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The excellent potencies selectivities and
2023-01-14

The excellent potencies, selectivities and improved PK associated with the piperazine class triggered more extensive off-target screenings of the highlighted compounds. A screen of more than 100 enzymes, receptors, and ion channels resulted in activity at the norepinephrine transporter (NET). This m
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The present work has implications for our thinking about the
2023-01-14

The present work has implications for our thinking about the effects of antidepressant (e.g. SSRIs) use on maternal care in depressed mothers which consist of approximately 10–20% of all mothers (Gjerdingen and Yawn, 2007, Susser et al., 2016), and more than 40% of depressed mothers are prescribed w
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br Conflict s of interest br Retinopathy of prematurity
2023-01-14

Conflict(s) of interest Retinopathy of prematurity (ROP) is a leading cause of childhood blindness Retinopathy of prematurity (ROP) is a disease of premature infants which disrupts normal retinal vascularization (Fleck and McIntosh, 2008). With increased survival of extremely premature infants
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enfuvirtide mg At the last follow up nine patients had disco
2023-01-13

At the last follow-up, nine patients had discontinued pyridostigmine within the first year postoperatively. Only one patient required pyridostigmine at a higher dose, but this was accompanied by successful weaning of prednisolone. None of the 5 patients who were on pyridostigmine treatment alone pri
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Using constant potential amperometry and electrochemical enz
2023-01-13

Using constant potential amperometry and electrochemical enzyme-based biosensors selective for choline—and, therefore, an accurate readout of L-690,330 release (Baker et al., 2015; Bruno et al., 2006a; Parikh et al., 2004, 2007)—tonic and phasic release of acetylcholine were measured simultaneously
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To date more than different
2023-01-13

To date, more than 50 different mutations in the gene have been described (Human Gene Mutation Database at the Institute of Medical Genetics in Cardiff: SRD5A2 Gene: http://www.hgmd.cf.ac.uk). Most of them are missense mutations but premature stop codons and deletions leading to non-functional or su
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In order to improve the
2023-01-13

In order to improve the methodology of the synthesis of steroidal derivatives, our goal was the investigation of aza-Michael addition of different N-nucleophiles to 16-dehydropregnenolone in the presence of [DBU][OAc] as catalyst and reaction medium. Michael addition of electron deficient steroidal
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Compound was docked into the
2023-01-13

Compound was docked into the active site of Aurora B kinase using Tripos sybyl-X ver. 2.1.1. The crystal structure of human Aurora B kinase cocrystallized with its potent inhibitor VX-680 was used for the docking analysis (PDB ID: ). The most likely binding conformations were selected based on the
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V ATPase is a complex enzyme that is composed of
2023-01-13

V-ATPase is a complex enzyme that is composed of several subunits, which are assembled into two domains: trans-membrane (V0) and cytosolic (V1) domains [3,5]. Epididymal epithelial KB SRC 4 of rats has been reported to contain V-ATPase which is distributed at the apical pole of the narrow and clear
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br Experimental and simulation section br Acknowledgments Fi
2023-01-13

Experimental and simulation section Acknowledgments Financial support for this work was provided by the National Natural Science Foundation of China (No. 81101688). We would like to thank NC State University High Performance Computing Center for providing us computing resources, and Dr. Lihui
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Since immunoassays cannot specifically quantify
2023-01-12

Since immunoassays cannot specifically quantify each apelin peptide, a more reliable approach, mass spectrometry (MS) has been used recently to quantify and characterize apelin fragments in plasma. Using this technology, Zhen et al. showed that [Pyr-1]-apelin-13 was the major apelin form present in
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br Conclusions In summary KLA isolated
2023-01-12

Conclusions In summary, KLA isolated from K. senegalensis exerted the anti-inflammatory activity via inhibiting the activation of NF-κB, AP-1, AKT and upregulating p38 MAPK/Nrf2/HO-1 signaling in LPS-stimulated RAW 264.7 and BV-2 Topiroxostat (Fig. 9). These properties provide a potential mechani
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Here we found that AMPK directly phosphorylates EZH at
2023-01-10

Here we found that AMPK directly phosphorylates EZH2 at Thr311 to disrupt its interaction with SUZ12 and to inhibit PRC2 enzymatic activity, which is supported by the increased expression of PRC2-repressed genes. Furthermore, the T311E-EZH2 mutant that mimics AMPK-mediated phosphorylation status sup
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AMP activated protein kinase AMPK is composed of and
2023-01-10

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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A limitation of the NIA AA
2023-01-10

A limitation of the 2011 NIA-AA recommendations was that biomarkers were grouped into just two categories—amyloid and tau-related neurodegeneration. Tauopathy and neurodegeneration were placed into the same biomarker category. In persons with only AD, it is reasonable to assume that neurodegeneratio
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