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These findings further extend our knowledge of
2021-02-08

These findings further extend our knowledge of how P4 and/or E2 can mediate anxiety and fear responses. Female rats in behavioral estrous and ovx rats administered systemic P4 and/or E2 demonstrated significantly less anxiety in the open field and/or elevated plus maze, compared to diestrous rats, a
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br Methods br Results br Discussion There
2021-02-08

Methods Results Discussion There are two particularly important facets of the present ERK findings relevant to drug conditioning. One is the strong ERK signal observed in the medial prefrontal cortex and the nucleus accumbens during the immediate post-trial interval following the final cond
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br Introduction Rheumatoid arthritis RA is
2021-02-08

Introduction Rheumatoid arthritis (RA) is a chronic, systemic inflammatory disease that can be divided in at least two subsets based on the presence of antibodies to citrullinated proteins (ACPAs) [1]. Importantly, such ACPA target proteins [[2], [3], [4], [5]] also represent candidate autoantige
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Crystallographic and NMR based analyses have revealed that
2021-02-08

Crystallographic and NMR-based analyses have revealed that RINGs and U-boxes have a common mode of interaction with E2s (Fig. 2A). The key structural elements are two loop-like regions, which, in the case of RINGs, coordinate Zn. The loops surround a shallow groove formed by the central α-helix. Tog
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Although our knowledge of the biochemical and biological fun
2021-02-08

Although our knowledge of the biochemical and biological functions of E3 ubiquitin ligases has increased in B-cell malignancies, a deeper characterization of cell-context dependent substrate regulation and biological relevance is needed. The recent approval of a general proteasome inhibitor, VELCADE
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In plants SUMOylation has been shown to modulate plant hormo
2021-02-08

In plants, SUMOylation has been shown to modulate plant hormone signaling (Lois et al., 2003, Miura et al., 2009, Conti et al., 2014), root stem cell maintenance (Xu et al., 2013), and responses to abiotic and biotic stress (Lois, 2010). Many of the plant biological processes regulated by SUMOylatio
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The authors identified inhibitors of SUMOylation using two a
2021-02-08

The authors identified inhibitors of SUMOylation using two assays to monitor the conjugation of SUMO1 to RanGAP1 by E1 and E2 enzymes: a fluorescence resonance energy transfer (FRET) primary screen that evaluated over 250,000 compounds and a chemiluminescence secondary screen. A counter screen was u
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Many DNA repair pathways are candidates for DPC repair Nucle
2021-02-08

Many DNA repair pathways are candidates for DPC repair. Nucleotide excision repair (NER) is widely involved in both bacteria and eukaryotes in removing cross-linked protein with low molecular weights (11kDa) (Ide et al., 2011). The predominant pathway chosen by XEN445 australia may also depend on th
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Saururus chinensis Lour Baill Saururaceae a
2021-02-08

Saururus chinensis (Lour.) Baill. (Saururaceae), a perennial herb, is widely cultivated in China and southern Korea. It has been traditionally used as folk medicine for the treatment of inflammation, jaundice and gonorrhea [8]. Previous chemical studies of S. chinensis have revealed the presence of
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Epinephrine Bitartrate Ultimately we decided to investigate
2021-02-07

Ultimately, we decided to investigate the role of Cyp3a in obesity because Hepatic P450 Reductase-null (HRN) mice with no P450 activity show hepatic steatosis with increased Cyp2b10 and Cyp3a11 expression, perturbations in liver size, lipid homeostasis, and increased liver polyunsaturated fatty acid
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Published results have revealed relationships between serine
2021-02-07

Published results have revealed relationships between serine 81 in AR and some CDKs, especially CDKs 1, 5 and 9 [12], [13], [14], [15], [16]. These results are often supported by pharmacological inhibition of a certain CDK. An effect of CDK1 inhibition on suppression of S81-phosphorylation was previ
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br Clinical trials of CRM inhibitors KPT clinical trials hav
2021-02-07

Clinical trials of CRM1 inhibitors KPT-330 clinical trials have been initiated with promising very early results. One trial includes patients with advanced solid tumors whose disease has progressed after at least one prior therapy for metastatic disease (NCT01607905). Another trial includes patie
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P H is a nonheme iron
2021-02-07

P4H is a nonheme iron(II) dioxygenase that uses O2 and α-ketoglutarate as co-substrates (Fig. 1A). The three-dimensional structure of mammalian P4H is unknown. We reasoned that an electrophilic analog of α-ketoglutarate could serve as an irreversible inhibitor of the enzyme and, hence, a useful prob
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Binding affinity was measured by a scintillation
2021-02-07

Binding affinity was measured by a scintillation proximity binding assay using [H]4-OHT (ERRγ) or [H]estradiol (ERα/β) as radioligand. In all cases, the ERβ affinity was not significantly different from ERα. Compounds were compared to , which showed high affinity for both receptors and moderate (six
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The Liver X Receptor and LXRs NR H and NR
2021-02-07

The Liver X Receptor-α and -β (LXRs, NR1H3 and NR1H2, respectively) are members of the nuclear receptor superfamily that play a central role in controlling cholesterol homeostasis [9], [10]. In macrophages, LXRs can decrease the cellular sterol burden by inducing expression of the cholesterol efflux
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