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Vortioxetine is a multimodal antidepressant that acts as an
2023-06-14

Vortioxetine is a multimodal antidepressant that acts as an inhibitor at the serotonin (5-HT) transporter (SERT), an agonist at 5-HT1A receptors, a partial agonist at 5-HT1B receptors, and an antagonist at 5-HT1D, 5-HT3 and 5-HT7 receptors (Bang-Andersen et al., 2011, Sanchez et al., 2015). Based on
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Having taken a step back from affinity to gain
2023-06-13

Having taken a step back from affinity to gain better exposure and solubility, we started work to replace the unstable oxazolinone, and address the selectivity over the hERG channel. Keeping in mind the binding mode of the series from crystal structures, triazole was identified as another mildly aci
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br Materials and methods br Results br Discussion
2023-06-13

Materials and methods Results Discussion CUs, which have been used as traditional medicine for thousands of years in East Asian countries, have the potential to be used for cancer chemoprevention and chemotherapy [17], [18], [19], [20]. CuB is one of the most promising agents as it is repor
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br Crystal structure ACLY protein is a homotetramer of
2023-06-13

Crystal structure ACLY protein is a homotetramer of four identical subunits [9]. Each polypeptide chain contains 1101 amino-acid residues [10]. The crystal structure of full-length ACLY protein is yet unresolved. However, Sun et al. recently succeeded in crystallizing chymotrypsin-truncated human
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Although several ARIs have reached various phases of clinica
2023-06-03

Although several ARIs have reached various phases of clinical experimentation however most of them have been withdrawn either due to an insufficient bioavailability, their poor efficacy or adverse side effects. Currently Epalrestat is in clinical use for the treatment of diabetic neuropathy. The sid
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TMC647055 Choline salt receptor Since natural and recombinan
2023-06-01

Since natural and recombinant glycoprotein hormones exhibit some differences in their carbohydrate structures, we checked whether this could affect the permissive effect on FSK-induced cyclic AMP response in MLTC-1 cells. Fig. 6 shows that the same sensitizing effect to FSK is observed with pituitar
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Moreover showed reduction in fibroblast growth factor induce
2023-05-30

Moreover, showed 73% reduction in fibroblast growth factor–induced neovascularization in a mouse corneal micropocket assay at a dose of 100mg/kg and 50% reduction at 50mg/kg. Both results were highly statistically significant (PPFI 3 have recently shown only moderate efficacy (40% inhibition) in an
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br Research perspective In vitro and in vivo studies have
2023-05-30

Research perspective In vitro and in vivo studies have demonstrated that increased LPA/ATX signaling contributes to cancer initiation and progression. Recent findings on the role of non-tumoral ATX in cancer progression and metastasis highlighted a new functional contribution for the microenviron
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In this report the natural compound
2023-05-30

In this report, the natural compound deguelin potently and dose-dependently suppressed Aurora B kinase activity in vitro, indicating that this compound is an effective Aurora B inhibitor. The docking study indicated that deguelin was docked into the ATP-binding pocket of Aurora B and formed hydropho
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In this study we observed the ATPase activity of
2023-05-30

In this study, we observed the ATPase activity of RaGroEL at various temperatures and metal ions conditions and the role of GroES in the ATPase activity of RaGroEL. Furthermore, we quantified the expression of groEL genes under different abiotic stresses, including temperature, pH, salt and oxygen s
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The tumor suppressor function of LOX in
2023-05-30

The tumor-suppressor function of 15-LOX-2 in normal prostate epithelial cells may be explained by the induction of replicative senescence [14,15]. Thus, 15-LOX-2 is overexpressed in age-dependent prostatic hyperplasia, but cell senescence may hinder progression to malignant transformation. Notwithst
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In pancreatic islets we found an increase in protein
2023-05-30

In pancreatic islets we found an increase in protein expression of leukocyte 12/15-LO that paralleled the metabolic decline characterized by severe hyperglycemia and reduced islet numbers. Similar increase in 12/15-LO expression by Western blot was found in the control mice, which have a normal meta
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In Rainey et al published the results of a
2023-05-30

In 2008, Rainey et al. published the results of a targeted compound library screen for potential inhibitors of the ATM kinase. In this study, the compound CP466722 was identified as a highly selective and rapidly reversible ATM inhibitor, which did not inhibit PI3K or related PIKK family members. Mo
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The reasons why antibiotic treatment
2023-05-29

The reasons why antibiotic treatment may be detrimental are diverse. First, it may result in disruption of multifaceted microbe–microbe, as well as microbe–host, interactions that are key for the maintenance of homeostasis within this ecosystem. This can lead to the expansion of pathogenic microorga
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In addition unconventional mechanisms of internalization can
2023-05-29

In addition, unconventional mechanisms of internalization cannot be ignored. It is generally believed that the conventional homologous internalization of a GPCR depends on the activation of G proteins, since GRK activation requires the pre-activation of G proteins (Fig. 2). Feng et al. demonstrated
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