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In the present study the expression of the CYP
2020-12-14
In the present study, the brucine of the CYP2C11 gene and the levels of its protein and activity were decreased in rats with liver insufficiency and in rats after induced dysfunction of the serotonergic system during normal liver function. Moreover, serotonergic system dysfunction during liver insu
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Beside the previously reported Topo
2020-12-14
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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Another well established visceral action of CRF
2020-12-14
Another well-established visceral action of CRF and urocortin administered peripherally is the long-lasting lowering of blood pressure observed in various species ranging from rodents to humans [22]. Existing evidence suggests that the hypotensive action of CRF and urocortin is mediated by the inter
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Cathepsin S inhibitor Cubic equations of state CEoS are part
2020-12-14
Cubic equations of state (CEoS) are particularly popular due to their simplicity and relatively good accuracy in predicting vapour-liquid equilibrium and liquid-liquid equilibrium for small, non-polar, non-associating molecules, such as light hydrocarbons. CEoS can match the phase boundaries (L/LL a
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In addition to PDCA we also tested
2020-12-14
In addition to 2,4-PDCA, we also tested other broad-spectrum 2OG oxygenase inhibitors as vCPH inhibitors. N-Oxalyl glycine (NOG, IC50 = 21.2 ± 2.1 µM), a close 2OG isostere, and IOX1 (IC50 = 47.2 ± 2.7 µM), which is a relatively broad-spectrum JmjC demethylase inhibitor, were not as potent in inhibi
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Previous studies have documented that SCFAs may elicit effec
2020-12-14
Previous studies have documented that SCFAs may elicit effects on lipid metabolism via de novo synthesis and transport. Acetate is not only used as an energy source, but is also constituted as a substrate for the cholesterol synthesis in the liver through acetyl-CoA, thus affecting plasma cholestero
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br Allosteric inhibitors In general candidate drugs that bin
2020-12-14
Allosteric inhibitors In general, candidate drugs that bind to a GPCR at a site that is distinct (allosteric site) from the binding site of the endogenous agonist (orthosteric site) are attracting increasing attention 39, 42, 58. Allosteric modulators display saturability of their effect, probe d
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Natural progestogens play an important role in the
2020-12-14
Natural progestogens play an important role in the stimulation of oocyte growth and maturation as well as in spermatogenesis and sperm maturation, and they act as sex pheromones in teleost fish (Kime, 1990, Kobayashi et al., 2002, Nagahama and Yamashita, 2008, Scott et al., 2010). A complex series o
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In the literature we can
2020-12-14
In the literature, we can find two different modes of action for estrogens: Firstly there is the commonly accepted genomic pathway. Estrogens pass the cell membrane due to their lipophilic character via diffusion and bind to estrogen receptors (ERs) in the cytoplasm. After binding a dimerization of
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br Acknowledgments We are thankful to the University
2020-12-14
Acknowledgments We are thankful to the University of Guilan Research Council for partial support of this work. Introduction It is significant to predict the mass, number and velocity distribution of BAD generated by RHA subjected to penetration of EFP by the thickness of target and the impact
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br Introduction Receptor tyrosine kinases
2020-12-14
Introduction Receptor tyrosine kinases (RTKs) are critically involved in the development and progression of human cancers and are therefore useful targets for anti-cancer therapies [1]. The Eph receptors represent the largest subfamily of receptor protein kinases and interact with ligands called
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In contrast a single instillation of BLM results
2020-12-12
In contrast, a single instillation of BLM results in a progression of inflammatory events that culminates in marked remodeling of the lung interstitium. This process takes 2–3 weeks, with the fibrotic lesions becoming most pronounced within the first month [9]. Consequently, the BLM model offers the
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On the other hand the interaction of the Kaempferia parviflo
2020-12-12
On the other hand, the interaction of the Kaempferia parviflora extract with CYP3A was uncompetitive with a low Vmax value. In the in vivo study, the Kaempferia parviflora extract did not interfere with CYP3A activity throughout the entire duration of treatment. This is fortunate as CYP3A isoforms a
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In pregnancy maternal uterine spiral artery SA
2020-12-12
In pregnancy, maternal uterine spiral artery (SA) remodeling is essential for ensuring efficient blood flow to the developing fetus. A subset of CD49a+Eomes+ decidual NK CGP 35348 (dNK) that actively secretes GFs, such as pleiotrophin and osteoglycin, have recently been described in humans and in m
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The relatively less well studied encodes the E
2020-12-12
The relatively less well-studied encodes the E2 type SUMO-conjugating enzyme. In plants, the SCE family members play roles in abiotic stress responses. An E2 enzyme, SaSce9, from plays roles in salinity and drought stress responses (). Furthermore, SCE can respond to heat stress in rice (). However,
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