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Camptothecin is a type of topo
2022-04-08

Camptothecin is a type of topo I inhibitor, and its prodrugs irinotecan and topotecan have been approved by the FDA for clinical cancer treatment. It has been reported that SAHA can enhance the cytotoxicity of camptothecin derivatives in several cancer cell lines20., 21., 22., 23., 24.. Taking the s
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Another interesting approach is to use
2022-04-08

Another interesting approach is to use partial agonists as starting point to develop specific antagonists like done in earlier decades [64], [65]. Possible indications for an attenuation of the NO/sGC signalling pathway might be specific neuronal disorders: an involvement in the aetiology of migrain
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br S NO signalling during
2022-04-08

(S)NO signalling during the plant immune response Redox signalling molecules must exhibit specificity for their target substrate. Moreover, a given redox-based modification must be reversible to ensure transient signalling. Oxidative cysteine (Cys) modifications are integral to a variety of redox
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Modulation of the cannabinoid system has been reported to ex
2022-04-08

Modulation of the cannabinoid system has been reported to exert anti-parkinsonian properties through different mechanisms. On one hand, cannabinoids have neuroprotective properties in different rodent models of PD, both through a CB1/CB2 receptor-independent mechanism (Lastres-Becker et al., 2005) a
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T0901317 synthesis Abn CBD induced changes reduced microglia
2022-04-08

Abn-CBD induced changes (reduced microglial cell density, T0901317 synthesis size and a lower density of ramification) in the microglial morphology that could be compatible with a blockade of the neuroinflammation provoked by MPTPp. The absence of GPR55 transcripts in microglial cells in striatum an
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br The mode of binding of ligands to
2022-04-08

The mode of binding of ligands to GPR35 As noted above, although kynurenic lactacystin is an agonist at GPR35, this is true for neither kynurenine [8] nor kynurenic acid ethyl ester [13]. This implicates a key role for the carboxylate group in binding and/or activation of GPR35. Importantly, in
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With this goal in mind we proceeded to
2022-04-08

With this goal in mind, we proceeded to explore the C5-heteroaryl class of pyrazole-acids. Initial efforts, focused on a thiophene replacement, demonstrated little improvement. The 2-thiophene derivative (0.25μM and 0.24μM), a surrogate to the phenyl moiety, demonstrated only a modest boost in acti
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The mechanisms by which NEIL and NEIL
2022-04-08

The mechanisms by which NEIL1 and NEIL3 excise bulky adducts and unhook ICLs are unclear. Structures of NEIL1 are available only in complex with DNA containing small lesions 79., 80., 81., and the single available structure of NEIL3 lacks DNA (Figure 5D,E) [73]. Nonetheless, comparison of the two st
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To assess whether this coupling mechanisms might operate
2022-04-08

To assess whether this coupling mechanisms might operate also in a native system of untransfected cells, we select a cell line SH-SY5Y neuroblastoma that is known to express both the dopamine transporter and the M-currents (Jiang et al., 2004; Wickenden et al., 2008). These experiments were performe
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Accordingly it is tempting to speculate
2022-04-08

Accordingly, it is tempting to speculate that the maintenance of a stimulus representation in the A2 state for a short period of time after the presentation of a specific stimulus (i.e. self-generated priming) may rely upon GluR-A-dependent synaptic plasticity. If this were the case, GluR-A Phos-tag
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Multiple mechanisms have been suggested by which glucagon ca
2022-04-08

Multiple mechanisms have been suggested by which glucagon can increase energy expenditure although none have been conclusively proven to be responsible. Both enhanced gluconeogenesis and enhanced protein turnover secondary to hyperglucagonaemia have been suggested as the reason for the increased met
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We have previously shown in the
2022-04-08

We have previously shown in the same time frame reported here (10 min) that AG was not degraded into DAG [29] and that the half-life of AG in human serum is ∼10 min [49]. However, we cannot rule out in this study that there is not breakdown to DAG that could contribute to the levels of 125I-ghrelin
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The regulatory effects of NADPH oxidase
2022-04-07

The regulatory effects of NADPH oxidase on ferroptosis might also relate to neuroinflammation. Although ferroptosis can trigger inflammatory responses in the brain, neuroinflammation, in turn, can also modify ferroptosis. It has been reported that inflammatory conditions such as those found in neuro
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br Materials and methods Patients charts were
2022-04-07

Materials and methods Patients’ charts were reviewed retrospectively, and 165 consecutive patients (82 with cancer and 83 without cancer) who either started edoxaban (Lixiana®, Daiichi-Sankyo, Tokyo, Japan) therapy for the treatment of VTE or were switched from other oral anticoagulants to edoxab
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NMS-873 The present study was therefore
2022-04-07

The present study was therefore conducted with three aims; (1) we tested the effect of IRL-1620, a selective ETB receptor agonist, on the analgesic tolerance to morphine and oxycodone in mice; (2) we determined the expression of ETA receptors and ETB receptors in the NMS-873 of morphine and oxycodo
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