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A selected set of these
2023-02-13
A selected set of these new derivatives was then used for functional assays at the human A1AR showing, as expected, an antagonist profile with IC50 values at nanomolar level. The same molecules showed also to be efficacious as nanomolar antagonists in a functional assay aimed at analyzing their abil
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Metformin s pluripotent roles are
2023-02-13
Metformin's pluripotent roles are alluded to in terms of its antitumorigenic, glucose-lowering, and cardioprotective effects, which are due in part to its upregulation of AMPK activity [39,40]. Metformin's glucose-lowering effect is a result of reduced hepatic gluconeogenesis, whereas improved insul
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Caffeic acid dihydroxycinnamic acid is a natural
2023-02-13
Caffeic MCB-613 (3,4-dihydroxycinnamic acid) is a natural compound that inhibits 5-LO and exerts potent anti-inflammatory and antioxidant properties. Recently, Takeda et al. reported that caffeic acid provided neuroprotective and anti-depressive activities [23]. Sertraline, a selective serotonin re
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rs G allele was previously associated
2023-02-13
rs523349 G allele was previously associated with a decrease in the conversion rate of testosterone to DHT (Beesley et al., 2007). This SRDA52 variant may have a trend towards higher testosterone availability, which according to the US Food and Drug Administration is described as a teratogen of categ
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In conclusion we have designed
2023-02-10
In conclusion, we have designed and synthesized a series of 4-phenyl-thiazole analogues as potent ATX inhibitors. Total twenty-five compounds were synthesized and evaluated for their inhibitory activity on ATX using FS-3 and human plasma assays. Compound was found to be the most potent derivative p
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The synthesis of compounds in
2023-02-10
The synthesis of compounds in which the ethyl linker has been modified to the carbamate and urea derivatives , and is shown in . Thus the diamine was reacted with glycolic JDTic 2HCl to give the alcohol followed by Mitsunobu reaction with phthalimide to give . Deprotection with hydrazine gave t
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Despite the growing knowledge surrounding the link between A
2023-02-10
Despite the growing knowledge surrounding the link between ATX and cholestatic pruritus in PBC, it remains unclear if the role of the ATX-LPA signaling axis includes lymphocytes homing in the liver of PBC, and if the resulting inflammation is associated with PBC pruritus (Fig. 3). PBC is characteriz
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cck 1303 Telomerase action at the telomere is highly
2023-02-10
Telomerase action at the telomere is highly regulated; it preferentially elongates the shortest telomeres, and recruitment of the enzyme complex to the telomere occurs in mid-S phase of the cell cycle (Bianchi and Shore, 2007, Britt-Compton et al., 2009, Teixeira et al., 2004, Hemann et al., 2001, T
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Here the so called alkali assay is proposed as
2023-02-10
Here the so-called alkali assay [18] is proposed as a method to be applied directly on the purified recombinant enzyme sharing the same structural and functional features of the wild-type enzyme [19], [20], [21] using its physiological substrate androstenedione. The assay that was already successful
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Based on its kinetic parameters and quaternary structure
2023-02-10
Based on its kinetic parameters and quaternary structure, R. pycnus arginase is a typical ureotelic L-arginase [2]. The Km value of the enzyme was lower than other arginases from other organisms (Table 2), including S. cerevisiae (15.7mM), B. anthracis (10mM), B. caldovelox (3.4mM), human liver (2.3
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Among steroid saponins ginsenosides are the active component
2023-02-10
Among steroid saponins, ginsenosides are the active components of ginseng, a well-known chinese medicinal plant. More than hundreds of different ginsenosides have been isolated from ginseng and have shown in the past to be membrane active substances and to influence the membrane by modulating lipid
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Apelin is a peptide hormone and an endogenous ligand
2023-02-10
Apelin is a peptide hormone and an endogenous ligand for a G protein-coupled receptor named APJ [7], [8], and apelin and APJ are widely expressed in human organs including hypothalamus, heart, lungs, kidneys, adipose tissue, muscles, and others [9]. Apelin is initially synthesized as a 77-amino-acid
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GSK2578215A mg The studies have described that Candida
2023-02-10
The studies have described that Candida non-albicans are considered as remarkable pathogenic agents of OPC, and among them, C. tropicalis and C. glabrata are known as major strains that may replace C. albicans as the greatest causing agent of this infection [20], [21]. It has been shown that Candida
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Cilengitide It has been well established that shortly after
2023-02-10
It has been well established that shortly after systemic inflammation, NADPH oxidase and iNOS activity were increased in the Cilengitide and lead to overproduction of reactive oxygen species (ROS) and NO [66]. Moreover, previous studies indicated that Ang II induced an increased level of NADPH oxid
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br Funding br Introduction Plants absorb both inorganic nitr
2023-02-09
Funding Introduction Plants absorb both inorganic nitrogen (ammonium and nitrate) and organic nitrogen (amino acids and peptides) from the soil [1]. The first organic nitrogenous molecule produced from inorganic nitrogen is Gln, whose terminal amino group is successively transferred to make Gl
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