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hydroxydopamine OHDA is a selective catecholaminergic neurot
2025-02-06
6-hydroxydopamine (6-OHDA) is a selective catecholaminergic neurotoxin mainly used to generate lesions in the nigrostriatal pathway in rats (Ungerstedt, 1968). The most common use of 6-OHDA is via unilateral injection into the rat medial forebrain bundle (MFB). DA depletion, nigral DA cell loss, and
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br Diabetes and obesity fit or fat
2025-02-06
Diabetes and obesity: fit or fat; sugar or not: the autophagic verdict Type 2 diabetes and obesity are among the most emerging health problems worldwide. The factors that are responsible for the establishment of diabetes include decreased BMP-2 cytokine production, rise in adiposity, and an incre
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Recent studies showed that the increased
2025-02-06
Recent studies showed that the increased expression of Aurora B kinase directly proportional to the tumor invasion and metastasis [61]. The Aurora B kinase regulates the PI2K/Akt signaling pathway has a significant role in tumor invasion and metastasis that leads to phosphorylation of GSK3β on ser 9
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In this review we will present the traditional
2025-02-06
In this review, we will present the traditional and actual strategies to study orphan receptors and identify their ligands. An extensive description of the orphan GPCR field has been published in 2013 by Davenport et al. [22]. Therefore, we will focus on the deorphanizations that were reported since
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br Experimental Procedures br Acknowledgments
2025-02-06
Experimental Procedures Acknowledgments This work was supported by NIH/National Human Genome Research Institute (NHGRI)R00 HG006922 and NIH/NHGRIR01 HG008974 (to J.G.), the Huntsman Cancer Institute, and the Women’s Cancers Disease-Oriented Team at the Huntsman Cancer Institute. Research repor
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mTOR agonist In mice the Tfm mutation increased
2025-02-05
In mice, the Tfm mutation increased the anxiety-state assessed in the novel object and in light/dark box tests, whereas no changes were detected in the open field or elevated plus maze tasks (Zuloaga et al., 2008). As for Tfm rats, this seemed to be related to an increased HPA response to stress. Th
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The evidence points toward a role for
2025-02-05
The evidence points toward a role for 12/15-LO activity in WAT in modulating chronic local inflammation and subsequent systemic metabolic decline in the obese state. However, little is known as to the role of 12- and 15-LOs in BAT. Indeed, in addition to WAT, platelet- and leukocyte-type 12-LO are e
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br Downstream signalling of AKT A consensus phosphorylation
2025-02-05
Downstream signalling of AKT A consensus phosphorylation motif has been described for AKT substrates: R-X-R-X-X-S/T-B where X represents any amino EAI045 cancer treatment and B represents bulky hydrophobic residues (Alessi, Caudwell, Andjelkovic, Hemmings, & Cohen, 1996). Numerous AKT substrates
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Since the cloning of ARs in the beginning of the
2025-02-05
Since the cloning of ARs in the beginning of the 1990s, the efforts to characterize them have led to the accumulation of a substantial amount of experimental data. Decades of site-directed mutagenesis (SDM; Box 1) studies, in combination with pharmacological data and computational modeling, have pav
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We further analyzed selected hit
2025-02-05
We further analyzed selected hit compounds for their ability to inhibit human AdK in intact cells. Human 1321N1 astrocytoma Omega-3 receptor antagonist were utilized which were found to express AdK. The whole cell assay was performed using a 96-well format. The standard AdK inhibitor 5-iodotubercid
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On the basis of the above information we
2025-02-05
On the basis of the above information, we designed a new series of benzothiazole–piperazine derivatives (–) that have the aforementioned structural requirements (). Benzothiazole is an important ring system in the drug discovery studies of AD. There are several benzothiazole compounds that show pote
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Conclusion Twenty compounds with dinitrobenzoate scaffold
2025-02-05
Conclusion Twenty compounds with 3,5-dinitrobenzoate scaffold were synthesized and evaluated using cell-free and HWB assays for their 5-LOX inhibition activities. Compared to the parent compound, six compounds show significantly increased enzyme inhibition activities. The best compound, 3-tolyl 3,5
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Oil lignans br Introduction The vacuolar ATPases
2025-02-03
Introduction The vacuolar ATPases (V-ATPases) are ATP-driven proton pumps that play important roles in both normal and disease processes [1], [2], [3], [4], [5]. V-ATPases within cells function in such processes as intracellular membrane traffic, protein processing and degradation, coupled transp
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br Introduction Hepatocellular carcinoma HCC is an aggressiv
2025-02-03
Introduction Hepatocellular carcinoma (HCC) is an aggressive and malignant cancer detected in clinical practice, as it is the third key reason of tumor-related deaths worldwide, with > 800, 000 mortalities every year (Torre et al., 2015). Current treatments for HCC are surgical therapy, liver tra
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Overexpression of AR in a transgenic mouse model leads to
2025-02-01
Overexpression of AR in a transgenic mouse model leads to a capsular cataract phenotype involving proliferation and formation of a fibrotic plaque of cells reminiscent of cells at the posterior Lurasidone HCl in PCO [17]. To investigate the molecular mechanism that could link AR expression to this
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