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In this study we provide biochemical and immunohistochemical
2022-04-18
In this study we provide biochemical and immunohistochemical evidence for the localization of the glycine transporter GLYT1 in synaptic vesicles. Previously, it was thought that GLYT1 was exclusively a glial protein (Zafra et al., 1995a). However, due to a partial discrepancy between mRNA and protei
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FPS-ZM1 AFB Fapy dG has been
2022-04-18
AFB1-Fapy-dG has been long recognized as a substrate for nucleotide excision repair [24,25]. However, we recently demonstrated that this lesion is removed by FPS-ZM1 excision repair. We showed that DNA glycosylase NEIL1, a member of the Fpg/Nei glycosylase family, could excise AFB1-Fapy-dG from sit
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To examine the possible role of mGluRs in the LH
2022-04-18
To examine the possible role of mGluRs in the LH/PFA in the hypercapnic ventilatory response, a nonspecific antagonist of mGluRs, MCPG, was microinjected into the LH/PFA. MCPG elicited a significantly increased hypercapnic ventilatory response in awake rats, but not during sleep, in the light and da
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br Materials and methods br Results Aberrant A has
2022-04-18
Materials and methods Results Aberrant Aβ has been suggested to be an initiating factor for glutamate excitotoxicity in AD pathology. To investigate whether Aβ1-42 alters glutamate uptake in astrocytes, neurons, and astrocyte-neuron co-cultures, we used synthetic Aβ1-42 peptide. Aβ1-42 has fas
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In summary this study shows that
2022-04-18
In summary, this study shows that compound 4d has strong clinical potential as an efficient GLP-1/GCGR agonist exhibits weight-lowering, lipid-regulation and diabetes-protective effects and plays an important role in the prevention and therapy of diet induced obesity and dyslipidemia. The present st
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Extensive pharmacological and structural analysis
2022-04-18
Extensive pharmacological and structural analysis shows GCGR antibody REMD-477 competitively blocks GLC binding to the GCGR with 30-pM binding affinity, and can fully inhibit the receptor activity at low nanomolar concentrations in Ac-DEVD-AFC 14, 17, 20. Functionally identical to REMD-477, REMD2.5
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However ghrelin has a short half life of
2022-04-18
However, ghrelin has a short half-life of 15–20 min, because it is a natural peptide containing 28-amino acids, its clinical usefulness as a therapeutic agent may be limited (Mosińska et al., 2017; Vestergaard et al., 2007). Hence, many efforts have been made to elucidate the smallest segment of ghr
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Inhibitors of the G rdos effect include the
2022-04-18
Inhibitors of the Gárdos effect include the Ca2+-channel blocker nitrendipine with an IC50 of ∼103nM (Ellory et al., 1992, Ellory et al., 1992); its mode of action is likely to be from direct blockage of K+ flux through the Gárdos channel (Ellory et al., 1992, Ellory et al., 1992), and the peptidic
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br Gap junctions hemichannels and connexins Molecular charac
2022-04-18
Gap junctions, hemichannels and connexins: Molecular characteristics and function Cell-to-cell communication is of extreme importance in tissue homeostasis, which is maintained by transmission of regulatory signals (Fig. 1). Intercellular communication via gap junctions (GJs) represents one of th
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Interestingly GAL has also been shown to be co
2022-04-18
Interestingly, GAL has also been shown to be co-expressed and/or secreted in luteinizing hormone releasing hormone (LHRH) (Merchenthaler et al., 1991, Marks et al., 1994) and kisspeptin (KISS) neurons (Porteous et al., 2011). Furthermore, GAL was shown to stimulate luteinizing hormone (LH) secretion
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The overall decrease in consummatory drive seen in rodents t
2022-04-18
The overall decrease in consummatory drive seen in rodents treated with naltrexone in previous studies is in accordance with the effects seen with mice treated with SNAP 37889 in this study. While it may seem inappropriate to use a broad-acting drug like SNAP 37889 that suppresses overall consummato
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DAMPs are endogenous danger signals
2022-04-18
DAMPs are endogenous danger signals that can initiate and perpetuate a noninfectious cathepsin g during cell death [23]. HMGB1 is a well-studied nuclear DAMP in various types of regulated necrosis and has been implicated in the pathogenesis of infection and sterile inflammation. Our current data ind
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maprotiline australia br Expression and Purification of LSD
2022-04-16
Expression and Purification of LSD1 Proteins In Vitro Enzymatic Assays Analysis of LSD1 Demethylase Activity Acknowledgments Conflict of Interest Statement: Y.S. is a cofounder of Constellation Pharmaceuticals, Inc. and is a member of its scientific advisory board. Y.S. is also a consu
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Histone acetylation is regulated by two
2022-04-16
Histone acetylation is regulated by two groups of enzymes, histone acetyltransferases (HATs) and deacetylases (HDACs), with antagonizing functions (Wang et al., 2009b). Among members of HATs, p300 and CBP are homologous. Both are global transcriptional co-activators (Ogryzko et al., 1996), and play
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L-Homopropargyl Glycine receptor SCH is a H R receptor antag
2022-04-16
SCH-497079 is a H3R receptor antagonist introduced by Schering-Plough, without any publicized pharmacological and structural information. A Phase II clinical trial assessment of SCH-497079 on weight has been completed in a multicenter, randomized, parallel-group and placebo-controlled study in obese
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