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br Conclusion and future perspectives LDL cholesterol loweri
2019-10-15
Conclusion and future perspectives LDL cholesterol-lowering therapy is essential for cardiovascular risk reduction. On the background of a high inter-personal variation of cholesterol synthesis and cholesterol Anidulafungin mass the efficacy of cholesterol lowering, both, with statins and with e
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The optimization of the lead compound
2019-10-15
The optimization of the lead compound () was initiated and the initial key SAR and the results of the structural modifications of lead compound are summarized in . Replacement of the carboxylic Thiomyristoyl moiety with other functional groups led to loss of functional activity against EP4 recepto
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N Cyclopentylmethyl analog exhibited fold less potent recept
2019-10-15
N-Cyclopentylmethyl analog 25 exhibited 2.3-fold less potent receptor affinity and 1.6-fold less potent antagonist activity. Among the compounds tested, the N-isobutyl analog 23 showed the most potent EP1 receptor affinity and antagonist activity. In summary, a series of 4-( 2-[alkyl(phenylsulfonyl
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2-APB Endothelins ETs are peptides expressed in both the
2019-10-14
Endothelins (ETs) are peptides expressed in both the peripheral and the central nervous systems, which can contribute to sensory changes seen in animal models of inflammatory, cancer and neuropathic pain [10], [11]. All three mammalian isoforms (ET-1, ET-2 and ET-3) activate specific G protein-coupl
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Introduction Breast cancer is a highly prevalent malignancy
2019-10-14
Introduction Breast cancer is a highly prevalent malignancy. There are some recognized risk factors for breast cancer, like early menarche or late menopause, which increase the length of the exposure to hormones, as a result of a higher number of ovarian cycles [1]. Moreover, there is evidence supp
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The biological actions of ET are mediated via two
2019-10-14
The biological actions of ET‐1 are mediated via two distinct receptor subtypes, the endothelin A and endothelin B receptors (ETA/ETB). While activation of ETA is assumed to mediate contraction of smooth muscle cells, the activity of ETB is related to transient vasodilation [22]. In human corpus cave
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Introduction The Bromeliaceae family is one
2019-10-14
Introduction The Bromeliaceae family is one of the most morphologically and ecologically diverse flowering plant families native to the tropics and subtropics of the New World (Benzing, 2000). They comprise >3000 species and are traditionally divided into three subfamilies: Pitcairnioideae, Bromeli
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DDX belongs to the DEAD box family of
2019-10-14
DDX3 belongs to the DEAD-box family of proteins, ATP-dependent RNA helicases characterized by the presence of a highly conserved helicase core domain [13]. This catalytic core is composed of two RecA-like domains containing motifs involved in ATP binding/hydrolysis, RNA binding and helicase activity
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One specific brain region that may be involved in the
2019-10-14
One specific iMDK and region that may be involved in the reduction of anxiety after anti-SVG-30 treatment is the lateral septum which contains a high density of CRF2 receptors [5], [44]. The lateral septum often exhibits increased immediate early gene expression in response to stress and anxiety [14
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Hymenialdisine the most potent inhibitor of parasite TgCK
2019-10-14
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 emodin also displays poor activity against target enzymes in cultured cells. For example, in vitro IC50 values for inhibition of CDK5/cyc
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As a support chitosan presents interesting characteristics
2019-10-14
As a support, chitosan presents interesting characteristics that reinforce its great potential for enzyme immobilization [18,19]. Firstly, it is produced from renewable natural sources in addition to being biodegradable and water insoluble [20,21]. Also, the main peculiarity in the chitosan structur
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We not only found that the ISR
2019-10-14
We not only found that the ISR leads to attenuation of conventional cap-dependent translation with no change in RAN translation of the G4C2 expanded repeat, but also that GA translation from the expanded repeat (but not from 5 G4C2 repeats, perhaps because the protein product does not aggregate) is
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br Materials and methods br
2019-10-14
Materials and methods Results Discussion The phosphatidylinositol 3-kinase-like protein kinases, ATM, ATR, and DNA-PK, have all been implicated in H2AX phosphorylation in response to different stimuli [37], [41], [42], [43], [44], [45]. We show here that H2AX is phosphorylated in rodent and
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br DAG kinase activity is
2019-10-14
DAG kinase activity is confined to specific cell compartments A number of reports demonstrating agonist-dependent translocation of DGKs to distinct membrane compartments suggest that DGK activity is restricted to localized DAG pools generated after activation of receptors. Perhaps the best eviden
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In contrast T bet downregulated the expression
2019-10-12
In contrast, T-bet downregulated the expression of Tfh functional molecules, CD40L, ICOS, and IL-21; accordingly, T-bet overexpression abrogated the helper function of IL-12-stimulated CD4+ T cells. Thus, T-bet seems more involved in the downregulation of the helper functions than in the differentia
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