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In this review we first introduce the
2020-01-13
In this review, we first introduce the in vivo metabolism profile of VD3, and the mediation of Cyp3a gene transcription by PXR and CAR in humans, mice and rats. We then focus on the species-specific VDR-dependent regulation of human (CYP3A4, CYP3A5 and CYP3A7), mouse (mainly CYP3A11 and CYP3A13), an
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Beside the previously reported Topo I inhibition time
2020-01-13
Beside the previously reported Topo I inhibition, time and concentration dependent CRM1 inhibitory properties of klavuzon derivatives have been shown as a second mechanism of action in this work. Especially, compounds 3 and 20 are the most effective derivatives and they completely inhibit CRM1 activ
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Early studies from the mollusk Aplysia reported the presence
2020-01-13
Early studies from the mollusk, Aplysia, reported the presence of a unique class of h89 receptors in neurons, the acetylcholine-gated chloride channels (ACCs) (Kehoe and McIntosh, 1998). Later, studies identified these receptors in the model nematode Caenorhabditis elegans (Putrenko et al., 2005; W
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In addition to carbamates organophosphates are classic inhib
2020-01-13
In addition to carbamates, organophosphates are classic inhibitors of cholinesterases. Previous studies with aquatic organisms have demonstrated their sensitivity to such chemicals. For example, individuals of the freshwater fish Colossoma macropomum exposed to the organophosphate dichlorvos, chlorp
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br Discussion Of the age related differences in serum
2020-01-13
Discussion Of the age-related differences in serum non-cholesterol sterols, we first deal with the cholesterol precursors. After birth, the markedly elevated serum desmosterol values decreased during the first year of life, and after 1 year of age they were similar between the other age groups. S
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The previously described endogenous patterns of
2020-01-13
The previously described endogenous patterns of IGF-1-induced kinase signaling, and resulting interaction between MAPK and PI3K, differ across neuronal sub-types. In R28 retinal neuron-like cells, IGF-1 treatment elicits prolonged activation (at least 80 min) of both PI3K and MAPK (Kong et al., 2016
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br Oxidoreductase like MEM for prodrug activation br
2020-01-13
Oxidoreductase-like MEM for prodrug activation Future outlook Although MEM-mediated prodrug activation has been performed by different MEMs and prodrugs, and their effectiveness have been proved in vivo, only a few types of MEMs or prodrugs have been explored in prodrug activation until now [2
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br Conclusions We can conclude that Arg is important
2020-01-13
Conclusions We can conclude that Arg293 is important but not indispensable for MeGlcA recognition by EcXyn30A since the R293A variant still retains activity and preference for MeGlcA-substituted substrates. The substrate specificity of GH30_8 glucuronoxylanases is most probably determined by an o
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br A major physiological action of ET is
2020-01-13
A major physiological action of ET-1 is to function as one of the most powerful vasoconstrictors of human blood vessels. As such, ET-1 plays a major role in regulating vascular function in all organ systems, including the kidney (Fig. 1). As in other vessels, ET-1 is thought to be released from en
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The possibility of harm with DPP inhibitors
2020-01-13
The possibility of harm with DPP-4 inhibitors in patients with clinically overt heart failure has been recently highlighted by the results of the VIVIDD (Vildagliptin in Ventricular Dysfunction Diabetes) trial (68), the only trial to date that has been designed to evaluate the effects of a DPP-4 inh
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Except for S adenosylmethionine SAM Fig sources of endogenou
2020-01-13
Except for S-adenosylmethionine (SAM, Fig. 1), sources of endogenous DNA alkylation are not well defined. Other possible sources include nitroso compounds related to the well known mutagen methylnitrosourea which are generated in vitro by nitrosation of cellular amines including amino acids, protein
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br Materials and Methods br Acknowledgements br
2020-01-13
Materials and Methods Acknowledgements Introduction Collagen fibrillogenesis, the assembly of collagen fibers, is a critical process in the development, maturation, and repair of mammalian tissue. Alterations in the structure and amount of deposited collagen fibers can greatly alter the int
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br Acknowledgments br Introduction Cell cycle
2020-01-11
Acknowledgments Introduction Cell cycle arrest or delay may occur at 3 major checkpoints, i.e. G1/S, intra-S and G2/M. p53 has a central role in controlling the G1/S checkpoint, and its loss or deactivation, occurring in the majority of cancers, forces cancer cells to rely on the S and G2/M ch
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ET expression occurs in many carcinomas including
2020-01-11
ET-1 expression occurs in many carcinomas, including those arising in the kidney [38], prostate [7], ovary [5] endometrium [39], melanocyte [40], and central nervous system [41], [42], among others [43]. The endothelin axis expression in RCC appears to be dependent upon the tumor subtype [38]. In se
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DNA replication checkpoint kinases in
2020-01-11
DNA replication checkpoint kinases in both yeast and human Digoxigenin-11-UTP upregulate dNTP levels under replication stress to mediate their essential function at replication forks (Yeeles et al., 2013). It is possible that upregulation of dNTP levels under replication stress helps fork restart o
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