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Initially the synthesized compounds from were evaluated for
2022-04-11
Initially, the synthesized compounds from were evaluated for human GSNOR potency before generating additional SAR in order to understand scaffold feasibility and required functionality as illustrated in . Commercially available 4′-hydroxy-[1,1′-biphenyl]-4-carboxylic pyruvate dehydrogenase kinase i
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AZ 628 br Materials and methods br
2022-04-11
Materials and methods Results Discussion Chronic neuroinflammation underlies the pathogenesis of HAND (Saylor et al., 2016, Sodhi et al., 2004). Infected immune cells release viral proteins and inflammatory factors which act on microglia, astrocytes, and neurons to produce the synaptodendri
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Compared to methadone or morphine buprenorphine is a partial
2022-04-11
Compared to methadone or morphine, buprenorphine is a partial mu-opioid agonist, which shows high affinity for, and slow dissociation from, mu-opioid receptors. This maintenance of homeostasis may help to counter the development of an overt withdrawal syndrome, and may explain the lower risk of deve
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The occurrence of MDR in cancer patients undergoing
2022-04-11
The occurrence of MDR in cancer patients undergoing chemotherapy can be mimicked in the laboratory by culturing cancer Wnt-C59 in the presence of chemotherapeutic drugs, thereby enforcing the evolution of acquired drug resistance. This has been described in multiple model systems including the rhab
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In our study we observed elevation
2022-04-11
In our study, we observed elevation of the fluorescent intensity in the layers without synaptic contacts (OS, ONL, INL, and GCL). In the enzyme-linked fluorescence assay system, released glutamate is catalyzed by the enzyme on the surface of a quartz glass. Therefore, the diffusion of glutamate onto
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CaCl was from the Radiochemical Centre
2022-04-09
45CaCl2 was from the Radiochemical Centre (Amersham, UK), NaVO3 was from Reachim (Moscow, Russia). Tetrodotoxin was purchased from Calbiochem, DTNB from Merck, Darmstadt, Germany. Nifedipine was synthesized in the Institute of Drug Research, Modra, Slovakia and was kindly provided by Dr. Zdeno Mahrl
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Herein we describe the development of
2022-04-09
Herein, we describe the development of second generation GSM compounds aimed at improving critical physicochemical properties while maintaining the potent activity of the parent AGSM. Ligand design focused on identifying heterocyclic replacements for the hydrophobic D-ring as a means to improve ADME
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vitamin d receptor Zn is the second most
2022-04-09
Zn2+ is the second most abundant trace metal in many cells and neurons in the brain. It regulates cellular functions such as gene expression, epigenetic enzymatic activity, protein structural stability, and neuronal plasticity. Zn2+ is particularly abundant in the cortex and limbic system, including
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Ru II complexes have been reported
2022-04-09
Ru(II) complexes have been reported to be both duplex and G-quadruplex structure stabilizers, and potent anticancer agents [[11], [12], [13], [14]]. Barton, Norden, as well as Ji groups have provided detailed information about recognition and reactions of classical duplex DNA by Ru complexes [[47],
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br Acknowledgments R Dalmann has obtained a bourse Cifre gra
2022-04-09
Acknowledgments R. Dalmann has obtained a “bourse Cifre” (grant 304/2011) from the ‘Association Nationale de la Recherche Technique’ and Bristol-Myers-Squibb. Introduction Endocannabinoids, their molecular targets (receptors), their synthetic and degrading enzymes and proteins that transport
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EZH mutations or amplifications have been found in
2022-04-09
EZH2 mutations or amplifications have been found in a broad spectrum of human cancers including B cell lymphoma, ovarian cancer, breast cancer, melanoma, bladder cancer, gastric cancer, and other cancers (Kim and Roberts, 2016). Given the evidence of EZH2 as a cancer driver, numerous efforts have be
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Evidence suggests that phosphorylation increases synaptotagm
2022-04-09
Evidence suggests that phosphorylation increases synaptotagmin affinity for the SNARE complex [15], [128]. It is, however, unclear how this might affect release. Synaptotagmin has been identified as part of the minimal vesicle docking machinery in chromaffin AS-605240 [129]. Thus, phosphorylation o
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Our results on the other hand shows that
2022-04-09
Our results, on the other hand, shows that there is no upregulation of ETBR on the spinal cord after SCI, but there is a significant difference of mRNA on days 2, 7 and 28 on the SCI group on the spinal cord and no changes on the DRG, suggesting that the spinal cord injury may reduce the renovation
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Renal disease is characterized by aberrant
2022-04-08
Renal disease is characterized by aberrant fibrotic remodeling of renal tissue, elevated apoptosis in kidney tissue, and eventual organ failure. In addition, patients with renal disease are more likely to suffer from systemic hypertension due to oxidative damage (reviewed in Ref. [18]). Treatment of
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br The SRP SR Heterodimer GTPase
2022-04-08
The SRP/SR Heterodimer: GTPase Tangos Drive Co-Translational Protein Targeting SRP and SR mediate a universally conserved protein targeting pathway responsible for the delivery of 25–30% of newly synthesized proteome to the eukaryotic endoplasmic reticulum (ER) or the bacterial plasma membrane 11
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