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The results of bisaryl ether linker study are shown
2021-03-27

The results of bisaryl ether linker study are shown in . It was found that the methylene linker () moderately improved the binding to the DP receptor. The increased binding potency was also diminished in the presence of plasma, possibly due to higher plasma protein binding. Other linkers, such as th
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Another question concerns the mechanism of PC reduction
2021-03-27

Another question concerns the mechanism of PC reduction during the phosphate starvation response. There are at least three main mechanisms of PC depletion: suppression of PC synthesis due to substrate exhaustion, downregulation of PC synthase expression by suppression of gene transcription or intens
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So what can we glean from this illuminative foray
2021-03-27

So what can we glean from this illuminative foray into how Chk1 and MK2 participate in checkpoint control? First and foremost, this work reveals that Ketorolac deficient in the tumor suppressor p53 contain two spatially distinct G2/M phase checkpoint control kinase networks. This provides compelling
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GW788388 br Conflicts of interest br Acknowledgements This
2021-03-27

Conflicts of interest Acknowledgements This work was supported, in part or in whole, by the grants from the National Natural Science Foundation of China (11802056, 11772088), the China Postdoctoral Science Foundation (2018M640904), and the Fundamental Research Funds for the Central Universitie
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br Iterative design approach overview
2021-03-26

Iterative design approach overview An iterative design strategy is used to identify a peptidase-resistant reporter that acts as an efficient substrate for kinases in cell lysates as well as intact cells (Fig. 1). In this process, small-scale, rationally designed libraries are used to screen pepti
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Many studies have documented that enolase acts as a
2021-03-26

Many studies have documented that enolase acts as a plasminogen-binding protein and this interaction is involved in the tissue invasion and pathogenicity of the causative agents (Almeida et al., 2004; Avilan et al., 2000; Marcilla et al., 2007; Mundodi et al., 2008; Vanegas et al., 2007). Furthermor
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Introduction Pain is frequently the first clinical symptom o
2021-03-26

Introduction Pain is frequently the first clinical symptom of head and neck carcinoma. Indeed, pain is the initial reason leading ∼70% of cancer patients to seek professional assistance (Lam & Schmidt, 2011; Rettig & D’Souza, 2015; Schmidt, 2014). Clinically, cancer-induced facial pain can be evoke
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EBI remains an orphan GPCR and
2021-03-26

EBI2 remains an orphan GPCR and the identity and source of its ligand are yet to be described. Molecular studies of EBI2 have suggested that this receptor has constitutive activity, similar to that observed for many herpesvirus-encoded 7TM receptors (Benned-Jensen and Rosenkilde, 2008, Rosenkilde et
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br Materials and methods br Results br Discussion EP
2021-03-26

Materials and methods Results Discussion EP is an important tick borne disease caused by T. equi and B. caballi. Current chemotherapeutic drugs for EP are limited, as only diminazene aceturate and imidazole dipropionate are available. Novel and effective chemotherapeutics for treatment of E
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SJ 172550 One of the features of ROCO
2021-03-26

One of the features of ROCO proteins, controlled by their domain architecture is their oligomerization status. By size-exclusion chromatography and Western blot analysis, DAPK1 was proved to form homodimers via its GTPase and kinase domains [53]. Similarly, SJ 172550 microscopy studies conducted on
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We report here that DAPK signaling pathways play significant
2021-03-26

We report here that DAPK signaling pathways play significant roles in OGD-induced neuronal death. Exposure of the ion channel to OGD led to DAPK activation, which then promoted cell death through BimEL overexpression. Furthermore, DAPK-induced BimEL overexpression was mediated by inactivating ERK1/2
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br Materials and methods br
2021-03-26

Materials and methods Results and discussion Conclusions Clitocypin is another member of the mycocypin family of cysteine protease inhibitors that is unique to GS-9973 shown to exhibit strong insecticidal activity against Colorado potato beetle larvae. This effect is concentration dependen
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Recently a sandwich cultured hepatocyte model
2021-03-26

Recently, a sandwich-cultured hepatocyte model has been proved to be a valuable in vitro system that maintains specific hepatic cytomorphology and function relevant to drug metabolism, disposition and toxicity, and thus, closely resembles the in vivo setting. This hepatocyte model was recognized as
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br Discussion Our data demonstrate that the
2021-03-26

Discussion Our data demonstrate that the bicyclam AMD3100 strongly interacts with CXCR-4, whereas DS and AR177, two other compounds that also interfere with virus entry into the Thiazovivin synthesis (and interfere with virus binding), do not. AMD3100 is a unique compound in that it interferes wi
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Transduction of cellular signals by G protein coupled recept
2021-03-26

Transduction of cellular signals by G protein-coupled receptors (GPCRs) is stringently regulated to prevent the deleterious effects of unrestrained GPCR signaling. The rapid termination of signaling mediated by agonist-occupied GPCRs is referred to as homologous desensitization and involves the foll
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