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Compared to the other histamine
2022-06-08

Compared to the other (±)-Nutlin-3 receptor subtypes, the H3 receptor exhibits rather complex pharmacology, being subject to extensive splicing, leading to two major (H3-445 and H3-365) and possibly more functional human receptor isoforms; for a comprehensive review please see Leurs et al. (2005) a
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br Introduction Hepatitis B virus HBV infects about billion
2022-06-08

Introduction Hepatitis B virus (HBV) infects about 2 billion people worldwide and is a leading cause of liver disease including liver fibrosis, cirrhosis and hepatocellular carcinoma (Trepo et al., 2014). Most current HBV therapies are based on nucleos(t)ide analogs and pegylated interferon alpha
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Recently a receptor for nicotinic
2022-06-08

Recently, a receptor for nicotinic acid, named GPR109A (also known as HM74a in man or PUMA-G in the mouse) has been identified (Lorenzen et al., 2001, Lorenzen et al., 2002, Soga et al., 2003, Tunaru et al., 2003, Wise et al., 2003). This receptor, a member of the 7 transmembrane G-protein coupled f
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Previous researches about ghrelin focused primarily on gastr
2022-06-08

Previous researches about ghrelin focused primarily on gastrointestinal functions [30], energy balance [31], weight [32], and more recently on anxiety [33], [34], [35] and depression [36]. Here, we provided the first demonstration that chronic peripheral or central ghrelin treatment to CUMS rodents
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In this study an galactosidase gene
2022-06-07

In this study, an α-galactosidase gene, GalA, from a Aspergillus oryzae strain RIB40 [14] was artificially synthesized. To produce high levels of secretory expression in Pichia and facilitate its industrial application, we systematically investigated the gene dosages and the role of the ERSAs, namel
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To ensure the induction of CYP
2022-06-07

To ensure the induction of CYP enzymes by several inducers, specific monooxygenase activities of variously induced, uninduced and pooled liver microsomes were compared (Fig. 3). Although 3-MC, phenobarbital, acetone, and dexamethasone could induce CYP1A-, CYP2B-, CYP2E1-, and CYP3A-selective enzyme
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Acetylation of histones by histone acetyltransferases stimul
2022-06-07

Acetylation of histones by histone acetyltransferases stimulates gene expression by relaxing Prednisone receptor structure, allowing access of transcription factors to DNA, whereas deacetylation of histones by histone deacetylases promotes chromatin condensation and transcriptional repression. Rece
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Ticlopidine HCl Histamine which was used as the agonist
2022-06-07

Histamine, which was used as the agonist, had low potencies in our functional experiments when compared to its affinity from binding studies (e.g. Lim et al., 2005). This phenomenon is related to the fact that the coupling of the presynaptic receptor to the transduction machinery and the final funct
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At the present time there
2022-06-07

At the present time, there are several clinical trial studies being conducted with a variety of indications for pitolisant. Various studies in different phases assess different aspects of pitolisant efficacy and safety in narcoleptic patients (Szakacs et al., 2017) (NCT01800045, NCT02611687, NCT0343
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The observed tendency for higher plasma lactate levels in
2022-06-07

The observed tendency for higher plasma lactate levels in the aerated thermal exposure suggests increased reliance on melk inhibitor metabolism to maintain function. This finding is supported by a recent study that observed an increased ṀO2 in European perch (Perca fluviatilis) exposed to a hyperox
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We are pursuing a hit to lead medicinal
2022-06-07

We are pursuing a hit-to-lead medicinal chemistry campaign to optimize inhibitors of the HBV RNaseH. Here, we report the activity of seven new HIDs and nine new HPDs, with significant improvements in in vitro potency and cytotoxicity profiles for the HPD compounds. Materials and methods Result
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Among the GSK inhibitors available in market lithium is
2022-06-07

Among the GSK-3 inhibitors available in market, lithium is probably the only example and the oldest one. Some molecules, both natural and synthetic, such as maleimide derivatives, staurosporine (from the bacterium Streptomyces storosporeus), indole derivatives such as indirubin (used since long in t
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br Author contributions Animal experiments real time PCR and
2022-06-07

Author contributions Animal experiments, real time PCR and western blots were performed at the Department of Physiology, CIMUS, University of Santiago de Compostela and Department of Cell Biology, Physiology and Immunology, Instituto Maimónides de Investigaciones Biomédicas (IMIBIC) / Reina Sofia
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Some years ago it has been described that CD
2022-06-07

Some years ago, it has been described that CD45RA+ CD62L+ naïve CD4+ T mavacamten can be further differentiated into two distinct subpopulations by analysing their surface expression of CD31(Kimmig et al., 2002a; Kohler and Thiel, 2009; Kohler et al., 2005b). CD31+ thymicnaive CD4+ T cells are enri
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We suggest that the FRET enhancement observed when the modif
2022-06-07

We suggest that the FRET enhancement observed when the modified mD1 protein containing Acd at position 28 was excited at 260nm (), may differ from the diminution in fluorescence observed following excitation at 280nm due to the excitation of different transitions in Trp (i.e., the L and L transition
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