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The extent to which GPCR oligomerization is
2024-08-03
The extent to which GPCR oligomerization is a regulated process still remains unclear. Reported effects of ligands on both GPCR homo- and heteromers are highly variable and depend on GPCR subtypes and the specific ligand used. According to our data, chronic treatment of mice with both paroxetine or
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Herein we disclose novel dihydropyrano c
2024-08-03
Herein, we disclose novel 2,4-dihydropyrano[2,3-c]pyrazoles that inhibit human ATX (hATX). Our results demonstrate and further support previous findings showing that a desired biological action can be achieved without targeting the catalytic site of the enzyme. Moreover, this study validated hen eg
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br COPD As in asthma also
2024-08-03
COPD As in asthma, also in COPD, increased expression of arginase has been reported, and tobacco smoke may increase expression of arginase in human subjects [46, 47]. Increased ADMA levels have also been reported in COPD, and both the increased expression of arginase and ADMA contribute to remode
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As with most G protein coupled receptors GPCRs
2024-08-03
As with most G protein-coupled receptors (GPCRs), sustained activation of APJ can cause desensitization and this has been reported to occur for APJ-mediated effects on cytoplasmic Ca2+ concentration, as well as for effects on activity of adenylyl cyclase, ERK and Akt (Ishida et al., 2004, Masri et a
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The subnuclear localizations of redox
2024-08-03
The subnuclear localizations of redox regulators is also largely unknown. The potential role of thiol reductases as transcription regulators or DNA repair molecules may suggest an association to DNA. In this way, the presence of a zinc finger domain potentially involved in protein/DNA interactions o
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3'-O-(2-nitrobenzyl)-2'-dATP With wide spread use of
2024-08-03
With wide-spread use of corticosteroids to combat inflammation and allergies, even children are susceptible to corticosteroid-induced muscle wasting. Although non-steroidal SGRMs that spare muscle and bone, but have significant anti-inflammatory effects, have been preclinically developed and tested,
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We designed SSOs that block APP
2024-08-03
We designed SSOs that block APP exon 17 splicing and induce the production of an alternatively spliced APP mRNA lacking exon 17 (APPΔex17). APPΔex17 mRNA encodes an APP protein isoform that lacks 49 ON123300 including the γ-secretase cleavage sites that give rise to the toxic, AD-associated Aβ42 pe
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br Introduction Diabetes mellitus DM is a chronic metabolic
2024-08-02
Introduction Diabetes mellitus (DM) is a chronic metabolic disorder characterized by elevated levels of glucose in the blood. Type 1 diabetes is characterized by insufficient insulin production and needs a daily administration of insulin. Actually, no prevention is known for Type 1 diabetes. Type
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Ac-DEVD-AFC Human testicular peritubular cells HTPCs are als
2024-08-02
Human testicular peritubular Ac-DEVD-AFC (HTPCs) are also the only human testicular cell type that can be isolated, cultured and studied in vitro (Albrecht et al., 2006, Mayerhofer, 2013). Results from recent studies indicate that their roles go beyond sperm transport and include immunological func
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In the previous study we demonstrated the importance of
2024-08-02
In the previous study, we demonstrated the importance of the mPFC postsynaptic 5-HT1A receptor in the sustained antidepressant effects, because a sustained antidepressant effect was obtained with intra-mPFC injection, but not systemic injection of 8-OH-DPAT, a 5-HT1A receptor agonist (Fukumoto et al
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In this study high concentrations
2024-08-02
In this study, high concentrations (0.5–4 mM) of thuringiensin were required to stimulate the basal adenylate cyclase activity Fig. 2, Fig. 3, Fig. 4, but low concentrations of thuringiensin (1–100 μM) were sufficient to inhibit the forskolin-stimulated adenylate cyclase activity in rat cerebral cor
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br Materials and methods br Results
2024-08-02
Materials and methods Results Discussion This study demonstrates that treatment with a selective adenosine kinase inhibitor ABT-702, thereby enhancing extracellular adenosine, can provide partial protection from age-related hearing loss in C57BL/6J mice. Chronic treatment with ABT-702, comm
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br Experimental section br Results and discussion br Conclus
2024-08-02
Experimental section Results and discussion Conclusion Acknowledgements This work was financially supported by Recruitment Program of Global Experts, and the Director Foundation of XTIPC, CAS, Grant No. 2015RC011. This work was also financially supported by Natural Science Foundation of
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In summary we could identify and experimentally confirm two
2024-08-02
In summary, we could identify and experimentally confirm two novel SBEs within the 5-LO promoter and we were able to demonstrate that TGFβ and SMADs stimulate 5-LO promoter activity. Moreover, an elevated 5-LO expression has been linked to different forms of leukaemia. Therefore, the influence of ML
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A promising target that is involved in the biosynthesis of
2024-08-02
A promising target that is involved in the biosynthesis of the precursor LTA4 is the 5-LO-activating protein (FLAP), which in vivo is seemingly indispensable for LT formation [8], [9]. FLAP, a member of the MAPEG family (membrane-associated proteins in eicosanoid and glutathione metabolism), is an i
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