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The IP R is a ubiquitously
2021-02-07

The IP3R is a ubiquitously expressed Ca2+-release channel from the ER, activated by IP3, produced upon cellular stimulation by hormones, growth factors or neurotransmitters. Three genes are coding for the IP3R and their gene products (IP3R1, IP3R2, IP3R3) assemble in functional homo- or heterotetram
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Functional studies suggested the presence of
2021-02-07

Functional studies suggested the presence of a cysLT1 receptor. We observed an LTD4-induced cytosolic calcium response, albeit one that was very weak by most standards. The magnitude of the average response was partially explained by the low percentage of UM 171 showing a very transient response. B
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Compounds were screened for their activity against the hERG
2021-02-05

Compounds were screened for their activity against the hERG channel, with the 2,3-Cl compounds more active here than the 2,4-F compounds. The homopiperazine examples (, , , ) showed increased hERG activity relative to the corresponding piperazines. The cell data for the 6,7-dimethoxyquinoline compo
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br Chk and Chk mediated signaling act as
2021-02-05

Chk 1 and Chk 2 mediated signaling act as a barrier to tumorigenesis It was hypothesized recently that early events during tumorigenesis, such as the overexpression of oncogenes, lead to a DNA-damage response which, in turn halts tumor progression [44], [45], [46]. The DNA-damage response is prop
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Co operation or synergy between PKA
2021-02-05

Co-operation or synergy between PKA and Epac has been recently reported in PCCL3 thyroid cell line in which cAMP is pro-mitogenic, in Alda 1 to VSMC [19]. Our study demonstrates for the first time that PKA and Epac also synergise to inhibit cell proliferation in a cell type where cAMP in anti-mitog
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Each of these substrate receptors belongs to
2021-02-05

Each of these substrate receptors belongs to a multigene family with tens, if not hundreds of members in plants, and with in part overlapping and in part differential substrate specificities [4]. The complexity of the system is nicely illustrated by the F-box protein and auxin receptor TRANSPORT INH
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Several functions of FAT have been suggested It has
2021-02-04

Several functions of FAT10 have been suggested. It has been shown that FAT10 binds noncovalently to the mitotic spindle checkpoint protein MAD2 and that this binding might cause chromosome instability in the cancer 76 7 synthesis overexpressing FAT10 (Liu et al., 1999, Ren et al., 2006). In other st
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Similarly synthetic analogs of Alogliptin by replacing the c
2021-02-04

Similarly synthetic analogs of Alogliptin by replacing the cyanobenzyl group with the butynyl group have been synthesized and tested as selective DPP-4 inhibitors [7], [8]. Additionally, quinazolines [9], [10], pyridopyrimidinediones [11], pyrazolopyrimidinones [12] and pyrimidines [13] as DPP-IV in
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Regarding their reported beneficial properties on the digest
2021-02-04

Regarding their reported beneficial properties on the digestive tract, the aim of this study was to evaluate the effect of water extracts of three Hypericum sps., HP, HA, HU and some of the main phenolic compounds (Ch, R and Q) on DNA protection against oxidative and alkylating DNA damage induced by
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LPA is known to regulate the peroxisome proliferator activat
2021-02-04

LPA is known to regulate the peroxisome proliferator-activated receptor γ and the reorganization of actin cytoskeleton [58]. However, the physiological functions of LPA in cells are still poorly understood. The simultaneous production of PA with/without 1-LPA or 2-LPA may be important to maximize a
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Here we describe a novel
2021-02-04

Here, we describe a novel series of arylazoderivatives developed from CAN508, one of the first known selective CDK9 inhibitors. We focused on modification of both ends of parental molecule, CAN508, in order to improve cytotoxicity and CDK activity. We therefore analyzed how changes in molecules will
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Targeting a specific cell type rather
2021-02-04

Targeting a specific cell type, rather than the broad cytotoxicity exhibited by some of the pharmacological agents currently used to treat lupus, may improve efficacy and decrease off target toxicity. Thus, evidence that macrophages and microglia are important to the pathogenesis of LN and NPSLE, re
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We further correlated OPRK and OPRM methylation levels
2021-02-04

We further correlated OPRK1 and OPRM1 methylation levels with individual characteristics in Xinjiang Han and Uygur controls. Partial correlation analyses showed that OPRK1 methylation was positively correlated with age in Uygur male controls (r=0.72, p=0.001, adjusted by body mass index (BMI), gluco
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In patients with CTEPH ET levels are raised and have
2021-02-04

In patients with CTEPH, ET-1 levels are raised and have been shown to fall after PEA surgery [24]. After an acute pulmonary embolism there is obstruction of the pulmonary YT Broth, 2X powder blend by acute thrombus and elevated levels of ET-1 [28], [30]. Elevated levels of ET-1 have also been observ
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We hypothesize that both IGF dependent kinase
2021-02-04

We hypothesize that both IGF-1-dependent kinase activation and locally synthesized neuroestrogens interactively regulate estrogen receptor activity in neuronal AR-12 in the absence of exogenously applied estradiol. The Neuro-2A cell line was chosen as the model system for these studies because IGF-
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