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br Most reported binding data are obtained by performing het
2020-08-04
Most reported binding data are obtained by performing heterologous AMD-070 hydrochloride binding experiments and expressing the results as relative binding affinity (RBA). The constructed binding curves should theoretically be sigmoidal in shape with a Hill slope value of one, for a single ligand
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br Conclusion The past few years have witnessed substantial
2020-08-04
Conclusion The past few years have witnessed substantial progress in understanding the structural mechanisms of substrate recognition and the reactions catalyzed by the O-GlcNAc-cycling enzymes, but more work remains. In particular, future research will be needed to establish how OGT and OGA inte
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Sexually dimorphic testosterone hydroxylase activities have
2020-08-04
Sexually dimorphic testosterone hydroxylase activities have been suggested as a biomarker of endocrine disruption caused by xenobiotics (Wilson et al., 1999). The results from the studies reported here suggest that dietary exposure to the endocrine active test compounds, all of which have demonstrat
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Imaging of primary Tfh cells at
2020-08-04
Imaging of primary Tfh cells at the peak of the GC response revealed clear spatial segregation in the FM and GC compartments. This confinement was confirmed by TPP and discontinuous cell tracking 24 hr later, which showed retention of the majority of photoconverted GC Tfh cells in the original GC an
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The involvement of MDM in mechanisms
2020-08-04
The involvement of MDM2 in mechanisms underlying development of inflammatory autoimmune diseases is additionally supported by recent data showing that MDM2 promotes rheumatoid arthritis [33]. Here, collagen-induced arthritis mouse model was used to demonstrate that high MDM2 levels correlated with d
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br Results and discussion br Conclusion We have constructed
2020-08-04
Results and discussion Conclusion We have constructed a series of potent and greatly selective DPP-4 inhibitors with pyrazolo[1,5-a]pyrimidin-7(4H)-one core surrogates. The modification of the core led us to b2 which has IC50 of 80 nM and > 1000 fold selectivity over DPP-8 and DPP-9. We utiliz
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The action of DPP inhibitors as insulin secretagogues
2020-08-04
The action of DPP-4 inhibitors as insulin secretagogues results from their ability to potentiate of GLP-1 and glucose-dependent insulinotropic polypeptide (1). Endogenous GLP-1 is wholly responsible for the hypoglycemic actions of DPP-4 inhibitors (8). However, DPP-4 inhibitors also act to enhance t
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br Materials and methods br Results Artemis has been reporte
2020-08-04
Materials and methods Results Artemis has been reported to possess 5′–3′ exonuclease activity in vitro on ssDNA, as well as DNA-PK-dependent endonuclease activity on single-strand overhang and hairpin DNA structures [11]. However, enzymes within the metallo-β-lactamase family typically contain
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miRNAs are known to regulate the autophagy related
2020-08-03
miRNAs are known to regulate the autophagy-related genes and their activities. Also, miRNAs modulate autophagy at different stages such as autophagic induction, vesicle nucleation, vesicle elongation and completion, by targeting autophagy complexes via different miRNAs [[56], [57], [58]]. Recently,
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The covalent linkage of hemin with nucleic acids
2020-08-03
The covalent linkage of hemin with nucleic acids is one of the alternative strategies for catalytic capacity improvement of hemin, which has been proved to significantly improve hemin’s solubility and recover peroxidase activity [28]. In previous work, we have investigated the catalytic properties a
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We next determined the kinetic parameters
2020-08-03
We next determined the kinetic parameters of TgTCEA and TgTCEB with A-type analogues (, , and ) and chiral B-type analogues (, , and ), and compared with those for authentic substrates, PosA and PosB. The kinetic parameters of TgTCEA and TgTCEB are listed in , , respectively (see , respectively, for
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br Conclusion S chirata and ursolic acid
2020-08-03
Conclusion S. chirata and ursolic Caspase Inhibitor Set I sale showed very less inhibition on both CYP3A4 and CYP2D6 isozymes which was insignificant as compared to their known inhibitors (ketoconazole and quinidine). The tested heavy metals and trace elements present in S. chirata were within t
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To the best of our
2020-08-01
To the best of our knowledge, this is the first association study to analyze COMT Val158/108Met and the ROCF immediate and delayed scores in veterans with PTSD. The significant difference in ROCF immediate and delayed scores was detected between different COMT Val158/108Met genotype groups in vetera
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Taken together these results allowed us to conclude
2020-07-31
Taken together these results allowed us to conclude that LEI/SERPINB1 intrinsically possesses two enzymatic activities: an anti-protease activity dependent on its reactive site loop, which is analogous to the other proteins of the family and an endonuclease activity which is unveiled by the cleavage
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In anaphase APC CCDC recruits substrates
2020-07-31
In anaphase, APC/CCDC20 recruits substrates, while the APC2–APC11 cullin–RING catalytic core engages, positions, and activates transient E2∼Ub intermediates (e.g., UBE2C∼Ub, where ‘∼’ refers to thioester bond) from which Ub is transferred to a coactivator-bound substrate (Figure 2B, Conformation VI)
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