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Synthesis pharmacological evaluation for the binding at hA h
2024-09-14
Synthesis, pharmacological evaluation for the binding at hA, hA and hA ARs, and efficacy at hA subtype of the synthesized compounds, together with the assessment of their theoretical ADME properties were the guidelines in this preliminary drug discovery investigation. The synthetic pathways which y
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sVRPs were more sensitive to ABT than MSRs
2024-09-14
sVRPs were more sensitive to ABT-702 than MSRs. This result agrees with previous reports that the activation of A1 receptors more potently inhibits sVRPs than MSRs (Nakamura et al., 1997, Otsuguro et al., 2009). Importantly, sVRPs are thought to reflex C-fiber-evoked nociceptive transmission. Nocice
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The theoretical calculations of ADME parameters molecular we
2024-09-14
The theoretical calculations of ADME parameters (molecular weight (MW), log P, topological polar surface are (tPSA), number of hydrogen donors (nON) and acceptors (nOHNH), and volume) and DLS are presented in along with the violations of Lipinski’s rule. According to these data, all compounds (–) c
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Several tertiary prevention studies are currently underway e
2024-09-13
Several tertiary prevention studies are currently underway examining the use of dutasteride for prostate cancer treatment: (1) during expectant management of prostate cancer, (2) after radical prostatectomy in men at high risk for relapse, and (3) in men with metastatic disease. The Reduction by Dut
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Among the AXL positive tumors
2024-09-13
Among the AXL-positive tumors that we screened, the TNBC cell line MDA-MB-231 showed the highest AXL expression level. Additionally, AXL protein levels were higher in TNBC patient samples than in other breast cancers. Considering the difficulty of, and the urgent need for, effective treatments of TN
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br Exocytosis of GLUT by autophagy br
2024-09-13
Exocytosis of GLUT4 by autophagy Conclusion Conflict of interest Ethics statement Antigen processing and presentation Adaptive immune response has to be instructed to identify and eliminate specific pathogens or foreign entities defined by their antigenic determinants. Processed antig
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The phylogenetic relationship demonstrates that both bovine
2024-09-13
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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From an historical perspective ligands for GPCRs adrenaline
2024-09-13
From an historical perspective, ligands for GPCRs (adrenaline, serotonin, Benzamil or morphine, to name a few) have been identified before their receptor counterparts, at a time when the concept of receptor itself was controversial [15]. Although many cognate receptors for endogenous ligands were ra
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The apoptosis promoting Bcl family
2024-09-13
The apoptosis-promoting Bcl-2 family includes BH3-only proteins (e.g., Bim, Bid and Bad) and multiple-domain proteins (e.g., Bax and Bak). At the time of apoptosis stimulation (e.g., DNA damage), only the BH3-only protein is activated, directly or indirectly promoting Bax/Bak oligomerization, changi
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br Experimental procedures br Results br Discussion Although
2024-09-13
Experimental procedures Results Discussion Although previous studies have indicated that astrocyte aromatase plays a role in nociceptive processes (O'Brien et al., 2015, Smeester et al., 2016), the mechanisms responsible for the regulation of aromatase and its involvement in nociception rem
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Apelin APJ triggers a variety of cellular
2024-09-13
Apelin/APJ triggers a variety of cellular signaling pathways (Fig. 1). Recent studies from our laboratory showed that apelin-13 induces vascular smooth muscle cell (VSMC) proliferation by the upregulation of Cyclin D1 expression, which is involved in an ERK-dependent activation of Jagged-1/Notch3 si
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In addition to peroxyl radicals the most
2024-09-13
In addition to peroxyl radicals, the most found radical forms in biological systems, some of assays took into account other free radicals such as superoxide anion, hydroxyl, hydrogen peroxide, singlet oxygen and peroxynitrite. ORAC procedure was also modified using different radical sources such as
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Tumor tissues often experience hypoxia owing to accelerated
2024-09-13
Tumor tissues often experience hypoxia owing to accelerated growth rates of malignant cells, accumulation of metabolic products, disorganization of tumor blood vessels, and high interstitial fluid pressures (Makino et al., 2001). In response to AAD treatment, tumor vascular density often decreases t
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br Eprosartan The AT R antagonist eprosartan is approved
2024-09-13
Eprosartan The AT1R antagonist eprosartan is approved for the treatment of essential salicin and may be administered using a convenient once-daily regimen. The drug is a well-tolerated and effective antihypertensive agent with benefit in the secondary prevention of cerebrovascular events, indepe
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Of the cardiovascular studies involving ARBs reported renal
2024-09-13
Of the cardiovascular studies involving ARBs, 3 reported renal outcomes. In the Losartan Intervention For Endpoint study, albuminuria was observed less frequently in the losartan than in the atenolol arm (7% vs. 13%; p=0.002) (5). In the Candesartan Antihypertensive Survival Evaluation in Japan tri
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