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HOSu synthesis The kinetic data obtained from incubation of
2021-09-27

The kinetic data obtained from incubation of 4BAB with GLO1 show that 4BAB does not completely inactivate the enzyme (Figs. 2A and S6a). At low concentrations (4.7 and 14.4μM), 4BAB seemed to follow biphasic kinetics (Fig. 2A); even though regardless of the concentration 4BAB, there was a plateau at
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Crystal structures from soluble E constructs Khan et al Kong
2021-09-27

Crystal structures from soluble E2 constructs (Khan et al., 2014; Kong et al., 2013) have revealed globular protein with no regular structure in spite of having eight disulphide bonds (Kong et al., 2013). Although 62% of the protein exists in loops or disordered structures, overall it was well-defin
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The role of the ER EK
2021-09-26

The role of the ER22/23EK variant which is associated with relative resistance to GC, as shown by a reduction of transactivating capacity in vitro and less suppression of sodium butyrate levels after 1mg DST in vivo. Relative GC resistance associated with the ER22/23EK polymorphism might protect fr
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CSL is endowed with an intrinsic
2021-09-26

CSL is endowed with an intrinsic transcription-repressive function, and CAF-effector genes are induced as a consequence of CSL downmodulation (Hu et al., 2012, Procopio et al., 2015), as it can occur upon exposure to pro-carcinogenic stimuli such as UVA or smoke-derived compounds (Menietti et al., 2
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Serotonin hydroxytryptamine HT is a
2021-09-26

Serotonin (5-hydroxytryptamine, 5-HT) is a monoamine with dual functions in the developing and matured brain. 5-HT regulates development of the read this article as a neurotrophic factor and is involved in emotion and cognition as a neurotransmitter in adulthood (Gaspar et al., 2003; Daubert and Co
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Albumin is the major carrier
2021-09-26

Albumin is the major carrier of free fatty acids (FFAs) in plasma [59], and harbours seven binding sites that are common to FFAs with a range of chain-lengths (C10-C18) across its three domains (Fig. 1a) [60,61]. In vitro, saturated, mono- and poly-unsaturated FFAs, with chain lengths ranging from C
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However the clinical development of was terminated in
2021-09-26

However, the clinical development of was terminated in 2013 due to the concerns over liver toxicity, raising important questions regarding the long-term safety and viability of targeting GPR40 and, more specifically, about our understanding of the pharmacobiology and signaling spectrum of this recep
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Tetrazole is one of the
2021-09-26

1-Tetrazole is one of the most commonly used bioisosteres for carboxylic acids arising from their similarity in pKa (ca. 4.5–4.9 vs 4.2–4.4, respectively)., Metabolically, tetrazoles may exhibit an advantage over carboxylic acids because they form -glucuronides which are not as chemically reactive a
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Interestingly the subcellular localization of FBPase in hepa
2021-09-26

Interestingly, the subcellular localization of FBPase in hepatocytes and proximal tubule Carboplatin reveals that FBPase is also able to translocate to the nucleus in these cell types. The nuclear localization of muscle-FBPase was recently reported [35]. This data corroborate our results on the abi
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DAMPs are endogenous danger signals that can
2021-09-26

DAMPs are endogenous danger signals that can initiate and perpetuate a noninfectious nuclear receptors 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 d
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Our data show that oxidative stress high
2021-09-26

Our data show that oxidative stress (high levels of ROS) suppresses the process of lysosomal exocytosis, which would be predicted to impair the expulsion of toxic compounds from cells. Therefore, we propose that ROS have a biphasic effect on the lysosomal clearance: consistent with their role as a s
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br Materials and methods br
2021-09-26

Materials and methods Results Bgal from Alteromonas sp. ML117 had an open reading frame of 3126 bp encoding 1042 amino NCT-502 synthesis residues with a predicted mass of 120 kDa and a theoretical pI (isoelectric point) of 5.44. The recombinant Bgal contained a His tag, as well as other addit
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Recently accumulated evidence has revealed a close
2021-09-26

Recently, accumulated evidence has revealed a close link of FXR to gluconeogenesis. For example, activation of FXR by its agonist GW4064 improved hyperglycemia in db/db mice by repressing gluconeogenesis [15], and FXR agonist CDCA decreased transactivation activity of key gluconeogenic genes by indu
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br Lysophosphatidylinositol LPI LPI is a subspecies
2021-09-24

Lysophosphatidylinositol (LPI) LPI is a subspecies of lysophospholipid consisting of inositol as its head group, one glycerol molecule and one acyl chain (Piñeiro and Falasca, 2012). The biosynthesis of this lipid starts from Phosphatidylinositol (PI) and is catalysed by the enzymes phospholipase
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Interestingly zaprinast administration not only prevents the
2021-09-24

Interestingly, zaprinast administration not only prevents the development of hypersensitivity but also enhances opioid effectiveness. Opioids have long been considered among the most effective drugs used to treat pain (Watkins et al., 2005; Mika et al., 2013; Szczudlik et al., 2014a, Szczudlik et al
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