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The typical pharmacophore for GPR agonists
2021-12-21

The typical pharmacophore for GPR40 agonists contains four parts: head (acid moiety), central (phenyl ring), linker and tail (aromatic carbocyclic or heterocyclic ring) [20]. On the other hand, the chemical features that are required for the PPARγ agonists include hydrogen bond donors and acceptors
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Taken together the four HRs couple with several
2021-12-20

Taken together, the four HRs couple with several different signaling pathways modulating various G-proteins (Fig. 1). Histamine H1R The H1R, including many other biogenic amine receptors, is one of the GPCR family members (see for a complete list e.g. http://www.gpcr.org/7tm/ or http://tools.gpc
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The metal nanoparticles of gold Au
2021-12-20

The metal nanoparticles of gold (Au), silver (Ag), Platinum (Pt), Palladium (Pd) and/or their composites are also being widely used to develop electrochemical sensors because of their unique advantages such as (i) ease in immobilization of receptor molecules, (ii) catalysis of electrochemical reacti
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The following are the supplementary data related to this art
2021-12-20

The following are the supplementary data related to this article. Transparency document Introduction Hypoxia is a pathological process that causes abnormal changes in metabolism, function and morphological structure of tissue because of insufficient oxygen supply. It's reported that hypoxia w
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In plants NO production is one of the early responses
2021-12-20

In plants, NO production is one of the early responses to stress (Tossi, Lamattina, & Cassia, 2009). Usually, NO signal transduction requires the involvement of downstream signaling compounds. We further investigated the effects of cGMP on GSK-3 expression. The data showed that LY83583 (a cGMP inhib
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Conjugated BAs via S PR also activate ERK and AKT
2021-12-20

Conjugated BAs via S1PR2 also activate ERK1/2- and AKT-signaling pathways leading to the growth and invasion of cholangiocarcinoma cells. The role of conjugated BAs via S1PR2 to regulate apoptosis or cancer progression remains to be dissected. Nevertheless, there is no doubt that the composition of
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Ketamine has recently been found to exert rapid
2021-12-20

Ketamine has recently been found to exert rapid and sustained antidepressant effect. Single dose ketamine can have an efficacy of up to 1 week [20]. Furthermore, ketamine is an effective drug against refractory depression [21,22]. The antidepressant mechanism of ketamine is still unclear. Whether CO
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Exposure of human and animals to
2021-12-20

Exposure of human and animals to MPTP can reproduce all the characteristic motor and non-motor signs of PD, in addition to mimicking the same responses and side effects to drugs used to treat PD [37], [38]. Anatomically, intoxication with MPTP induces the same selective loss of substantia nigra DA n
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Also a large number of small molecules are potent
2021-12-20

Also a large number of small molecules are potent G-quadruplex ligands that exhibit anti-proliferative activity in cells [39,48]. Several small molecules, for example cyclic naphthalene diimide derivative [43], cationic porphyrins [2,[49], [50], [51], [52]] and pentaheteroaryls [53], quinacridines [
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Regarding IAV types of hemagglutinin and types
2021-12-20

Regarding IAV, 18 types of hemagglutinin and 11 types of neuraminidase were described and none of the commercialized antiviral drugs are susceptible to protect against all strains that will emerge from the animal reservoir (Webby and Webster, 2003). The strong dependencies of influenza viruses on we
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Compounds were tested for GPR
2021-12-20

Compounds , were tested for GPR40 activity in a functional assay monitoring calcium flux in CHO inno-206 transiently transfected with human GPR40 gene. As shown in , compound was found to be a nanomolar GPR40 agonist, while compound was much less potent than . To explore the structure activity re
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Fig illustrates the different signaling pathways elicited
2021-12-20

Fig. 1 illustrates the different signaling pathways elicited or modulated by H3R activation. Collectively, the modulation of the release of histamine and other neurotransmitters through H3R activation could be linked to several neurological disorders such as sleep disorders like narcolepsy, Alzheime
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GSTP has an antiapoptotic activity that is mediated by
2021-12-18

GSTP1 has an antiapoptotic activity that is mediated by the inhibitory interaction with JNK1. Our data suggest that GSTP1 treatment is associated with a significant down-regulation of caspase expression. This might explain the reduction in infarct-related cardiomyocyte death and saving the cardiomyo
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The following are the supplementary data
2021-12-18

The following are the supplementary data related to this article. Authorship SLC and CGE performed the study conception and experimental design, wrote the paper and directed the activities of this work. ESM and JICA performed most of the degranulation assays, [Ca2+] measurements regarding to the
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Originally identified as a GPCR upregulated on Burkitt lymph
2021-12-18

Originally identified as a GPCR upregulated on Burkitt lymphoma cells upon Epstein-Barr virus infection (Birkenbach et al., 1993), Ebi2 was later found to play critical roles in immunity by regulating the migration of activated RG2833 to extrafollicular sites for early plasmablast responses (Gatto
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