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br Significance Our understanding of the ubiquitin biology h
2019-09-10

Significance Our understanding of the ubiquitin biology has been rapidly expanding. The role of the ubiquitin system in the pathogenesis of numerous disease states has increased the interest in finding new strategies to pharmacologically interfere with the enzymes responsible of the ubiquitinatio
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br Materials and methods br Results br Discussion Natural co
2019-09-10

Materials and methods Results Discussion Natural compounds and their derivatives have been investigated as candidates for the treatment of bone diseases and can also be the sources of nutraceutical agents and therapeutic agents [28]. Using peptides as therapeutic effects on bone-related dis
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Hymenialdisine the most potent inhibitor
2019-09-09

Hymenialdisine, the most potent inhibitor of parasite TgCK1 enzymes in vitro has no whole cell anti-parasitic activity (Table 2). Like purvalanol B however, this flumethasone kinase also displays poor activity against target enzymes in cultured cells. For example, in vitro IC50 values for inhibition
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br Cholesterol handling in the
2019-09-09

Cholesterol handling in the arterial wall cells Foam cell formation in the arterial intima is a major hallmark of early-stage atherosclerotic lesions, which is attributed to uncontrolled uptake of modified lipoproteins, excess cholesterol esterification and impaired cholesterol release [44]. As a
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While agnathans appear to have
2019-09-09

While agnathans appear to have reduced their Ednr repertoire to the Ednra gene (that may have been amplified in the Arctic lamprey), gnathostomes in general have been relatively inert to Ednr gene loss. Strikingly, the only Ednr gene that has been lost repeatedly is EdnrB2 (lost in therian mammals,
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Donepezil HCl The small intestine in addition
2019-09-09

The small intestine, in addition to its primary role of absorption, has the ability to metabolize drugs and other xenobiotics through phase 1 and phase 11 metabolisms [25] since almost all the cytochrome P450 Donepezil HCl present in the liver are also present in the small intestine although, in lo
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daprodustat clinical The EGFR belongs to the
2019-09-09

The EGFR belongs to the ErbB family of receptor tyrosine kinases (RTKs), comprised of four members: EGFR (ErbB1, HER1), HER2 (ErbB2), HER3 (ErbB3) and HER4 (ErbB4) [24]. HER receptors are activated by a group of epidermal growth factor (EGF) ligands and undergo homo- or hetero-dimerization during th
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Although the implication of DA and glutamate
2019-09-09

Although the implication of DA and glutamate signaling crosstalk in drug-evoked neuronal adaptations is well acknowledged, targeting the cognate receptors to alleviate symptoms is associated with a loss of efficacy over time and the appearance of severe sides effects, likely due to the involvement o
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The co occurrence of the AA and the AA domains
2019-09-09

The co-occurrence of the AA12 and the AA8 domains in CcPDH would allow for electron transfer between these domains. Such electron transfer is known to occur in CDH, and the AA8 family in CAZy is in fact largely comprised of cytochrome domains of multi-domain CDHs. One notable exception concerns the
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The purposes of this study is to develop
2019-09-09

The purposes of this study is to develop an experimental model of CysLT2 receptor-mediated LTC4-induced lung air-trapping in guinea pigs using S-hexyl GSH, and to clarify the mechanism underlying response to such trapping using montelukast, a CysLT1 receptor antagonist, BayCysLT2RA, a CysLT2 recepto
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Cytochromes P CYP are a superfamily of
2019-09-09

Cytochromes P450 (CYP 450) are a superfamily of hemoproteins containing a heme cofactor, which are widely distributed in animals, plants and microbes (Hannemann et al., 2007). CYP450 exhibits a variety of biological functions including biotransformation of drugs, detoxification of endogenous and xen
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Our approach relied on measurement of bulk
2019-09-09

Our approach relied on measurement of bulk solute diffusivity in the three tissue types of interest. Our diffusivity values (Table 3) are on the order of 10−6 cm2/s and are comparable to the PG diffusion coefficient in water at infinite dilution, which is about 10−5 cm2/s at room temperature, as wel
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Natural progestogens play an important role
2019-09-09

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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From the general synthetic route we first synthesized a
2019-09-07

From the general synthetic route, we first synthesized a directed set of analogues of general formula , keeping the synthesis simple by using a symmetrical pyrazole (R=R=Me). The SAR of a set of 30 compounds in the GTPγS binding assay turned out to be quite tight: only 4 (13%) compounds showed moder
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br Materials and methods br
2019-09-07

Materials and methods Results Recently, a quantitative proteomic analysis of C2C12 mouse myoblasts cell line totally deprived of protein kinase CK2 catalytic subunits (CK2α/CK2α′(−/−)), suggested that the cellular expression of HSP27, a chaperone with multiple functions related to proteostasis
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