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We have previously reported DAPK inhibitors discovered
2021-05-24

We have previously reported DAPK inhibitors discovered through our structure-based virtual screening (SBVS) research program. In this paper, we describe the general protocol of our in silico approach, and the strategy used to develop hit compounds. In addition, the studies conducted on the structure
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Semantics play an important role in software component based
2021-05-24

Semantics play an important role in software component-based development as they improve components identification, selection and integration through, among others, the use of ontologies (Kaur and Mishra, 2017). Analogously, they allow to improve discovery, composition and reuse in the context of We
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The results of physical parameters
2021-05-24

The results of physical parameters of the prepared samples are summarized in Table 2. The equivalent diameter ranged from 1.09 to 1.14 mm, which is within the required size distribution of 0.8–1.25 mm. A slight increase in size is probably caused by increasing the thickness of the second coat. To d
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In cholesterol synthesis HMG CoA reductase
2021-05-24

In cholesterol synthesis, HMG-CoA reductase is the rate limiting step in cholesterol biosynthesis. Statins or HMG-CoA reductase inhibitors are commonly used for management of hypercholesterolemia. The presence of an HMG-like moiety on these drugs allows them to competitively bind to the catalytic do
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hesperetin mg In this study we were able
2021-05-22

In this study, we were able derive new insights into the biology of DDR2 including the demonstration that cellular tyrosine phosphorylated proteins co-localise with DDR2 and exogenously added collagen I (Fig. 1G). This finding suggests that similar to the focal adhesion complexes associated with int
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Enzymatic assay The usual in vitro test for the measure
2021-05-22

Enzymatic assay. The usual in vitro test for the measure of the activity of DbH involves ascorbate as a cosubstrate (e.g., 5mM) and tyramine as a substrate (e.g., 10mM). When using N-aryl-N′-hydroxyguanidines instead of ascorbate, the hydroxylase activity of DbH was measured by HPLC as the amounts o
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At present there have been relatively few studies that evalu
2021-05-22

At present, there have been relatively few studies that evaluated potential correlations between pulmonary and pleura metastases, hilar and mediastinal CB-5083 nodes, and organs associated with distant metastasis and EGFR mutations [33,34,37]. Further research on these relationships is needed, which
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In this study we have explored a functional role of
2021-05-22

In this study we have explored a functional role of the oxysterol/EBI2 system in this process. In 2011 we and others reported the discovery of oxysterols as ligands for EBI2 [6], [7]. Oxysterols are metabolites generated by hydroxylation of cholesterol and have been linked to a variety of fundamenta
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IFN-gamma, murine recombinant br The classical ubiquitinatio
2021-05-22

The classical ubiquitination pathway Ubiquitination is an enzymatic process that involves the addition of an ubiquitin protein to a substrate that usually becomes inactivated followed by degradation in the proteasome; however, several other functions have also been described. For the discovery of
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Based on the similar activities
2021-05-22

Based on the similar activities of Rad6p and Cdc34p (i.e., both are E2 ub-conjugating enzymes) on ubiquitinylation of p33 replication protein, we propose that Rad6p and the plant Ubc2p mono- and bi-ubiquitinate the viral replication proteins in order to facilitate the recruitment of the cellular ESC
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Historically covalent drugs have had
2021-05-22

Historically, covalent drugs have had great success (e.g., aspirin and penicillin), and covalent drugs have become a focus in anticancer and antiviral drug discovery (Kalgutkar and Dalvie, 2012, Singh et al., 2011). These compounds contain low reactivity warheads that allow covalent adducts to form
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A set of small molecule LigI inhibitors were
2021-05-22

A set of small molecule LigI inhibitors were identified through an in silico structure-based screen, using the atomic resolution structure of LigI complexed with nicked DNA [[18], [26]]. This screen yielded inhibitors that were selective for LigI (L82), inhibited both LigI and LigIII (L67) and inhib
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br Materials and Methods br Acknowledgements br Introduction
2021-05-22

Materials and Methods Acknowledgements Introduction Collagen fibrillogenesis, the assembly of collagen fibers, is a critical process in the development, maturation, and repair of mammalian tissue. Alterations in the structure and amount of deposited collagen fibers can greatly alter the int
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DDI is one of the main
2021-05-22

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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We have previously characterized the leucine rich NESs
2021-05-22

We have previously characterized the leucine-rich NESs located within the zinc-binding domains of mucosal high risk HPV16 E7 (76IRTLEDLLM84) and low risk HPV11 E7 (76IRQLQDLLL84) mediating their nuclear export in a CRM1 dependent manner (Knapp et al., 2009, McKee et al., 2013). The zinc-binding doma
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