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Another significant group of reductase inhibitors is the ste
2024-06-20
Another significant group of 5α-reductase inhibitors is the steroidal 3-carboxylic BINA synthesis derivatives (relevant examples in Fig. 5), which were designed to mimic the putative enzyme-bound enolate intermediate. This was achieved by introducing sp2-hybridized centers at C3 and C4 and an anioni
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Here we report discovery of highly selective pan Aurora
2024-06-20
Here we report discovery of highly selective pan-Aurora kinase inhibitors through phenotypic screening. The co-crystal structure of Rose Bengal bound in the ATP binding site of Aurora A is described, and provides insight into the possible structural basis for the selectivity of the interaction. T
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A disruption of lung barrier function caused
2024-06-20
A disruption of lung barrier function caused by PM2.5 has been observed in our experiments; however the underlying mechanism has not been investigated. Zhao et al. (2018) reported that PM2.5 down-regulated the expression levels of tight junction (TJ) proteins and resulted in nasal epithelial barrier
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The presence of crown like structures
2024-06-20
The presence of crown-like structures and inflammatory factors in the breast of obese patients is associated with considerable changes in intracellular signaling and a profound cellular dysfunction. Secreted pro-inflammatory factors can directly promote breast carcinogenesis as they have been report
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br Acknowledgements This work was supported in part
2024-06-19
Acknowledgements This work was supported, in part, by NIH grant R01-GM071760. Introduction The MADS box genes encode a eukaryotic family of transcriptional regulators involved in diverse and important biological functions. This class of proteins has been identified in yeasts, plants, insects,
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There are some limitations and
2024-06-19
There are some limitations and further experiments that are required. First, to our surprise, measurement of the cardiomyocyte cross-sectional area in Akt1−/−/iAkt2 KO mice showed comparable areas to WT mouse despite of reduced heart weight. In addition to measuring cardiomyocyte cross-sectional are
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Fig A shows a schematic representation of histological resul
2024-06-19
Fig. 2A shows a schematic representation of histological results according to the Franklin and Paxinos Mouse Brain Atlas (2001). The black circles represent the sites of drug infusion that were on-target within the amygdala. Gray circles represent the animals that had infusion locations outside the
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Serum soluble sCD is a shedding product from the ectodomain
2024-06-19
Serum soluble sCD21 is a shedding product from the ectodomain of membrane CD21 after B cell activation (Masilamani et al., 2003, Masilamani et al., 2004a, Masilamani et al., 2004b, Grottenthaler et al., 2006, Hoefer et al., 2008), which resembles the ligand-binding capacity of intact CD21 (Wu et al.
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br Introduction Myasthenia gravis MG is an autoimmune diseas
2024-06-19
Introduction Myasthenia gravis (MG) is an autoimmune disease in which antibodies against targets on the postsynaptic muscle membrane cause neuromuscular transmission failure. About 85% of patients with MG have autoantibodies against AZD0156 receptor (AChR) [1]. In AChR negative MG patients antib
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Using constant potential amperometry and electrochemical
2024-06-19
Using constant potential amperometry and electrochemical enzyme-based biosensors selective for choline—and, therefore, an accurate readout of Bialaphos sodium salt mg release (Baker et al., 2015; Bruno et al., 2006a; Parikh et al., 2004, 2007)—tonic and phasic release of acetylcholine were measured
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(-)-Quinpirole hydrochloride ATX LPA signaling in cancer is
2024-06-18
ATX/LPA signaling in cancer is also well known to promote chemotherapy and radiotherapy resistance [7]. Furthermore, others have recently shown that endothelial-derived ATX activity in renal cell carcinoma promotes renal tumorgenesis and acquired resistance to sunitinib through an IL-8-mediated mech
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Having taken a step back from affinity to gain better
2024-06-18
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
2024-06-18
Materials and methods Results To explore the potential role of autophagy in drug resistance, we firstly performed immunohistochemistry to compare the Pregnenolone Carbonitrile receptor of p62 in paired primary, metastatic, and recurrent tumor tissues from 26 ovarian cancer patients. The expre
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APJ is mainly coupled to PTX sensitive Gi o
2024-06-18
APJ is mainly coupled to PTX-sensitive Gi/o proteins [33], and thus, it is associated with the inhibition of adenylyl cyclase and the activations of PI3K/Akt signaling and MAPKs signaling pathways [23], [54], [55], [56]. In a previous study, apelin stimulations of the PI3K/Akt and/or the MAPK pathwa
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The objectives of this study were to investigate the
2024-06-18
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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