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For the first series we decided to verify the effects
2025-02-20

For the first series we decided to verify the effects induced, on the ALR2 inhibitory properties, of an additional steric hindrance on the carbon in α position with respect to the carboxylic group, by introducing a methyl group (R2=Me). Therefore, we synthesized a series of new α-alanine derivatives
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dgat inhibitor Growing evidence indicates that GRKs can exer
2025-02-20

Growing evidence indicates that GRKs can exert different effects within the cell depending on the stimulus, cell type, and localization [97], [121]. In this sense, we were the first to demonstrate a mitochondrial localization for GRK2 [122], later confirmed by other investigators [123], establishing
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Beside activation of adenosine receptors A
2025-02-20

Beside activation of adenosine receptors (A2a.1, A2a.2, A2b) by FSK treatment, the expression of adenosine receptors was also upregulated, when embryos were exposed to inhibitors (SU5416 and DAPT) alone and also combined with FSK. Our data imply that adenosine receptor was associated with a positive
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The first suggestions that the cleaved intracellular domain
2025-02-20

The first suggestions that the cleaved intracellular domain of APP, AICD, might transit to the nucleus and hence selectively regulate gene transcription arose from analogies with the Notch receptor signalling system where similar intra-membrane proteolysis occurs [84], [85] and it was later confirme
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szl australia The extent to which GPCR oligomerization
2025-02-20

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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Application of the broad acting HTR antagonist methiothepin
2025-02-20

Application of the broad-acting 5-HTR antagonist methiothepin (Bard et al., 1996, Hoyer et al., 1994, Peroutka, 1990) converted the TBS-induced response of both thalamocortical and intracortical A1 synapses from LTP to LTD, an effect that was mimicked by the selective 5-HT2R antagonist ketanserin (L
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br Conflicts of interest br Acknowledgments The authors ackn
2025-02-20

Conflicts of interest Acknowledgments The authors acknowledge National Institute for Medical Research Development (NIMAD) project no. 940943 and National Research Institute for Science Policy (NRISP) no. 1456 for financial support of this work. AM appreciates National Institute for Genetic Eng
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The phylogenetic relationship demonstrates that both bovine
2025-02-20

The phylogenetic relationship demonstrates that both bovine and porcine 12/15-LO is more related to the human enzyme than the rabbit enzyme, despite the fact that the rabbit reticulocyte enzyme is a 15-lipoxygenase. The rabbit is one single species that expresses a 12/15 LO with 15-LO activity while
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APJ receptors have a amino acid
2025-02-19

APJ receptors have a 380 amino Mubritinib sequence with a characteristic G-protein structure, including seven transmembrane domains and post-translation modification sites for phosphorylation, palmitoylation and glycosylation along with association sites for β-arrestin (O'Dowd et al., 1993). APJ re
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Dopaminergic neurons are vulnerable to oxidative products an
2025-02-19

Dopaminergic neurons are vulnerable to oxidative products and inflammatory responses; these processes may play important roles in the etiology of PD. Because glial nampt inhibitor are the main generators of inflammatory responses in the CNS, the possibility that PD results from glial cell dysfuncti
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Regardless of the initial treatment most patients with advan
2025-02-19

Regardless of the initial treatment, most patients with advanced NSCLC experience relapse and disease progression [15]. A subpopulation of immediate concern and clinical need is patients who have advanced NSCLC that is especially aggressive, which is usually defined as disease that rapidly progress
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Dual acting RAAS blockade and neprilysin inhibition has been
2025-02-19

Dual-acting RAAS blockade and neprilysin inhibition has been evaluated in several clinical HF trials. In PARADIGM-HF [6,7], LCZ696 was superior to enalapril in reducing mortality and HF hospitalizations in symptomatic patients with HF with reduced EF. Augmented benefits on maladaptive cardiac remode
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A phase I trial has recently evaluated
2025-02-19

A phase I trial has recently evaluated enzalutamide, an anti-androgen agent, in patients with ER- and AR-positive advanced BC to estimate safety and tolerability of enzalutamide therapy alone or in association to anastrozole, exemestane or fulvestrant [65]. The results of major clinical trials with
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br AR expression in breast tissue Although androgenic signal
2025-02-19

AR expression in breast tissue Although androgenic signalling is chiefly associated with the development and maintenance of primary and secondary male characteristics, especially during puberty when the testes are by far the major source of testosterone, the AR also plays important functions in f
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In our sequential model for tau and
2025-02-19

In our sequential model for tau and Aβ deposition, we included the tau deposition in the medial temporal npy receptor in the absence of Aβ deposition, which is a pathological definition of primary age-related tauopathy (PART). Although the tau pathologies in PART and AD are almost identical in thei
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