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br Funding M I is supported by European
2021-10-28
Funding M.I. is supported by European Research Council (ERC) Consolidator Grant 725038, Italian Association for Cancer Research (AIRC) Grant 19891, Italian Ministry of Health (MoH) Grant GR-2011-02347925, Lombardy Foundation for Biomedical Research (FRRB) Grant 2015-0010, the European Molecular B
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Through the analysis of various synthetic GPR agonists
2021-10-28
Through the analysis of various synthetic GPR40 agonists as reported in literature, we found that a number of these compounds contained a phenylpropanoic Dantrolene, sodium salt motif which was inspired from naturally occurring medium to long chain fatty acids. For instance, in the early period of
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neuropeptides br Introduction When human red blood cells hRB
2021-10-28
Introduction When human red blood neuropeptides (hRBC) are suspended in depolarising Ringers, they respond by opening a non-selective voltage-dependent cation pathway, the NSVDC channel, which is permeable to mono- and divalent cations [1], [2], [3]. In patch clamp experiments on excised hRBC ins
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(-)-Bicuculline methiodide synthesis Comparison of dlGALRs d
2021-10-28
Comparison of dlGALRs deduced amino (-)-Bicuculline methiodide synthesis sequences with that of human GALRs demonstrate that the GALR1 ortholog sequences have diverged less than those of GALR2. Since often duplicate genes undergo divergent evolution through sub-functionalization, loss or gain of new
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Recently they reported an enyne chemotype agonist
2021-10-28
Recently, they reported an enyne chemotype agonist (21, Fig. 13) with low lipophilicity, small polar surface area (PSA) and high potency (Clog P=3.8, tPSA=37 A2, EC50=20nM), further derived from TUG-424. The compound endowed fast oral GSK 0660 (tmax=15min) and a decent pharmacokinetic profile, a sat
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The knowledge that piroxicam competes with ligands that bind
2021-10-28
The knowledge that piroxicam competes with ligands that bind to FPR may be of importance for a deeper understanding of the anti-inflammatory effects possessed by this NSAIDs. It has recently been reported that not only phagocytes but also platelets express FPR on their cell surface and that these re
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In cardiomyocytes mechanical stress builds up via
2021-10-28
In cardiomyocytes mechanical stress builds up via FAs and the related costamere structures, and excessive stress can cause cardiac hypertrophy. Cardoso et al. (2016) report a comprehensive study that demonstrates the link between stress-induced FAK activation and a FAK-mediated initiation of a trans
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Focal adhesion kinase Fakir et al also known as
2021-10-28
Focal adhesion kinase (Fakir et al., 2006), also known as non-receptor tyrosine kinase (PTK2), is a 125-kDa protein that regulates cell migration, adhesion, proliferation, and survival (Tavora et al., 2014; Yang et al., 2016; Tian et al., 2017). Many studies have observed FAK overexpression and/or h
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The present findings demonstrate for the first time in
2021-10-28
The present findings demonstrate for the first time in immature rats that hippocampal infusion of ET-1 results in a rapid and long-lasting decrease in regional cerebral blood flow (rCBF) and oxygen saturation (pO2). These data are in accord with the results of studies and adult animals, which have s
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A subsequent modeling study by a different group
2021-10-27
A subsequent modeling study by a different group was based on the bovine rhodopsin homology model using the 1L9H construct [38]. However, the site-directed mutagenesis data and docking suggested that the niacin-binding pocket is different to that described in the aforementioned report, but similar t
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Molecular modeling studies also revealed insignificant diffe
2021-10-27
Molecular modeling studies also revealed insignificant differences in ligand-receptor interaction energies between R and S enantiomers of LPCs or their 2-OMe-analogues, suggesting that enantiomers of a particular structure should exert similar GPR119-mediated biological effect. Indeed, when studied
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Many studies support that the increase
2021-10-27
Many studies support that the increase of P4 improves embryonic survival and reduces embryonic losses in ruminants [6,[18], [19], [20]]. However, experimental results are variable, contradictory and often inconclusive results. Certain studies showed that administration of GnRH or hCG after artificia
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Alpha synuclein AS is a protein located
2021-10-27
Alpha synuclein (AS) is a protein located in presynaptic terminals of neurons that functions in recycling and storage of neurotransmitters [17]. Under conditions of inflammation and oxidative stress, AS proteins misfold and accumulate into Cap Firefly Luciferase [81], [90]. The aggregates of misfold
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Overall the multiple nucleic acid hybridization method is us
2021-10-27
Overall, the multiple nucleic W-7 hydrochloride hybridization method is useful for detecting specific transcripts within tissues of nematodes. The present study suggests that Peq-pgp-11 and Peq-pgp-16 mRNAs are expressed in many tissues of Parascaris. Our results indicate that Pgps could protect ne
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br Results br Discussion Our cardiomyocyte
2021-10-27
Results Discussion Our cardiomyocyte-specific GR knockout mice did not show spontaneous cardiac hypertrophy unless pressure overload was given to the heart. This finding is somewhat different from previous work of a cardiomyocyte-specific GR UCB 35625 mouse model using GR-floxed mice with lox
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