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DNA damage represents a persistent threat to genomic stabili
2020-03-23

DNA damage represents a persistent threat to genomic stability. A critical link exists between DNA mutation, chromosomal rearrangement and cancer development. In myeloid malignancies, various chromosomal translocations and/or mutations increased cellular reactive oxygen species (ROS), followed by DS
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A great deal of research has focused on candidate
2020-03-23

A great deal of research has focused on candidate medications to modulate dopaminergic mechanisms through which psychomotor stimulants produce addictive effects, i.e., drugs that expressly target the DA transporter, D1-like receptor, or D2-like receptors., , However, effective dopaminergic-based ph
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Clotrimazole br Experimental Procedures br Author Contributi
2020-03-23

Experimental Procedures Author Contributions Acknowledgments Research in the Davis laboratory was supported by grants 4R37NS019904, 5R01NS052351, and 1R35NS097224 from NINDS. Research in the Martemyanov laboratory was supported by grants DA036596 and DA026405 from NIDA, and MH105482 from NI
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All tested antibodies exhibited positive
2020-03-23

All tested NLG-8189 exhibited positive immunoreactivity in NSCLC tumors, with N’-epitope being the less expressed (both as overall positivity and number of positive cases, or intensity combined with number of positive cells, as provided by H-Score. This result is in accordance with previous studies
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In ER group Histopathological examination followed
2020-03-23

In ER + group, Histopathological examination followed by Fluorescence in situ hybridization (FISH) had revealed the absence of HER2 receptors. Co-targeting of ER and HER2 appears to provide benefit without a significant increase in toxicity although formal trials have not been carried out [18]. Adop
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In summary we have identified a series of amides
2020-03-23

In summary, we have identified a series of amides as ERRγ agonists with suitable potency for further development. Our SAR studies of this chemotype identified SR19881 as the most potent full agonist of ERRγ with an EC=0.39 μM in a binding assay and an EC=4.7 μM in a cell-based assay. SR19881 was als
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br STAR Methods br Acknowledgments
2020-03-23

STAR★Methods Acknowledgments We thank members of R.L. lab and F. Schweisguth for critical reading of the manuscript. We are also grateful to F. Janody, M. Miura, C. Bökel, H.D. Ryoo, G. Jiménez, the Bloomington Drosophila Stock Center, the Drosophila Genetic Resource Center, the Vienna Drosoph
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br The synthesis of these antagonists relied
2020-03-23

The synthesis of these antagonists relied heavily on Stille and Suzuki coupling reactions. The preparation of the required building blocks is presented in . Reduction of ethyl 6-bromo-2-pyridinecarboxylate with diisobutylaluminum hydride in tetrahydrofuran followed by treatment with triisopropylsi
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Alda 1 This pre GC B cell differentiation deficiency
2020-03-23

This pre-GC B cell differentiation deficiency caused by RD2 loss of function was explained at least in part by the finding that the BCL6 RD2 domain is required to repress expression of the key migration factors GRP183 and S1PR1. Downregulation of GRP183 is critically important for B cell migration i
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br Results br Discussion The results showed a surprising
2020-03-21

Results Discussion The results showed a surprising salicin of DNA in stains even at extreme environmental conditions (35–65 °C, 100% relative humidity), provided the stains had been dried prior to incubation. We had expected a rapid decay of DNA at high relative humidity but observed, on the
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It is well established that
2020-03-21

It is well established that p53 maintains genomic integrity in response to a variety of cell stresses including DNA damage and oncogenic stress among others [6], [7], [8], [9]. p53 promotes the expression of several genes to cause SB408124 synthesis arrest and to repair cellular damage. There is gro
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Previous studies showed that many steroidogenic enzymes act
2020-03-21

Previous studies showed that many steroidogenic enzymes act when the enzyme binds to the cofactor first [30]. In the present study, we showed that HPTE inhibited both AKR1C14 and RDH2 in a mixed mode when cofactor was used. This indicates that HPTE interferes with cofactor-binding residues although
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CYC202 br Genomic and non genomic
2020-03-21

Genomic and non-genomic signaling crosstalk As exemplified in the previous sections, it is evident that the mechanisms of action of estrogen in the various cell targets represent a combination of complex multifactorial processes. Besides the independent genomic and non-genomic pathways described
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The compounds listed in Table Table Table
2020-03-21

The compounds listed in Table 1, Table 2, Table 3, Table 4, Table 5 were biologically evaluated for their inhibition of the specific binding of a radiolabeled ligand [3H]PGE2 to membrane fractions prepared from cells stably expressing each mouse prostanoid receptor. The EP1 antagonist activity of th
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The mechanisms by which coregulators control
2020-03-20

The mechanisms by which coregulators control the actions of estrogen receptors are still a topic of ongoing research. From studies in cancer cells, we have learned that a large group of coregulators have specific structural motifs that than affect their contact with ER ligand-binding domains (Heery,
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