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However although in vitro studies in heterologous systems ha
2024-10-28
However, although in vitro studies in heterologous systems have provided very important indications of potential novel pharmacology, the studies with endogenous receptors in native tissues are essential to provide evidence for GPCR heteromerization in vivo and to confirm its physiological relevance.
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Here we report discovery of highly selective pan Aurora kina
2024-10-28
Here we report discovery of highly selective pan-Aurora kinase inhibitors through phenotypic screening. The co-crystal structure of Colistin Sulfate bound in the ATP binding site of Aurora A is described, and provides insight into the possible structural basis for the selectivity of the interactio
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The first objective of the present study
2024-10-28
The first objective of the present study was to investigate the impact of ageing on arginase activity in tissues which exhibit age-related impairments in their function. The second objective was to determine whether l-arginine supplementation modulated the effect of ageing on arginase activity. The
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In our study we provide evidence for the
2024-10-26
In our study we provide evidence for the existence of an endosome-lysosomal pathway for the proteolytic degradation of AR triggered by its interaction with the ESCRT-I component TSG101. The following findings of this study support this notion: (1) We showed that TS101 interacts with endogenous or ec
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Cancers that responded to immune checkpoint inhibitors
2024-10-26
Cancers that responded to immune checkpoint inhibitors were shown to present a type I interferon (IFN) signature in the TME 33, 34. Type I IFNs positively regulate the expression of tumor antigens and their crosspresentation by DCs to tumoricidal CTLs. Furthermore, CD8+ T cell develops full effector
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Circulating adrenal derived stress hormones
2024-10-26
Circulating adrenal-derived stress hormones, epinephrine and corticosterone mediate their tissue effects through adrenergic (AR; α and β) and glucocorticoid (GR) receptors. AR are widely distributed throughout the body and although epinephrine is a prototypical agonist for all types of AR, the selec
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br Detection and possible treatments for prostate cancer
2024-10-26
Detection and possible treatments for prostate cancer PC can be diagnosed, by screening for prostate-specific antigen (PSA) and after diagnosis, treatments may include intense observation, radical prostatectomy, radiation, chemotherapy, hormone therapy or vaccination depending on the type and sta
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The potential use of derivatives belonging to this
2024-10-26
The potential use of derivatives belonging to this series as therapeutic agents mostly depends on their pharmacokinetics and pharmacodynamics. The pharmacokinetic phase includes absorption, distribution, metabolism and excretion (ADME) of the studied compounds. Therefore, preliminary data for theore
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Changes in actin microfilaments are mediated by changes in
2024-10-26
Changes in Repaglinide microfilaments are mediated by changes in extracellular matrix, mechanical stimulation or growth factors intracellular signaling. We observed significant changes in a number of intracellular signaling pathways associated with changes in actin dynamics during hMSCs differentiat
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br Oxidative microbe killing and V ATPase Oxidative
2024-10-25
Oxidative microbe killing and V-ATPase Oxidative killing of phagocytosed microorganisms is predominately achieved through the uptake of large quantities of molecular oxygen by the infected cell and the activity particularly of the NADPH oxidase complex on phagosomes (Savina et al., 2006) and the
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Analysis of ASK crystal structures
2024-10-25
Analysis of ASK1 crystal structures as well as an investigation of how bms-536924 4 might bind were undertaken to understand opportunities for engaging Gln756. To this end a docking model derived from PDB 3VW622 was used to predict the binding mode of amide 4 in the ASK1 active site as shown in Fig
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Furthermore because most of foods and beverages have been co
2024-10-25
Furthermore, because most of foods and beverages have been consumed after processing, researchers have focused on the effects of processing (e.g. blanching, cooking, drying, cooling, freezing, high-pressure treatment, pulsed electric field) on total antioxidant capacity of foods. In general, there w
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Although little is known about the etiopathogenesis of preec
2024-10-25
Although little is known about the etiopathogenesis of preeclampsia, this syndrome has a major impact on maternal and fetal health worldwide, since it is responsible for 10–15% of maternal deaths [16], [17], preterm births, intrauterine growth restriction (IUGR), and fetal deaths [2]. In developing
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Although our sample size is not enough to
2024-10-25
Although our sample size is not enough to conclude that there is no great genetic variation of the AR gene in most New World monkeys, it would be reasonable to state that the microsatellite region in the exon 1 of the androgen receptor gene of New World monkeys (platyrrhine) is relatively shorter th
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AMP activated protein kinase AMPK is composed of and subunit
2024-10-25
AMP-activated protein kinase (AMPK) is composed of α-, β-, and γ-subunits [17,18]. Phosphorylation of α-subunit at Thr-172 residue is essential for AMPK activation [17,18]. The serine/threonine kinase coordinates metabolic pathways in response to energy supply and demand [17,18]. Studies have shown
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