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Ryoichi et al modified potent
2023-09-22
Ryoichi et al. modified potent clinical candidate VX-680 (6) with 3-cyano-6-(5-methyl-3-pyrazolamino)pyridine as Aurora kinase inhibitor. Substituted cyano pyridine derivative (7) inhibited proliferation of HCT-116 cells with an IC50 value of 115 nM. It showed tumor inhibition in mice model at a dos
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In the last decade the zebrafish
2023-09-22
In the last decade, the zebrafish has emerged as a valuable vertebrate model to systematically dissect the genetic underpinnings of both vertebrate heart development and function [8,9], as well as distinct cardiac diseases such as congenital heart disease [10], cardiomyopathies [11,12] and cardiac a
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Recent progress has been made in translating animal findings
2023-09-22
Recent progress has been made in translating animal findings on memory performance and amnestic effects – that are largely determined by tonically active receptors in which α5 contributes to the benzodiazepine binding site. Based on the observation that deletion of this subunit led to improved spati
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br Introduction The apelin receptor angiotensin
2023-09-22
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 Methodology br Antibiotics in lakes br Antibiotic resista
2023-09-22
Methodology Antibiotics in lakes Antibiotic resistance genes in lakes Perspectives of study on Afuresertib mg and ARGs in lakes Conclusion This paper systematically reviewed the distribution of antibiotics and ARGs in global lakes. A total of 57 antibiotics reported at least once in
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br AR signaling and urothelial cancer
2023-09-22
AR signaling and urothelial cancer progression As shown in other types of malignancies, such as prostate cancer cells, it has been documented that androgens induce AR expression and its nuclear translocation as well as ARE promoter activity in urothelial cancer cells (Chen et al., 2003, Izumi et
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br Results br Discussion Cardiac dysfunction common complica
2023-09-22
Results Discussion Cardiac dysfunction, common complication of severe sepsis, is one cause of death in intensive care units. Accumulated evidence revealed the regulatory effect of autophagy on sepsis-induced cardiac dysfunction [15], [22], although the mechanisms in young and aging are not elu
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(-)-epicatechin br Conflict of interest statement br Introdu
2023-09-22
Conflict of interest statement Introduction Tanshinone IIA (Tan IIA) is a major active component of Salvia miltiorrhiza (S. miltiorrhiza), a well-known Chinese traditional medicine that is used for the treatment of cardiovascular and cerebrovascular diseases [1]. Tan IIA exhibits diverse pharm
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We find that the interaction of NSF and SNAP
2023-09-22
We find that the interaction of NSF and SNAP is critically involved in NMDAR-induced PICK1 unclustering. The binding of SNAP to NSF increases the ATPase activity of NSF, which is known to be essential for the unbinding of PICK1 from GluR2 (Hanley et al., 2002). Disruption of the association between
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The rescue of the behavioral deficit was associated
2023-09-22
The rescue of the behavioral deficit was associated with a significant reduction in the levels of both soluble and insoluble Aβ peptides and their deposition in the Deferiprone receptor of the same animals. In search for the mechanism behind the reduced amyloidosis, we assessed APP metabolism. Confi
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To determine the post translation
2023-09-21
To determine the post-translation modifications in chicken adiponectin, we isolated adiponectin from chicken adipose tissue by immunoprecipitation. Chicken adiponectin was then subjected to tryptic digestion and UPLC/MS/MS. The collagenous domain of chicken adiponectin was found to possess certain A
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Since the cloning of ARs in the beginning of
2023-09-21
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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Further investigations were concerned to study the mechanism
2023-09-21
Further investigations were concerned to study the mechanisms by which GABA modulates adenosine-mediated effects in hippocampal tissue. From these results it can be concluded that endogenous GABA exerts an inhibitory effect through GABAA receptors via a predominant adenosine-mediated action and this
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br Disclaimer br Conflicts of interest
2023-09-21
Disclaimer Conflicts of interest Role of the Sponsor Acknowledgements Funding/support: This project was supported by a grant from the Department of Surgery (R5129), Western University and by the Institute for Clinical Evaluative Sciences (ICES) Western site. ICES is funded by an annual g
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Moreover our present work suggests
2023-09-21
Moreover, our present work suggests that AXL could be a modulator of sunitinib response, at least for cell lines that present high endogenous levels of this RTK activation, since we observed an increased responsiveness to sunitinib in GNE-617 activated with AXL receptor ligand. A role for AXL in mol
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