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Molecular docking quantitative structure activity relationsh
2024-12-02

Molecular docking, quantitative structure–activity relationship (QSAR) and high-throughput virtual screening (HTVS) studies have a very widespread use in computer-assisted drug design.25, 26, 27, 28 Suvannang et al. used the published X-ray crystallographic data to examine known aromatase inhibitors
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Dabrafenib Mesylate synthesis br Introduction The apelin rec
2024-12-02

Introduction The apelin receptor (angiotensin receptor-like 1, APJ) is a seven transmembrane receptor (7TMR) that belongs to the class A peptidergic G protein-coupled receptors (GPCR) superfamily [1]. The endogenous ligands of APJ are the different isoforms of apelin (namely apelin-13, −17, and −
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br Material and methods br Results br Discussion Aminopeptid
2024-11-29

Material and methods Results Discussion Aminopeptidase N is a transmembrane protease present in a wide variety of human tissues and cell types (endothelial, epithelial, fibroblast, leukocyte). APN expression is dysregulated in inflammatory diseases as well as in solid and hematologic tumors
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br Introduction Diabetes mellitus DM is a chronic metabolic
2024-11-29

Introduction Diabetes mellitus (DM) is a chronic metabolic disorder characterized by elevated levels of glucose in the blood. Type 1 diabetes is characterized by insufficient insulin production and needs a daily administration of insulin. Actually, no prevention is known for Type 1 diabetes. Type
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br Introduction Nausea and vomiting are among the most
2024-11-29

Introduction Nausea and vomiting are among the most distressing side effects associated with chemotherapy in cancer patients (Billio et al., 2010). Severe emesis can negatively affect a patient's nutritional state, ability to work and motivation, which can, in turn, interfere with the clinical co
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We investigated the role of ABT treatment in MAPKinase activ
2024-11-29

We investigated the role of ABT 702 treatment in MAPKinase activation in mouse microglia in vitro. In Fig. 7D immunocytochemistry results revealed that Iba1 and p-ERK1/2 co-localized in LPS induced mouse microglia. In our previous study we have reported that LPS activates ERK1/2 phosphorylation (Ahm
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Brain damage diseases such as cerebral ischemia brain trauma
2024-11-29

Brain damage diseases, such as cerebral ischemia, brain trauma and infection are characterized by the increase in oxygen free radicals. Therefore, deeper understanding of the character and mechanism of free radical damage in the brain is important to ultimately relieve diseases and promote recovery
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In fact serotonin is a major modulator of dopaminergic DA
2024-11-29

In fact, serotonin is a major modulator of dopaminergic (DA) neuronal activity through the 5-HT2C receptor. Studies have shown that the selective 5-HT2C receptor agonist Ro60-0175 blocks the burst-firing of mesolimbic DA neurons, which project from the ventral tegmental area (VTA) to the nucleus acc
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In conclusion we have produced some highly
2024-11-29

In conclusion, we have produced some highly potent inhibitors of P450 in comparison to the standard Nitazoxanide KTZ. Also, due to the limited specificity of these compounds against lyase in comparison to the 17α-OHase component, these compounds would be expected to have a major impact on corticost
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ptc124 Aurora kinases are a conserved
2024-11-29

Aurora kinases are a conserved family of serine/threonine kinases that are important for the transition through mitosis and amplification and overexpression of Aurora kinases have been implicated in ptc124 and transformation. Aurora B is located at the centromere and controls aspects of kinetochore
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Suspecting that ACL might regulate the expression or activit
2024-11-28

Suspecting that ACL might regulate the expression or activity of myogenic transcription factors, Das knocked down MyoD and found that such intervention abolished the effect of ACL on fast MyHC expression and that, conversely, MyoD overexpression partially rescued reduced fast MyHC expression caused
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The objectives of this study were to investigate the
2024-11-28

The objectives of this study were to investigate 1) the mRNA and protein expression of apelin and APJ in porcine ovarian follicles of different sizes, and their immunolocalization and concentrations in follicular fluid and ovarian follicle, and 2) the direct effect of recombinant human apelin-13 on
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br Implementation of sacubitril valsartan into clinical prac
2024-11-28

Implementation of sacubitril/valsartan into clinical practice Following on from the results of PARADIGM-HF, sacubitril/valsartan was given regulatory approval for use in patients who conform to the main inclusion criteria of the trial; NYHA functional class II–IV, reduced left ventricular ejectio
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We found that decreased Ng
2024-11-28

We found that decreased Ng levels lead to a lower threshold for LTD induction at L4–L2/3 synapses. Previous studies in hippocampal slice culture have shown that LTD at individual synapses induces spine elimination at both the targeted synapse and selective neighboring synapses when spines are monito
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N terminally extended antigenic peptide precursors that
2024-11-28

N-terminally extended antigenic peptide precursors that survive cytosolic degradation and enter the ER, need to be further processed by ERAP1 and/or ERAP2, in order to acquire the right length required for MHCI binding. ERAP1 (ERAAP in mouse) is an IFN-γ-inducible, metalloaminopeptidase that trims N
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