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A straightforward synthetic pathway was adopted to synthesiz
2022-12-09

A straightforward synthetic pathway was adopted to synthesize the target compounds as outlined in . The starting chloromethylquinazolinones (–) were synthesized from anthranilic 490 in two steps following reported procedures., , , The first step involves chloroacetylation of anthranilic acid using
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Introduction The lysosomal storage disorder Gaucher disease
2022-12-07

Introduction The lysosomal storage disorder Gaucher disease (Mendelian Inheritance in Man, OMIM #230800) results from the recessively inherited deficiency of lysosomal glucocerebrosidase (GCase, EC 3.2.1.45), caused by mutations in the gene GBA1 (MIM# 606463) located on chromosome 1q21. The enzymat
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Whereas more research is needed
2022-12-07

Whereas more research is needed to identify the precise mechanism by which FIN exerts its antidyskinetic effect, the Phosphoramidon Disodium Salt that it can negatively modulate dopaminergic transmission is also supported by our previous findings. Indeed, we have previously shown that FIN completel
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br Animals Female Sprague Dawley
2022-12-06

Animals Female Sprague Dawley (SD) rats, aged 3 months with body weight between 180-210 g were housed in cages and acclimatized to standardized lab conditions (temperature 23 ± 2°C, humidity 50 ± 5% and 12 h light-dark cycles). The rats were fed with standard rodent food pellet (Harlan Diet, Ross
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In the nineties we knew that
2022-12-06

In the nineties we knew that (-)baclofen was the stereo-selective ligand for the GABAB receptor which had been recognised by Norman Bowery as a receptor for GABA, which was different from the GABAA receptor (Hill and Bowery, 1981). GABAB receptor antagonists were also synthesised and made available
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This unsuspected antagonistic interaction of androgen with O
2022-12-05

This unsuspected antagonistic interaction of androgen with OXER1 could therefore explain the effect of plant derived compounds with this ligand-receptor system. For example, wedelolactone, a coumestan found in Eclipta alba (false daisy) and in Wedelia calendulacea that is the major component of ecli
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Since forskolin is known to act
2022-12-02

Since forskolin is known to act directly at the catalytic site of adenylate cyclases near the ATP binding (Tesmer et al., 1997), the synergistic and/or permissive effect of gonadotropins on FSK activity must occur at the level of AC itself or very near, at the level of one of its direct partner. The
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azd2171 receptor Previously we described that cadmium induce
2022-12-02

Previously, we described that cadmium induces a more pronounced, but not selective, cell death on primary cholinergic neurons from basal forebrain (Del Pino et al., 2014). Degeneration of septal cholinergic neurons from basal forebrain, as happens in AD, results in memory deficits (Scheiderer et al.
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During myeloid cell maturation expression of LO mRNA and
2022-12-02

During myeloid cell maturation, expression of 5-LO mRNA and protein is strongly induced (60–130-fold) by calcitriol (1,25(OH)2D3) and transforming growth factor-β (TGFβ) [6,7]. The upregulation of 5-LO mRNA transcription is mainly due to transcript elongation and mRNA maturation [8,9]. Interestingly
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Several tertiary prevention studies are currently underway e
2022-12-02

Several tertiary prevention studies are currently underway examining the use of dutasteride for prostate cancer treatment: (1) during expectant management of prostate cancer, (2) after radical prostatectomy in men at high risk for relapse, and (3) in men with metastatic disease. The Reduction by Dut
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porcine mg With regard to the first question subcellular
2022-12-02

With regard to the first question, subcellular fractionation studies revealed that BDK and PPM1K are clearly detectable in both the mitochondrial and cytosolic subcellular fractions, thus making it possible for these enzymes to interact with both the BCKDH and ACL substrates. The preferential presen
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br Mechanisms of GPCR internalization Like for
2022-12-02

Mechanisms of GPCR internalization Like for other types of receptors, prolonged agonist stimulation often leads to GPCR internalization, which can occur via different pathways ∗[2], [20], [21], [22], [23]. Of these pathways, clathrin-mediated SR 3576 (CME) is the best characterized and arguably m
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br Conclusion We have identified
2022-12-02

Conclusion We have identified potential inhibitors of C. albicans fungus specific nuclear target outer kinetochore Dam1 complex subunit Ask1, virtually screened through the PubChem compounds database (NCBI, USA) by utilizing state-of-art in silico methods in a pipeline. The 3D protein structure o
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There is little question that as we become
2022-12-02

There is little question that as we become more proficient in the diagnosis of arginase 1 deficiency individuals with intermediary elevations in arginine on newborn screening and partial defects in enzymatic activity will be found. There are no reliable data to determine a safe level of arginine and
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Furthermore we also found that the
2022-12-02

Furthermore, we also found that the basic level of ROS was markedly lower in mtDNA-reduced SW480 SC 79 than that in the parent cells. Endogenous ROS is most notably produced at the sites of complex I and complex III [5], it might be plausible that the decreased quantity of ROS observed in mtDNA-redu
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