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Repulsive interactions towards undesirable substrates
2019-10-09
Repulsive interactions towards undesirable substrates are arguably a very efficient means to implement specificity [8]. In particular, it could be assumed that discrimination against a substrate that is larger than the cognate substrate may be achieved easily by restricting the active site and explo
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A decrease in heme levels enables the phosphorylation of
2019-10-09
A decrease in heme levels enables the phosphorylation of eIF2α by HRI and thereby inhibition of eIF2α activity. Indeed, the relatively small change in cytosolic heme levels in SZ Etoricoxib showed downstream functional consequences manifested by almost 50% elevation in the phosphorylation of eIF2α
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br Conformational Activation of APC C
2019-10-09
Conformational Activation of APC/C Enables Binding to the Coactivator CDC20 APC/C comes to life by binding a coactivator. This is controlled in part by phosphorylation and APC/C conformational changes that expose the NSC59984 and for the C box and IR tail of the coactivator. In interphase when m
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br Cytochrome P monooxygenases Cytochrome P monooxygenases P
2019-10-08
Cytochrome P450 monooxygenases Cytochrome P450 monooxygenases (P450s) belong to one of Nature’s most versatile group of enzymes for C–H functionalization and are able to perform challenging regioselective and stereoselective activations of remote, unactivated C(sp3)–H bonds, for which there are o
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br O GlcNAcase Human OGA is a multidomain protein
2019-10-08
O-GlcNAcase Human OGA is a multidomain protein with an N-terminal domain similar to glycoside hydrolase family 84 (GH84) enzymes, a stalk domain, a C-terminal pseudo histone acetyltransferase (HAT) domain, and several low-complexity regions (Figure 1f) [43]. A splice variant that lacks the HAT do
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Methods br Results br Discussion In
2019-10-08
Methods Results Discussion In this study we make the novel observation that villin-1 and gelsolin are down-regulated in response to diverse cellular stressors, including bacteria associated with the pathogenesis of CD. The high plasticity and dynamics of the Olanzapine cytoskeleton are explo
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The UPR is composed of three different pathways that
2019-10-08
The UPR is composed of three different pathways that fall under the control of three respective ER transmembrane proteins: PERK, IRE1α (inositol-requiring enzyme 1α) and ATF6 (activating transcription factor 6). As a starting signal for the UPR, misfolded proteins induce the release of GRP78 from th
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br EBV BILF A Virus Encoded TM Receptor
2019-10-08
EBV-BILF1—A Virus-Encoded 7TM Receptor with Immune Evasive Functions The EBV-encoded BILF1 receptor (EBV-BILF1) is thought to be implicated in the immune evasion strategy of EBV.56, 61, 62 This orphan 7TM receptor is expressed at significant levels during the early lytic phase of the virus infect
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The interface between the E ligase and the E enzyme
2019-10-08
The interface between the E3 ligase and the E2 enzyme can vary, and ZNF451 and SP-RING ligases stabilize this interaction via noncovalent binding to a scaffold SUMO (SUMOB) on the backside of the E2 (Cappadocia et al., 2015; Eisenhardt et al., 2015; Streich & Lima, 2016). By contrast, RanBP2 does no
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Previous synthetic lethal screening efforts Cox et
2019-10-08
Previous synthetic lethal screening efforts (Cox et al., 2014) have mainly used RNAi as a means of identifying potential targets (Barbie et al., 2009, Kim et al., 2016, Luo et al., 2009, Scholl et al., 2009), although a few screens (Shaw et al., 2011, Steckel et al., 2012) have been performed with s
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DDR expression is upregulated in the glomeruli and
2019-10-08
DDR1 expression is upregulated in the glomeruli and tubules of injured kidneys [7], [8], [19]; however, what role this receptor plays in kidney resident vascular disrupting agent is unclear. A plausible hypothesis is that DDR1 might contribute to kidney injury by directly exerting a pro-fibrotic ac
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DNA promoter hypermethylation is an
2019-10-08
DNA promoter hypermethylation is an important mechanism in epigenetic modulation of gene expression.[16], [17], [18] When the promoter CpG island of a gene is hypermethylated, the transcription and its associated function of the gene will be subsequently altered.[19], [20], [21] In human cancers, w
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We report here that DAPK
2019-10-08
We report here that DAPK signaling pathways play significant roles in OGD-induced neuronal death. Exposure of the Annexin V-Cy5 Apoptosis Kit to OGD led to DAPK activation, which then promoted cell death through BimEL overexpression. Furthermore, DAPK-induced BimEL overexpression was mediated by in
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DDI is one of the
2019-10-08
DDI is one of the main problems with serious clinical consequences in clinical settings. Several reports have highlighted the role of modulation of drug-metabolizing enzymes, especially CYP450 s, as a major mechanism involved in clinical DDIs [3,4,7]. The present study aimed to investigate the effec
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br Additional CDKs with a role in
2019-10-08
Additional CDKs with a role in cancer Small molecule CDK inhibitors The majority of protein kinase inhibitors developed to date are type I inhibitors: they bind at the ATP–binding site, are ATP-competitive and target the kinase in its active state; with the activation loop DFG motif in the ‘in
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