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br Funding br Introduction l Dihydroxyphenylalanine l DOPA
2024-08-17
Funding Introduction l-3,4-Dihydroxyphenylalanine (l-DOPA) is the gold-standard treatment for the motor symptoms of Parkinson's disease (PD); however, its chronic use induces severe motor complications that eventually limit its long-term efficacy (Bastide et al., 2015). The most disabling side
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br Clinical realities br Commentary on uses of
2024-08-17
Clinical realities Commentary on uses of selective 17,20 lyase inhibitors If continued monitoring of these same parameters along with tracking of circulating ACTH in human trials confirms these new drugs are the long sought after 17,20 lyase inhibitors, then we may for the first time be able t
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In response to DSB the lesion recognition factor Mre
2024-08-17
In response to DSB, the lesion recognition factor Mre11-Rad50-Nbs1 (MRN) complex helps the recruitment of ATM to the damage site and its activation by phosphorylation [29]. However, whether UV-damage recognition factors directly influence ATR and ATM recruitment and their phosphorylation is not clea
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br Concluding Remarks Despite major
2024-08-16
Concluding Remarks Despite major advances in the development of antibody and small-molecule tumor angiogenesis inhibitors, therapy resistance, both innate and acquired, continues to limit further survival improvements for patients with cancer. Preclinical models of localized primary tumors and me
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br Conclusion We have identified three non
2024-08-16
Conclusion We have identified three non-competitive inhibitors of the human and porcine APN with Ki values in the μM range, by combining virtual screening and kinetic assays. Molecular docking simulations suggest these novel inhibitors block APN activity by an alternative mechanism to Zn coordina
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In this study we designed and synthesized two
2024-08-16
In this study, we designed and synthesized two ALK PROTACs (degraders), 5 (MS4077) and 6 (MS4078), by linking ceritinib and pomalidomide [45] through two different linkers. Using human ALCL and NSCLC cells, we characterized both compounds in a battery of assays to demonstrate their effects on reduci
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br Discussion AhR is a receptor that
2024-08-16
Discussion AhR is a receptor that binds to a great variety of lipophilic compounds, in particular those containing at least one aromatic ring (Abel and Haarmann-Stemmann, 2010, Guyot et al., 2013, Hahn, 2002). The main known function of this receptor is to induce the metabolism of these compounds
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Because activation of HT A receptor is capable
2024-08-16
Because activation of 5-HT2A receptor is capable of facilitating dopamine cell activity and dopamine release (Bortolozzi et al., 2003), and this action of dopamine is known to mediate rat maternal behavior, especially maternal motivation (Afonso et al., 2007, Febo et al., 2010, Li and Fleming, 2003,
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Similar to V the temporal neocortex of mammals including the
2024-08-16
Similar to V1, the temporal neocortex of mammals, including the primary auditory cortex (A1), is densely innervated by 5-HT fibers originating mainly in the dorsal raphe nucleus (Campbell et al., 1987, Harding and Paxinos, 2004, Törk, 1990), and the major (R)-PFI 2 hydrochloride of 5-HTRs are expres
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Adenosine is a ubiquitous homeostatic
2024-08-16
Adenosine is a ubiquitous homeostatic purine nucleoside that accumulates extracellularly in response to metabolic stresses such as hypoxia and inflammation. Activation of either G protein-coupled adenosine receptors (ARs; A1R, A2AR, A2BR, and A3R) by extracellular adenosine can modulate cell signali
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The anorexic effect observed when AR is infused into
2024-08-16
The anorexic effect observed when AR231630 is infused into the VTA could be the result of the DA release inhibition, as previously described [11]. However, there is also a hedonic aspect in feeding that possibly involves dopaminergic mechanisms of reward. Helm et al. showed a functional link between
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Vortioxetine is a multimodal antidepressant that acts as
2024-08-16
Vortioxetine is a multimodal antidepressant that acts as an inhibitor at the serotonin (5-HT) transporter (SERT), an agonist at 5-HT1A receptors, a partial agonist at 5-HT1B receptors, and an antagonist at 5-HT1D, 5-HT3 and 5-HT7 receptors (Bang-Andersen et al., 2011, Sanchez et al., 2015). Based on
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In addition to the data provided by the
2024-08-15
In addition to the data provided by the Ki16425 treatment in the K/BxN arthritis model, new findings from the study of two new LPA receptor antagonists confirm the involvement of the LPA pathway in the pathogenesis of experimental arthritis. In the study by Miyabe et al., the authors reported the tr
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br Results br Discussion Autophagy
2024-08-15
Results Discussion Autophagy is considered as an important process in physiological and pathological ovarian function. It is related mainly to follicular atresia and CL regression (for review see [20]). However, an involvement in luteal cell survival is also proposed [21], [22]. The present st
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Congruously our findings of voltage electrode clamping
2024-08-15
Congruously, our findings of voltage-electrode-clamping assays indicate that hipN851K mutation mediates partial loss of Na+/K+-ATPase pump currents, also confirming our thesis that hipN851K mutation acts as a hypomorph. As demonstrated here by our external electrical stimulation studies and ECG reco
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