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Our finding that activating DDR
2021-03-02

Our finding that activating DDR2 variants are a cause of this disease suggested that the ABL inhibitor dasatinib, a leukemia drug that also inhibits DDR2, could be used for treatment of affected individuals.10, 11 To examine the effect of dasatinib on p.Leu610Pro- and p.Tyr740Cys-induced autophospho
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In conclusion our findings demonstrated that
2021-03-01

In conclusion, our findings demonstrated that S1PC augments HMOX1 expression in a NO-dependent manner, and its effects are associated with the enhancement of BACH1 degradation. In addition, S1PC and NO potentially degrade BACH1 based on the observation that nuclear degradation of BACH1 differs from
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br Materials and methods br Results
2021-03-01

Materials and methods Results Discussion GOS potently inhibited SRD5A1 in COS-1 cells (Fig. 4A) and rat Leydig cells (Fig. 4B), possibly attenuating testosterone activation into DHT. It has been reported that gossypol inhibited human SRD5A1 with IC50 of 7 × 10−6 M [28]. Interestingly, gossy
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Consistent with previous simulations on
2021-03-01

Consistent with previous simulations on the DFG-Asp-out/-in interconversion of Abl kinase, we only observe the DFG flip with protonated Asp747 (Shan et al., 2009). We showed previously that the pKa for the DFG-Asp in Abl is elevated at 6.5. Further “constant pH” simulations whereby protonation event
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This structure guided the variation
2021-03-01

This structure guided the variation of the compounds aiming either at enhanced interaction with CK1 or to exclude interaction with CK1 (R=Me, 15). We chose the 5-cloro substituted oxoindole as backbone as it is supposed to show enhanced metabolic stability, which is commonly used in medicinal chemis
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topotecan The Ewing sarcoma breakpoint region gene EWSR is a
2021-03-01

The Ewing sarcoma breakpoint region 1 gene (EWSR1) is a partner in a large, diverse range of mesenchymal (and some nonmesenchymal) tumors (Tables 1 and 2). As the 5′ partner, EWSR1 is able to fuse with an array of genes. These fusions can generate genetically different but phenotypically identical n
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After activation AKT phosphorylates target proteins
2021-03-01

After activation, AKT phosphorylates target proteins involved in cell growth, metabolism and survival (Manning and Cantley, 2007). For example, AKT phosphorylates the pro-apoptotic protein BAD, preventing it from binding to and inactivating Bcl-xL in mitochondria (Datta et al., 1997). In turn, Bcl-x
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In conclusion our study has demonstrated that PGE stimulates
2021-03-01

In conclusion, our study has demonstrated that PGE2 stimulates expression of survivin in hepatocellular carcinoma cells. Although there are 4 subtypes of EP receptors, the EP1 receptor appears to be the predominant receptor that regulates PGE2-induced expression of survivin, mainly through trans-act
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Acidosis has lethal consequences but alkalosis due
2021-03-01

Acidosis has lethal consequences, but alkalosis (due to chloride depletion, potassium depletion, and excess mineralocorticoid) is not tolerated as well (Luke and Galla, 2012). In this regard, efforts to restore pH to normal physiological level, in the most benign way should be the goal of researcher
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Altogether the results of this
2021-03-01

Altogether, the results of this study demonstrate that peripheral blockade of both ETA and ETB receptors reduces tumor-induced facial heat hyperalgesia and increased spontaneous grooming, without modifying ongoing nociception. It is possible to suggest that bosentan is acting upon both receptors pre
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br Conflicts of interest br Financial
2021-02-27

Conflicts of interest Financial support NZ is an Established Investigator of the Dutch Heart Foundation (2013T111) and is supported by an ERC Consolidator grant (617376) from the European Research Council and by a Vici grant from the Netherlands Organization for Scientific Research (NWO; 91818
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Eggs have been recognized as an important contributor of
2021-02-27

Eggs have been recognized as an important contributor of functional ingredients for humans [3]. Egg yolk is composed of various biologically active proteins. The water-soluble proteins of egg yolk have been examined for their functional effects on longitudinal bone growth during the growth period in
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Why then is leading strand
2021-02-27

Why then is leading-strand DNA synthesis reduced relative to lagging-strand synthesis in rad53-1 mutant MRS1523 under replication stress? To gain insight into this question, we first determined whether the firing of late origins in rad53-1 mutant cells contributes to compromised leading-strand synt
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terbinafine hydrochloride Several reports by us and others h
2021-02-27

Several reports by us and others have highlighted that dimerization or oligomerization of DDR1 ECD and DDR2 ECD enhances their binding to triple-helical collagen.18, 19, 22, 28, 29, 30, 31 The ECD of DDRs consists of a discoidin domain and a stalk region. It has been reported that independent terbin
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Phylogenetically three related CXC chemokines are
2021-02-27

Phylogenetically three related CXC chemokines are classified as the possible ligands for the teleost CXCR1 and CXCR2. They are referred to as CXCL8_L1 (CXCL8/IL-8/CXCa), CXCL8_L2 (CXCc) and CXCL8_L3 (Alejo and Tafalla, 2011, Chen et al., 2013, Laing et al., 2002, Laing and Secombes, 2004, Nomiyama e
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