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Targeting the MAPK pathway has attracted significant interes
2019-11-28
Targeting the MAPK pathway has attracted significant interest in cancer therapy. Efforts directly targeting RAS protein are believed to be very challenging in spite of the promise shown by a few RAS inhibitors in the early development stage. Clinical benefits achieved by BRAF and MEK inhibitors have
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In the past few years
2019-11-28
In the past few years we and others have reported that GLP-1 may also be secreted by sub-populations of alpha Tubastatin A in human pancreatic islets (Marchetti et al., 2012, Ellingsgaard et al., 2011), which could contribute to beta cell function and survival (Marchetti et al., 2012, Ellingsgaard
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Rapalink-1 As previously reported azole class antifungal dru
2019-11-28
As previously reported, azole class antifungal drugs inhibit fungal CYP450 14α-demethylase, as this interrupts the conversion of lanosterol to ergosterol, a component of the fungal cell membrane (Hof, 2006). Furthermore, correlation between fluconazole dose, the extent of hepatic hypertrophy, the le
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Although the presence of calcium in RHA P active
2019-11-27
Although the presence of calcium in RHA-P active site is confirmed by the homology modeling, some additional observations can be made following the metal depletion and reconstitution experiments performed on RHA-Phis. EDTA-treated RHA-Phis recovers its activity in the presence of divalent cations su
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Interferon IFN induces formation of a heterotetrameric IFN
2019-11-27
Interferon (IFN)-γ induces formation of a heterotetrameric, IFN-gamma-activated inhibitor of translation (GAIT) complex in human monocytic 5 aza 2 deoxycytidine sale (Mazumder et al., 2003a, Sampath et al., 2004). The complex binds a bipartite stem-loop element in the 3′UTR of vascular endothelial g
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br Methods br Results IAA abrogated the protective effects
2019-11-27
Methods Results IAA-94 abrogated the protective effects of IPC as it increased myocardial infarction (MI) due to IR injury in vitro (Diaz et al., 1999), and also prevented cyclosporine A mediated cardioprotection (Diaz et al., 2013). Moreover, IAA-94-sensitive currents were observed in cardiac
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topotecan br Materials and methods br
2019-11-27
Materials and methods Results and discussion Concluding remarks Together, the results of the theoretical kinetic simulations and of the analysis of the experimentally determined kinetic data of SoBADH performed in this work show that ignoring substrate inhibition causes potentially importan
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The Acat gene was identified by functional
2019-11-27
The Acat1 gene was identified by functional complementation of a Chinese hamster ovary cell mutant lacking ACAT activity [12]. Unlike most other genes, human Acat1 is located in two different chromosomes, (R)-(-)-Niguldipine hydrochloride 1 and 7, with each site containing a distinct promoter: chro
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br Acknowledgments br Introduction Hypertensive retinopathy
2019-11-27
Acknowledgments Introduction Hypertensive retinopathy is a disease of the retinal microvasculature associated with elevated blood pressure (Fraser-Bell et al., 2017). Narrowing of retinal arterioles occurs in the early stage of the disease, and with persistent hypertension further vascular pat
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Based on the above background gliptins may exert natriuretic
2019-11-27
Based on the above background, gliptins may exert natriuretic and diuretic effects as well [[112], [119]]. In accordance with this, Girardi and co-workers have demonstrated a physical interplay between DPP-4 and the NHE3 exchanger in the brush-border epithelium of the proximal renal tubule, suggesti
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In contrast to the methylation that
2019-11-27
In contrast to the methylation that is catalyzed exclusively by DNMTs, there have been suggested several pathways that could induce demethylation (Watt & Molloy, 1988). However, the existence and influencing of enzymes that promote active demethylation remains elusive. Studies aiming to gain more in
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YC 1 Effect of a C C
2019-11-27
Effect of a C4-C5 double bond — The presence of a double bond at the substrate’s C4-C5 position affects the reactivity of Δ1-KSTDs to varying extent, depending on the enzyme. Most 3-ketosteroids that are converted by Δ1- KSTDs have this double bond. For some Δ1-KSTDs this double bond is even require
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Direct coupling between DNA methyltransferase enzymes and
2019-11-26
Direct coupling between DNA methyltransferase enzymes and posttranslational modifications on histone proteins has been observed in mammals. For example, DNMT3A recognizes unmodified H3 through an ATRX-DNMT3-DNMT3L (ADD) domain, and its activity is inhibited by methylation of H3 at K4 (Li et al., 201
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br Introduction Although not fully
2019-11-26
Introduction Although not fully understood, the molecular toxicology of sulfur mustard (bis(2-chloroethyl)sulfide, SM; CAS–Nr. 505-60-2), an alkylating warfare agent, has been attributed to DNA alkylation [1], [2], [3]. The same principle holds true for other alkylating compounds such as nitrogen
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In present study we measured the methylation and expression
2019-11-26
In present study, we measured the methylation and Mubritinib levels of CDKL2 in HCC tissues and cell lines. Meanwhile, correlations between the methylation and mRNA expression, clinicopathological features were evaluated. Materials and methods Results Discussion DNA methylation is a herita
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