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8711 To simulate the inhibition of the enzyme by
2020-05-14

To simulate the inhibition of the enzyme by organophosphorus, carbamate insecticides or nerve agents, a reversible cholinesterase inhibitor physostigmine was used for most experiments for safety reasons. However, the results of the measurements were verified using the soman organophosphate, which is
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Repulsive interactions towards undesirable substrates are ar
2020-05-14

Repulsive interactions towards undesirable substrates are arguably a very efficient means to implement specificity [8]. In particular, it could be assumed that discrimination against a substrate that is larger than the cognate substrate may be achieved easily by restricting the active site and explo
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br STAR Methods br Acknowledgments
2020-05-14

STAR★Methods Acknowledgments We thank the City of Hope core facilities, including the Animal Model Core, Bioinformatic Core, NMR Core, Flow Cytometry Core, and Florescence Microscopy Core for excellent technical support, and NIH grants R01GM086171, R01GM102538, and R01CA212119, R01CA216987, an
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The findings of Qiu et al represent
2020-05-14

The findings of Qiu et al. (2016) represent the first instance of a Ub-specific mono-ADP-ribosyltransferase, as well as the first documentation of E1/E2 independent ubiquitination. Post-translational modification of Ub certainly adds layers of complexity to our understanding of the Ub signal and sho
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The fact that the mean tumor size of
2020-05-14

The fact that the mean tumor size of the E1202-654 + α-GalCer group was much smaller than that of the α-GalCer inoculated group in both protocols indicates that immunization with E1202-654 plus α-GalCer, which induces a strong CD8+ T cell E1 antigen-specific immune response, is involved in the elimi
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Diacylglycerol kinase was one of the hits identified from th
2020-05-14

Diacylglycerol kinase was one of the hits identified from the RNAi screen. Diacylglycerol kinases are conserved across a Reversine of species with more complex, multicellular organisms possessing several DGKs with differing protein domains, expression patterns and functions [61], [62], [63]. Some o
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LPA is known to regulate the peroxisome proliferator activat
2020-05-14

LPA is known to regulate the peroxisome proliferator-activated receptor γ and the reorganization of actin cytoskeleton [58]. However, the physiological functions of LPA in cells are still poorly understood. The simultaneous production of PA with/without 1-LPA or 2-LPA may be important to maximize a
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As described above we designed and synthesized
2020-05-13

As described above, we designed and synthesized a new 1,4-di-substituted isoquinoline lead compound, and was identified as a ligand with moderate potency for the CRTH2 receptor. We initially we examined the effects of the steric factor of R group on the CRTH2 binding potency (). When the methyl gro
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Hymenialdisine the most potent inhibitor of parasite TgCK
2020-05-13

Hymenialdisine, the most potent inhibitor of parasite TgCK1 enzymes in vitro has no whole cell anti-parasitic activity (Table 2). Like purvalanol B however, this Aclacinomycin A also displays poor activity against target enzymes in cultured cells. For example, in vitro IC50 values for inhibition of
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GLP also showed cardioprotective effects i
2020-05-13

GLP-1 also showed cardioprotective effects (i.e., infarct size reduction and ejection fraction improvement) in experimental models of myocardial ischemia-reperfusion injury by suppressing caspase-3 activation and preventing apoptosis of cardiomyocytes [[50], [51]]. Of note, such a cardioprotection w
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br Materials and methods br Results br Discussion DDR
2020-05-13

Materials and methods Results Discussion DDR2 played a role in cell motile behavior, but the relationship between motility and collagen activation of DDR2 tyrosine kinase was unclear. Studies with smooth muscle cells from DDR1−/− mice demonstrated a defect in cell attachment to collagen and
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A small subset of compounds composed the triazino indole clu
2020-05-13

A small subset of compounds composed the 5-[1,2,4]triazino[5,6-]indole cluster (). This series of compounds was characterised by a central heterocyclic core with an R1 alkyl amine chain, required for potency (. , , and ), with preference for morpholine over piperidine (. ). The scaffold can be subst
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nor-NOHA acetate br Materials and methods br Results br Disc
2020-05-13

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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br When Does Activity with Alternative Substrates Depend on
2020-05-13

When Does Activity with Alternative Substrates Depend on Neutral Drift? In a final scenario, the alternative reaction catalyzed by an enzyme might have no significant (positive or negative) effects on the system fitness, and thus it would be invisible to natural selection and essentially subject
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Prochlorperazine In conclusion using human liver microsomes
2020-05-13

In conclusion, using human liver microsomes, supersomes from baculovirus-transformed insect cells expressing different human CYP450 isoforms, and V79MZh3A4 cells, MB2 and MB4 were formed from TRB and MC from TRC. The amounts of MB2, MB4, and MC formed were related to the 6β-testosterone hydroxylase
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