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Furthermore Survivin is a member of the inhibitor of
2021-04-21

Furthermore, Survivin is a member of the inhibitor of apoptosis family. IR induces a rapid nuclear accumulation of survivin and subsequent phosphorylation of the protein in the nucleus. Co-immunoprecipitation and immunofluorescence co-localization analyses revealed an interaction among survivin, Ku7
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br Regulation of DGK activity Activation of the
2021-04-21

Regulation of DGK activity Activation of the DGKs is complex and unique for each DGK isotype. In most cases, DGKs must translocate to a membrane compartment to access DAG. However, translocation does not necessarily activate the enzyme [57]. In addition, DGK activity can be modified by other cofa
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A An optimized BEI SEIscore based on the trends
2021-04-21

(A) An “optimized BEI-SEIscore” based on the trends, emerged from the statistical analysis of several optimization studies in pharmaceutical industry (Abad-Zapatero, 2007, Abad-Zapatero and Blasi, 2011). This type of optimized scores has been used in many previous studies. Ki=1nM at 300° K, compare
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Classical DHFR inhibitors such as methotrexate MTX
2021-04-21

Classical DHFR inhibitors such as methotrexate (MTX) bind tightly to the enzyme and possess adequate clinical pharmacokinetics. MTX bind to the DHFR binding site through the formation of hydrogen bonds with Asn64, Lys68, Arg28, Arg70, Val115 and Ile7 amino Nystatin residues as well as hydrophobic i
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Ung et al examined a
2021-04-21

Ung et al. examined a variety of structural features based upon the location of the DFG-motif and the αC-helix to define the conformational space of the catalytic domain of protein kinases [75]. They reported that the DFG motif can move from its active DFG-Din location to the inactive DFG-Dout locat
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Many PIM inhibitors have been reported to
2021-04-21

Many PIM inhibitors have been reported to date [7], [8], [9] however, none of them has been marketed so far. SGI-1776 is a representative first-generation PIM inhibitor, which had been under clinical trials for leukemia and prostate cancer [10]. While most of the first-generation PIM inhibitors are
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br Acknowledgements br A subgroup of pediatric solid neoplas
2021-04-20

Acknowledgements A subgroup of pediatric solid neoplasms, collectively referred to as small round cell tumors (SRCTs) of childhood, demonstrates undifferentiated small round cell morphological characteristics. The SRCTs include neuroblastomas, lymphomas, and several bone and soft tissue sarcoma
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The activity of cysteine endopeptidases involved in the germ
2021-04-20

The activity of cysteine endopeptidases involved in the germination of caryopses is generally regulated at two levels: the hormonal induction of synthesis by gibberellins (Drzymała et al., 2008) and a putative regulation of activity by phytocystatines (Kiyosaki et al., 2007, Martinez et al., 2009),
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Therefore HNE is an attractive therapeutic target and the de
2021-04-20

Therefore, HNE is an attractive therapeutic target and the design of new HNE inhibitors is a demanding field that has been extensively investigated in order to provide inhibitors with new molecular architectures, including the potent oxo-β-lactam class [14]. In the present work, a coumarin-based oxo
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The most significant finding was
2021-04-20

The most significant finding was the inhibition of EROD and BFCOD activity by CLO. Inhibition of EROD and BFCOD were reversible, as pre-incubation did not enhance CLO inhibitory potency, and no reductions in IC50 values were observed. We further characterized the kinetic pattern of inhibition using
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br Conclusion The present study is the first
2021-04-20

Conclusion The present study is the first to provide in vivo evidence that the σ1R deficiency can cause age-related increases in aggregation and phosphorylation of αSyn in dopaminergic neurons of SNpc. The σ1R has been reported to be decreased in the flt3 inhibitor region of the nigrostriatal do
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As CP is a crucial
2021-04-20

As CP110 is a crucial player in centriole duplication, it is intriguing to ask whether centriole duplication would also be affected in the absence of the CP110-stabilizing effects of USP33. Li et al.[4] found that USP33 depletion did not inhibit normal centriole duplication through loss of centriole
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br Discussion Several DPP inhibitors are currently available
2021-04-20

Discussion Several DPP-4 inhibitors are currently available for use in the treatment of type 2 diabetes mellitus. Due to the different chemical structures there are marked differences both in the binding kinetics on the target enzyme [10] and also different pathways of elimination [13] exist. In
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br Materials and methods br Results br Discussion Plg plays
2021-04-20

Materials and methods Results Discussion Plg plays important roles in various physiological processes, such as fibrinolysis, proteolysis, cell migration, differentiation, tissue remodeling, and inflammation [6], [7], [8]. We herein found that Plg deficiency enhanced insulin secretion, and w
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br Acknowledgements We thank Dr James Ritchie and his dedica
2021-04-20

Acknowledgements We thank Dr. James Ritchie and his dedicated staff (Deptartment of Pathology, Emory University) for performing measures of serum VPA levels; Sumitomo Pharmaceuticals (Osaka, Japan) for the generous donation of DOPS, which is required for breeding Dbh −/− mice; Pfizer (Sandwich, K
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