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In conclusion a novel series of GPR agonists containing nitr
2021-12-09

In conclusion, a novel series of GPR40 agonists containing nitrogen heterocyclic rings derived from TAK-875 were designed and synthesized. The structural activity relationship studies indicated that the substituents on the nitrogen EGTA had a remarkable effect on the GPR40 agonistic activity. Compo
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br Discussion Our results showed that the histamine H recept
2021-12-09

Discussion Our results showed that the histamine H1 receptor antagonist/inverse agonists, pyrilamine and cetirizine, attenuated not only NMDAR-mediated synaptic current but also LTP in Shaffer collateral-CA1 pyramidal neuron synapses. The H1 receptor antagonist/inverse agonist-induced attenuation
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Oltipraz has been shown to inhibit
2021-12-08

Oltipraz has been shown to inhibit the growth of HCC epinephrine adrenaline and is being evaluated in clinical trials as a potential anti-cancer drug for HCC (Mann et al., 2009; Piton et al., 2005; Yates and Kensler, 2007). The present observation that pre-treatment of tumorigenic liver cells with
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There is increased awareness of HBV reactivation in chronic
2021-12-08

There is increased awareness of HBV reactivation in chronic HCV/HBV co-infected patients treated with DAAs [1], [2]. The recent emergence of this adverse event of DAA therapy is due to the exclusion of HBV co-infected subjects from registration clinical trials evaluating the safety of these treatmen
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The Fe deficiency treatment significantly increased the
2021-12-08

The Fe-deficiency treatment significantly increased the shoot/root Fe ratios in both WT and transgenic lines (Fig. 5C), which implied that the Fe distribution from root to shoot may be an adaptive mechanism or stress response in tomato plants. Thus, the overexpression of GSNOR had a positive effect
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orexin a In order for cytokines to exert any
2021-12-08

In order for cytokines to exert any effect on the NSC population, they must first bind to specific receptors on the cell surface. Numerous pro- and anti-inflammatory cytokines are able to exert effects on the NSC population, including IL-1β through IL-1R1 and IL-1R2, TNFα through TNFR1 and TNFR2, IL
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The facts mentioned above indicate that glycine
2021-12-08

The facts mentioned above indicate that glycine function in brain is tightly regulated or pathologically altered mostly by glycine transporters. Modification of cytosolic regions of transporters, which interconnect them with intracellular regulatory pathways, could be one of the ways to provoke brai
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Over expression of Glo can
2021-12-08

Over-expression of Glo-1 can suppress inflammatory responses. Methylglyoxal mediates vascular inflammation in human endothelial AZD2932 [33], indicating that Glo-1 may attenuate inflammation via eliminating methylglyoxal. Glo-1 knockdown mediated methylglyoxal accumulation provokes collagen expressi
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KNK437 br Experimental br Acknowledgment This work was suppo
2021-12-08

Experimental Acknowledgment This work was supported in part by a Grant-in-Aid for Scientific Research from the Ministry of Education, Culture, Sports, Science and Technology of Japan. Glyoxalase I (GLO1) is a zinc enzyme that catalyzes the isomerization of a hemithioacetal, formed from glut
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Our overall goal is to develop selective
2021-12-08

Our overall goal is to develop selective compounds for low-affinity/high-capacity transporters inhibitors (i.e. OCT1–3 and PMAT), and provide the field with much needed, specific pharmacological tools to study these transporters. In our initial efforts, we synthesized halogen substituted analogs and
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A pooled overall survival analysis at year showed no
2021-12-08

A pooled overall survival analysis at 1year showed no difference in survival between the two study arms, although these studies were not designed or powered to demonstrate a survival benefit. Among the 979 total patients in both ROMANA 1 and 2, about 55% continued on to the ROMANA 3 trial. That tria
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We addressed the role of GSNOR mediated T cell
2021-12-07

We addressed the role of GSNOR-mediated T-cell activation in HHcy-accelerated atherosclerosis in vivo by two mouse models. Generated for the first time, GSNOR-/-ApoE-/- double knock-out mice showed decreased atherosclerosis in aortic roots in response to HHcy. The specificity of GSNOR ablation in T
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TP-0903 The physiological role of lactate induced antilipoly
2021-12-07

The physiological role of lactate-induced antilipolytic effects is less clear. It has been speculated that GPR81 mediates the inhibition of lipolysis during intensive exercise, a condition which results in high systemic lactate plasma concentrations 9, 10. Owing to oxygen shortage resulting from int
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En el caso de la foliculitis decalvante
2021-12-07

En el caso de la foliculitis decalvante (FD), se ha publicado un estudio multicéntrico español de 82 pacientes en el que se concluye que el tratamiento que consigue una mayor efectividad (mejora en 15/15 pacientes tratados) y un mayor periodo de remisión postratamiento (7,2 meses) es la combinación
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br Concluding remarks Several orphan GPCRs have expression p
2021-12-07

Concluding remarks Several orphan GPCRs have expression profiles that indicate they are worthy of consideration as therapeutic targets. This view can be supported via various transgenic techniques, and it would be interesting to have wide-ranging phenotypic information on GPR35 knockout mice. Bas
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