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Substituents at the C position An oxygen containing substitu
2021-06-21

Substituents at the C11 position — An oxygen-containing substituent at the C11 position also affects the catalytic activity of Δ1-KSTDs. The Δ1-KSTDs from the Gram-positive bacteria R. equi [29], N. simplex ATCC 6946 and IFO 12069 [48,49,52], and R. rhodochrous IFO 3338 [27] were able to 1(2)-dehydr
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In our model CSF R blockade with
2021-06-21

In our model, CSF-1R blockade with PLX647 mainly targeted the more abundant MDSCs instead of macrophages, suggesting that the role of CSF-1 may be tumor model-dependent. Different tumor models, genetic backgrounds, or treatments may induce different growth factors or cytokines in the tumor microenvi
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Substitutions on the benzene ring of the
2021-06-21

Substitutions on the benzene ring of the phenyl acetic topotecan moiety were evaluated to study their effect on DP and CRTH2 selectivity (). Compound has strong affinity for CRTH2, but it only has moderate affinity for DP. Small substitutions such as methoxy () and fluorine () next to the aryloxy
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To assess which export pathway is used by the iNOS
2021-06-21

To assess which export pathway is used by the iNOS mRNA, we inhibited CRM1 activity by incubation of DLD-1 Solasodine with LMB. Since LMB covalently and exclusively binds to CRM1, it represents a potent and specific inhibitor of the CRM1 transport activity [38]. Inhibition of CRM1 activity as well
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Both anxiogenic and antinociceptive effects produced by CRF
2021-06-21

Both anxiogenic and antinociceptive effects produced by CRF seem to be selective for the CRF1 receptor, since intra-dPAG microinjection of ASV 30, a CRF2 receptor antagonist, altered neither the anxiety nor the antinociception response. Intra-dPAG ASV 30 was also unable to prevent the anxiogenic (ob
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Accurate equilibrium predictions of CO containing
2021-06-21

Accurate equilibrium predictions of CO2 containing mixtures, however, are challenging with traditional equations of state. The reason for this may be that CO2 has a large quadrupole moment. The large quadrupole moment of CO2, as well as size asymmetry, are for instance believed to be the reasons for
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Measurement of Chol absorption synthesis and
2021-06-21

Measurement of Chol absorption, synthesis and catabolism would be very helpful to determine the underlying cause of hypercholesterolemia in individual patients at risk for atherosclerosis. The information could help to determine the best therapeutic approach to reduce Chol absorption, to reduce Chol
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The repeat sequence TTAGGG of
2021-06-21

The repeat sequence “TTAGGG” of telomere could be directly recognized by TERF1. TERF1 is indispensable for the maintenance of telomere TASIN-1 structure and integrity (Tan et al., 2017). Trf1 genetic depletion in vivo induces a persistent DNA damage response and telomere uncapping, which effectivel
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br Materials and methods br Results and
2021-06-19

Materials and methods Results and discussion Concluding remarks Together, the results of the theoretical kinetic simulations and of the analysis of the experimentally determined kinetic data of SoBADH performed in this work show that ignoring substrate inhibition causes potentially importan
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Three kinase inhibitors dasatinib type I imatinib type
2021-06-19

Three kinase inhibitors dasatinib (type I), imatinib (type II) and nilotinib (type II), identified initially as inhibitors of tyrosine kinase BCR-ABL, were found to target DDRs in a chemical proteomic profiling study (Bantscheff et al., 2007, Hantschel et al., 2008). These tyrosine kinase inhibitors
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To study the effect of DDR
2021-06-19

To study the effect of DDR inhibition by imatinib, nilotinib and dasatinib in a cellular environment we generated DDR1 and DDR2 expressing HEK293 cell lines by stable transfection. Of the five DDR1 splice variants we focused on the 1b variant whose over-expression has been associated with pulmonary
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br E E backside interaction The E
2021-06-19

E3–E2 backside interaction The E2 possesses an important regulatory interface which is termed its backside as it is opposite to the catalytic cleft that bears the active-site cysteine forming the thioester with SUMOD. This backside site interacts noncovalently with a scaffold SUMOB and was origin
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br Acknowledgements The authors are supported by National In
2021-06-19

Acknowledgements The authors are supported by National Institutes of Health grants (CA162804, CA92584, and CA13499 to DJC and CA166677 to BPPC) and Cancer Prevention and Research Institute of Texas (RP110465 to DJC). The cellular response to DNA double-strand break (DSB) formation is an essent
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Like compound substitution on compound contains amino and
2021-06-19

Like compound substitution on compound () contains amino and carboxamide groups attached to adjacent ring positions. These groups have similar interactions as compound with the protein backbone and Glu114. The triazole core is coordinated with Lys291. The triazole ring core π-stacks with Tyr226. Th
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br Other Alterations in Triglyceride Metabolism in DGAT Defi
2021-06-19

Other Alterations in Triglyceride Metabolism in DGAT-Deficient Mice Consistent with the enzyme's ubiquitous expression pattern, DGAT deficiency also altered triglyceride metabolism in other tissues. For example, postpartum Dgat−/− female mice were unable to nurse their young owing to an absence o
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