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br Acknowledgements MC and PD were
2024-12-05
Acknowledgements MC and PD were funded by the Michael J Fox Foundation (Grant ID 9969). We would like to thank Pierluigi Saba, Francesco Traccis and Barbara Tuveri for their technical assistance. Introduction In the prostate, androgens play a crucial role in normal, BPH and cancerous growth b
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Our results showed suppressed autophagy in GECs under
2024-12-05
Our results showed suppressed autophagy in GECs under HAGG stimulation. Recently, people have paid more attentions on the roles of autophagy in lupus and tried to use autophagy regulators for therapy. Rapamycin could prevent the development of nephritis [49] and attenuate the established nephritis [
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In this paper we described synthesis biological
2024-12-05
In this paper, we described synthesis, biological evaluation and docking study of 3-aroyl-1-(4-sulfamoylphenyl)thiourea derivatives 4a–o as 15-lipoxygenase inhibitors. Results and discussion Conclusion We designed and synthesized a novel of thiourea derivatives containing phenylsulfonamide mo
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D-(-)-Salicin Two major categories of arginase inhibitors ha
2024-12-04
Two major categories of arginase inhibitors have been distinguished (Fig. 3): the first category comprises synthetic arginase inhibitors, which have been developed from the substrate l-arginine [35]; and the second category includes inhibitors derived from natural products [36]. The category of synt
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br STAR Methods br Acknowledgments We
2024-12-04
STAR★Methods Acknowledgments We thank Simcere Pharmaceuticals, Nanjing, China, for providing a rabbit anti-VEGF neutralizing monoclonal antibody. We thank Dr. Schlisio in the Ludwig Institute for Cancer Research, Karolinska Institute, for assistance with hypoxia assay. Y.C.’s laboratory is sup
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Based on structure activity relationship of several SARM tem
2024-12-04
Based on structure activity relationship of several SARM templates, Ligand Pharmaceuticals chose LGD2226 as their first clinical candidate (Miner et al., 2007). Although LGD2226 demonstrated myo- and osteo-anabolic activity and maintenance of sexual function in various preclinical models, the develo
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Following activation of mGluRs GRIP stabilized AMPARs appear
2024-12-03
Following activation of mGluRs, GRIP-stabilized AMPARs appear to be the primary target for endocytosis. Consistent with this model, we find that using siRNA to reduce GRIP1/2 expression blocks the AMPAR internalization and the synaptic depression mediated by mGluRs. Reductions in GRIP1/2 expression,
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br Introduction There are greater
2024-12-03
Introduction There are greater than five million Americans living with Alzheimer's dementia and more than 35 million people worldwide [1], and without a way to stop or slow the progression, there will be nearly a tripling of individuals affected by 2050 (13.8 million) [1]. The urgency to develop
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Imeglimin hydrochloride In our previous study we found that
2024-12-03
In our previous study we found that the total activity of aldehyde dehydrogenase in cancer Imeglimin hydrochloride of RCC is at the same level as in normal renal tissue [10]. These findings are similar to our results in serum patients with renal cancer. There is no significant difference between ALD
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Akt Inhibitor IV In these experiments recordings were perfor
2024-12-02
In these experiments, recordings were performed continuously in the homecage and during the first 5 days of training on a randomized forced alternation T-maze working memory task (Figures 1A, 1B, 3A, and 3B) (Kucewicz et al., 2011). Sleep and wake states were determined by simultaneous recording of
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The observation that vortioxetine blocks HT induced currents
2024-12-02
The observation that vortioxetine blocks 5-HT-induced currents in 5-HT3 receptor-expressing oocytes suggests that vortioxetine acts to functionally antagonize these receptors, and is in line with previously published data (Bang-Andersen et al., 2011). For example, Mørk et al. (2012) demonstrated tha
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Compound was docked into the active site
2024-12-02
Compound was docked into the active site of Aurora B kinase using Tripos sybyl-X ver. 2.1.1. The crystal structure of human Aurora B kinase cocrystallized with its potent inhibitor VX-680 was used for the docking analysis (PDB ID: ). The most likely binding conformations were selected based on the
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ARG I is one of the most important
2024-12-02
ARG I is one of the most important mammalian enzymes responsible for nitrogen metabolism since it comprises the main route for the elimination of excess nitrogen resulting from amino cdk9 inhibitor receptor and nucleotide metabolism [18]. ARG I deficiency leads to hyperargininemia, characterized by
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Several enzymes in serine and
2024-11-29
Several enzymes in serine and glycine metabolism have been proposed as biomarkers for cancer stage and prognosis. Phosphoglycerate dehydrogenase (PHGDH), phosphoserine phosphatase (PSPH), and serine hydroxymethyltransferase (SHMT) levels are high in TNBC and low in luminal-A breast cancers (Kim et a
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Most of the identified aldose reductase inhibitors possess u
2024-11-29
Most of the identified aldose reductase inhibitors possess undesirable effects like poor pharmacokinetic properties, hypersensitivity and Steven-Johnson Syndrome [1]. However, the main side effect is the lack of selectivity relative to aldehyde reductase (ALR1, EC 1.1.1.2). ALR1 plays the important
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