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Most human diseases e g cancer diabetes and neurodegenerativ
2023-12-28

Most human diseases (e.g., cancer, diabetes, and neurodegenerative diseases) are complex and multifactorial. Several investigations in the literature focused on new multi-target drug development, which implies active pharmacophores incorporation in one scaffold (Meunier, 2008, Lazar et al., 2004, Te
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We also found that the size of mEPSC
2023-12-28

We also found that the size of mEPSC amplitude was reduced in unc-43 mutants, consistent with the decrease in synaptic GLR-1/GLR-2 heteromeric receptors. The decrease in mEPSC amplitude was not as great as that observed when measuring current in response to pressure application of glutamate. These d
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br Conclusions Our study confirms
2023-12-28

Conclusions Our study confirms that N-terminal mutations can affect Aβ fibril and oligomer formation, despite lying outside the core amyloid region of Aβ. Of the three factors that may influence Aβ-mediated toxicity (primary structure of Aβ, assembly structure and cellular responses), our results
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A has been reported to decrease insulin
2023-12-28

Aβ has been reported to decrease insulin receptors and impair insulin signaling in neurons, preventing phosphorylation of Akt and glycogen synthase kinase 3β (GSK-3β), downstream of insulin signaling, and to increase phosphorylation of tau protein causing neurofibrillary tangles (Tokutake et al., 20
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calcium ionophore br Functional repercussions of each trimmi
2023-12-28

Functional repercussions of each trimming pathway A main difference between the two pathways presented in Fig. 1 lies in enzyme kinetics and selectivity. In pathway #1, the substrate for ERAP1 is free peptide, and so both kinetics and selectivity are determined by interactions between the peptide
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In conclusion we identify in this report the molecular
2023-12-28

In conclusion, we identify in this report the molecular nature of the 12- and 15-lipoxygenases in M. mulatta and P. pygmaeus and also that the expression of the rhesus enzyme in lung epithelial cells is regulated by interleukin-4. The switch from a mainly 12-LO enzyme to a mainly 15-LO enzyme during
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The current study was designed
2023-12-28

The current study was designed to investigate the effects of the 12/15-LOX inhibitor, LOXBlock-1 (LB1) in mice using a FeCl3-induced distal MCAO model, and to test its utility in conjunction with subsequent thrombolysis with tPA, which is to date the only FDA-approved drug for acute stroke treatment
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It is well known that
2023-12-28

It is well-known that TCDD is the most potent ligand of AhR and it regulates gene expression, such as CYP1A1, via activation of AhR (Mimura and Fujii-Kuriyama, 2003). Besides Tomblin et al. (2016) have recently shown that TCDD via AhR regulated L-type amino AZD1152-HQPA synthesis transporter 1 expr
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CCK Octapeptide, non-sulfated Young et al described the role
2023-12-28

Young et al. [40] described the role of adenine monophosphate-activated protein kinase (AMPK) in the translocation of GLUT4 in the heart. The AMPK is activated during muscle contraction [74] by converting AMP to ATP. The adenosine analog, 5-aminoimidazole-4-carboxamide ribonucleotide (AICAR), is a c
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AMPK is an essential player in
2023-12-28

AMPK is an essential player in adiponectin signaling pathway that regulates energy metabolism. The fact that suppression of AMPK activity by compound C largely diminished candesartan-mediated inhibition of NFκB via blocking AT1 also suggests that the AT1-mediated effect is at least partly resulted f
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Thioguanine The subdivision of HT receptors started in the
2023-12-28

The subdivision of 5-HT receptors started in the 1950s by Gaddum and colleagues, when they realised that in the guinea pig ileum, the effects of 5-HT could be blocked in part by morphine (M), and in part by dibenzyline (D). Gaddum and Picarelli proposed two receptor classes, 5-HT M and 5-HT D (1957)
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A more versatile cellular delivery
2023-12-28

A more versatile cellular delivery system for adenosine was generated by engineering mouse embryonic stem cells to lack both MK-2461 of Adk (Fedele et al., 2004). Using a step-wise differentiation protocol (Okabe et al., 1996) Adk−/− ES cells were differentiated into transplantable adenosine-releasi
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br Conflict of interest br Ethics committee br Introduction
2023-12-28

Conflict of interest Ethics committee Introduction Severe combined immunodeficiency due to adenosine deaminase deficiency (ADA-SCID) is characterized by impaired function and differentiation of T, B, and natural killer (NK) cells. Non-immunological abnormalities may also occur, including fa
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Encouraged by this observation a systematic SAR
2023-12-28

Encouraged by this observation, a systematic SAR study on the A ring -alkoxy was conducted as summarized in . The A ring methoxy-containing KRCA-0008 was proven an optimal substituent in terms of potency after all and its bigger size derivatives were detrimental in both biochemical and H3122 cellula
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Whereas more research is needed to identify the precise mech
2023-12-27

Whereas more research is needed to identify the precise mechanism by which FIN exerts its antidyskinetic effect, the KH CB19 synthesis that it can negatively modulate dopaminergic transmission is also supported by our previous findings. Indeed, we have previously shown that FIN completely reversed t
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