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LY335979 To study systemic potential of the
2020-10-28
To study systemic potential of the selected compounds as EP1 receptor antagonist, they were evaluated with regard to the sulprostane-induced increase of intravesical bladder pressure in rats. Some of the analogs, 13 and 15–17, which were selected on the basis of their in vitro EP1 receptor affinity,
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The other scenario pertaining to the significance
2020-10-28
The other scenario pertaining to the significance of H2AX phosphorylation is based on the fact that the initiation of DNA fragmentation by CAD facilitates the chromatin condensation that occurs concurrently [15]. Apoptotic DNA fragmentation and chromatin condensation are important for the efficient
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Here we investigate in more detail how Dot function
2020-10-28
Here we investigate in more detail how Dot1 function contributes to the regulation of DNA damage tolerance. We find that Dot1 modulates the response to the alkylating agent MMS through its catalytic activity on H3K79. In fact, progressively reduced levels of H3K79 tri-methylation result in gradually
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br Conflicts of interest br Introduction Arylamine N acetylt
2020-10-28
Conflicts of interest Introduction Arylamine N-acetyltransferase 1 (NAT1, EC 2.3.1.5) is a cytosolic enzyme that catalyses the acetylation of small molecule arylamines, hydrazines and sulphonamides (Hein, 2002). Found in most Aprotinin in the body, NAT1 expression is regulated at the transcri
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Oral antipsychotics are substrates of CYP enzymes which
2020-10-27
Oral antipsychotics are substrates of CYP450 enzymes, which are crucial to their metabolism and elimination (Fig. 1). The efficacy and toxicity of antipsychotic agents is affected by factors that induce or inhibit CYP450 expression and function, such as drug–drug interactions. Additionally, the mult
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Atipamezole hydrochloride Fig S an adrenoceptor antagonist i
2020-10-27
Atipamezole hydrochloride (Fig. S1), an α2-adrenoceptor antagonist, is commonly used by veterinarians to recover animals from sedation-anesthesia induced by α2-adrenoceptor agonists. Recent studies in animals suggest that atipamezole might have beneficial effects in GDC-0994 damage repair, it also h
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Midazolam oral clearance is used for characterization of bot
2020-10-27
Midazolam oral clearance is used for characterization of both intestinal and hepatic CYP3A activity. However, the identification and subsequent use of metabolic markers of CYP3A activity can eliminate the need for unnecessary administration of probe drugs such as midazolam. Such metabolic markers wo
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Western blotting Western blotting was performed following th
2020-10-27
Western blotting: Western blotting was performed following the standard protocol as previously described [16]. All the images were collected using the Odyssey Fc imaging system (Li-COR Biosciences). In vitro kinase assays were performed on ∼1 μg of purified CDK5/p35 complex in 30 μL of kinase buffe
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The estrogenic activity of steroids with a
2020-10-27
The estrogenic activity of steroids with a C19 methyl group may provide a selective advantage in estrogen physiology that is not provided by E2. In this regard, 5α-androstanediol has been proposed to be a second physiological estrogen in fetal mouse Ellipticine based on the timing of ERβ synthesis
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Anidulafungin Raloxifene is a second generation SERM that
2020-10-27
Raloxifene is a second generation SERM that has tissue-specific effects that differ from those of tamoxifen. Raloxifene was marketed for prevention and treatment of osteoporosis in postmenopausal women in the US and Europe. In a phase II randomized double-blind study, tamoxifen and raloxifene were e
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EP EP and EP receptor expression on
2020-10-27
EP1, EP3 and EP4 receptor expression on HMVEC-L was shown recently by flow cytometry [14]. However, only EP4 mRNA expression was previously described in these cells [49]. Our data obtained with RT-PCR showed EP4 mRNA and very low levels of EP1 mRNA, but no EP2 and EP3 mRNA expression was detectable
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Preliminary studies suggest that dimerization of
2020-10-27
Preliminary studies suggest that dimerization of the AT1 receptor occurred during the biosynthesis in the endoplasmic reticulum before surface expression [27,40], which may explain the presenece of these Raltitrexed before the addition of any ligand. Our results showed that the presence of Ang II
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The activity of cysteine endopeptidases involved in the germ
2020-10-27
The activity of cysteine endopeptidases involved in the germination of caryopses is generally regulated at two levels: the hormonal induction of synthesis by gibberellins (Drzymała et al., 2008) and a putative regulation of activity by phytocystatines (Kiyosaki et al., 2007, Martinez et al., 2009),
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Introduction Cholesterol plays a pivotal role as a
2020-10-27
Introduction Cholesterol plays a pivotal role as a constituent of biological membranes and as a precursor for vitamins, hormones and bile acids. Accordingly, its production, distribution, and elimination must be tightly regulated at the cellular and organismal level. Accordingly, dysregulated chole
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Everolimus treatment showed an increase in
2020-10-27
Everolimus treatment showed an increase in the number of plaques and a reduction in plaque size, depending on concentration and treatment time (Fig. 1, Fig. 2). Everolimus-pretreated prostaglandin receptor adsorbed less virus with more plaque formation in the initial phase of infection (Fig. 3). Th
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