, 2001). It is also known that presynaptic A1 receptors are involved in the inhibition of transmitter release (Vizi and Knoll, 1976). Extracellular
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br The concept of the axo myelin synapse
2021-09-14

The concept of the axo-myelin ‘synapse’ Axons can release glutamate in a Ca+-dependent and independent manner (reviewed in [13,69]). Glutamate released from axons activates GluRs located in myelin, a feature that gave rise to the idea of the axo-myelin ‘synapse’ by analogy with classical synaptic
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br Conclusions Osteoclcastogenesis is regulated by
2021-09-14

Conclusions Osteoclcastogenesis is regulated by multiple signal transduction pathways. To maintain bone homeostasis, osteoclast cells must achieve a balance regulation of formation, function, and trafficking of its precursors. Here, we proposed a model in which crosstalk between Fas and S1P/S1P1
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FDP is considered as key intermediate in the
2021-09-14

FDP is considered as key intermediate in the isoprenoid biosynthetic pathway, since it is the common precursor of polyisoprene units and farnesylated proteins (Cao et al., 2012). In order to understand the role of FDP gene in rubber-producing plants it is of critical importance to BCECF-AM and chara
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bcl-2 inhibitor The finding of histamine action on ASICs als
2021-09-14

The finding of histamine action on ASICs also raises the question about possible action of other histamine receptor ligands. In the present work we selected several compounds and performed electrophysiological testing of their action on recombinant homomeric ASIC1a and ASIC2a. Nα-methylhistamine is
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br Discussion In this study we show that conditional
2021-09-14

Discussion In this study, we show that conditional loss of Yap/Taz in the endocardium results in a thin compact myocardium and early postnatal lethality. We also report that loss of Yap/Taz in the endocardium leads to diminished expression of Nrg1, which is a crucial endocardial-derived factor th
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The concentration of rapamycin that gave half maximal
2021-09-14

The concentration of rapamycin that gave half-maximal induction of the expression of HO-1 and Prx-1 mRNA in normal hepatocytes was 0.05 μM, with maximal induction at about 0.1 μM rapamycin. While, at rapamycin concentrations higher than 0.1 μM, the degree of enzyme induction decreased, elevated expr
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br Mechanism of HH pathway activation in NSCLC
2021-09-14

Mechanism of HH pathway activation in NSCLC Despite the role of the HH pathway in basal cell carcinoma and medulloblastoma, it has been postulated that epithelial tumors do not demonstrate cell autonomous HH ligand activity. The main evidence comes from the study by Yauch et al showing no correla
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br Significant efforts are currently focused on
2021-09-14

Significant efforts are currently focused on non-dopaminergic strategies to address the unmet medical needs in schizophrenia, and targeting -methyl--aspartate (NMDA) bafilomycin a1 hypofunction has garnered a great deal of attention., , Elevation of synaptic glycine levels near NMDA-containing s
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Much less is known about the and subunits
2021-09-14

Much less is known about the α3 and α4 subunits. GlyR α3 subunit immunoreactive synapses are concentrated in discrete bands across the IPL; besides, bipolar, amacrine and ganglion cells have been suggested to express it (Haverkamp et al., 2003, Wässle et al., 2009). In fact, All amacrine express α3β
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In the present study co
2021-09-14

In the present study, co-administration of TM (AT1 receptor blocker) and PD (AT2 receptor blocker) were made in ischemic mice to explore the significance of AT2 receptors in cerebral ischemia while blocking central AT1 receptors. Also to prove that AT2 receptors should be free after ischemic injury
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Herein we report the discovery of
2021-09-14

Herein, we report the discovery of AM-3189 (). AM-3189 maintains the in vivo efficacy of AMG 837 while displaying a superior pharmacokinetic profile and minimal CNS exposure. As we reported previously, activity on the GPR40 receptor varies significantly with substitution at the β-carbon relative to
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