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Because the E enzyme directly recognizes a
2020-08-05
Because the E2 enzyme directly recognizes a SCM, it can modify substrates in vitro at high enzyme concentrations as we illustrate in Fig. 1A. Hence, it is important to use a low E2 concentration in E3-dependent reactions that either show no or only marginal substrate modification by the E2 alone. At
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br Declaration of interest br Author contributions br
2020-08-05
Declaration of interest Author contributions Acknowledgement This study was supported by a Grant-in-aid for Scientific Research from The Ministry of Education, Culture, Sports, Science, and Technology of Japan (No. 26670733 and No. 26293363 to K. Miyado). Introduction Lead (Pb) is an im
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The nitro furan ylmethylene dioxo pyrazolidin yl benzoic
2020-08-05
The 4[4-(5-nitro-furan-2-ylmethylene)-3,5-dioxo-pyrazolidin-1-yl]-benzoic lp-pla2 ethyl ester (hereafter PYR-41) and related pyrazones are cell-permeable UBE1 inhibitors identified in high-throughput screening of the UBE1–UBE2–UBE3 cascade, which selectively and irreversibly inhibits UBE1 activity
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Alogliptin is a potent selective inhibitor of the serine pro
2020-08-05
Alogliptin is a potent, selective inhibitor of the serine protease DPP-4 [10]. Alogliptin or (2-[[6-[(3R)-3-amino-1-piperidinyl]-3,4-dihydro-3-methyl-2,4-dioxo-1(2H)-pyrimidinyl]methyl] benzonitrile) (C, Fig. 2), a potent (IC50 10,000 over DPP-8 and 9) was identified by replacing the quinazolinone
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Next we evaluated whether DPP inhibitor suppressed osteoclas
2020-08-05
Next, we evaluated whether DPP-4 inhibitor suppressed osteoclast formation by downregulating LPS-induced RANKL expression in stromal cells; DPP-4 inhibitor did not inhibit LPS-induced RANKL expression. Furthermore, we evaluated the effect of DPP-4 on LPS-induced RANKL expression in stromal cells, bu
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br DNA PK kinase activity
2020-08-05
DNA-PK kinase activity As previously stated, DNA-PKcs recruitment to the DSB results in translocation of the Ku heterodimer inward on the dsDNA allowing DNA-PKcs to interact directly access DSB end, which results in activation of the catalytic activity of the enzyme [42], [43]. DNA-PKcs has no to
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br Molecular modeling study Molecular modeling study was ess
2020-08-05
Molecular modeling study Molecular modeling study was essentially needed to understand and interpret the DHFR inhibitory pattern of this new class of compounds. Computational docking is an algorithm designed to estimate two main terms. The first is to determine the suitable position and the orien
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br Materials and methods br Results br Discussion Consistent
2020-08-05
Materials and methods Results Discussion Consistent with previous reports (Barr et al., 2010, Vuong et al., 2010), the current study demonstrates that rats treated with amphetamine exhibit heightened anxiety states during withdrawal. Furthermore, icv. infusion of a CRF2 receptor antagonist
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Nevirapine Radioligand selection may be the critical factor
2020-08-05
Radioligand selection may be the critical factor for detecting CRF1 receptor antagonists that bind to the ECD. Compounds with this site of action could be useful starting points for developing therapeutic agents with improved physical properties over J-site antagonists. However, it remains to be see
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In our recent work we established a
2020-08-05
In our recent work, we established a different and new strategy to overcome the immunogenicity problem. We showed that isolation of a novel form of the protein used with different epitops could also minimize the patient immune response. We showed that the antibody of one form of the enzyme does not
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br DNA PK kinase activity As previously
2020-08-04
DNA-PK kinase activity As previously stated, DNA-PKcs recruitment to the DSB results in translocation of the Ku heterodimer inward on the dsDNA allowing DNA-PKcs to interact directly access DSB end, which results in activation of the catalytic activity of the enzyme [42], [43]. DNA-PKcs has no to
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Previously a linear rolling circle
2020-08-04
Previously, a linear rolling circle amplification (RCA) has been employed to create DNA nanochains or DNAzyme chains for DNA [15], miRNA [16], protein [17] detection. In RCA-based assays, target quantification is achieved through the quantification of the RCA products. In order to improve the sensit
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We also performed a correlation analysis
2020-08-04
We also performed a correlation analysis independent of annotated gene sets to identify potentially novel genes that are co-expressed with DHODH. Using the top 100 DHODH co-expressed genes in COAD, LGG, STAD, and PAAD diseases, we identified four common genes across all four diseases (Fig. 9). These
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At the cellular level a widening
2020-08-04
At the cellular level, a widening waistline is a result of lipid accumulation in adipose tissue, and the morbidities are linked to ectopic lipid accumulation in non-adipose tissues such as liver, skeletal muscle, and pancreas [8]. The accumulated lipids are largely TAG sequestered into lipid droplet
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DDR is widely expressed in several tissues
2020-08-04
DDR1 is widely expressed in several tissues (Alves et al., 1995, Curat & Vogel, 2002, Ferri et al., 2004, Hou et al., 2001, Mohan et al., 2001, Sakamoto et al., 2001, Tanaka et al., 1998) including the mouse (Bhatt et al., 2000, Franco-Pons et al., 2009, Sanchez et al., 1994, Seo et al., 2008, Zerli
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