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The mechanisms by which coregulators
2020-10-28
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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br Early developments Historically the advent of
2020-10-28
Early developments Historically, the advent of SMEPT can be traced to the 1980′s, where the first example of localized prodrug conversion was achieved using a judiciously placed enzyme – in order to achieve a localized feed of 5-fluorouracil (5-FU). Immobilization of E. coli-derived cytosine deam
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The imaging and biochemical data
2020-10-28
The imaging and biochemical data presented here demonstrated that in T cells, AEP played a specific function in cleaving Foxp3 but not Tbet. These results are in accordance with previous AEP studies where it has been shown that AEP substrates in part are not amenable to other protease activity. In a
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br Acknowledgements E B was supported by grant mol
2020-10-28
Acknowledgements E.B. was supported by grant 16-34-60213 mol_a_dk from the Russian Foundation for Basic Research (RFBR). R.S. and A.V. were supported by grant of the President of Russian FederationMK-4253.2018.4. The work was performed according to the Russian Government Program of Competitive Gr
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The expression of cytokine inducible
2020-10-28
The expression of cytokine-inducible genes is mediated by a number of components within the cell. It has been shown that Jak2 and the Ras/Raf/MAP kinase signaling cascades are required for the expression of DUB-1[9], [29]. However, the enhancer domain of DUB-1 lacks a consensus sequence for Stat bin
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br Introduction The identification of
2020-10-28
Introduction The identification of genetic variants that influence susceptibility to Parkinson\'s disease (PD) determines functional studies, the generation of model systems and directs therapeutic strategies. To date, classical candidate gene association studies and genome-wide approaches have f
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An important question is to what extent any differences
2020-10-28
An important question is to what extent any differences in radioligand characteristics may have contributed to discrepancies between studies. Two studies on schizophrenia addressed this question directly by using [11C]SCH 23390 and [11C]NCC 112 in the same individuals, not finding any differences be
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br Signaling of DDR receptor and its regulation Being the
2020-10-28
Signaling of DDR2 receptor and its regulation Being the tyrosine kinase receptor, downstream signaling of DDR2 receptor is initiated by phosphorylation of cytoplasmic tyrosine residue upon ligand binding (Type II collagen) but the authentic facts or detail information of tyrosine phosphorylation
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br Results and discussion Compounds were
2020-10-27
Results and discussion Compounds were tested for their binding affinity to human CRTH2 in a radioligand binding assay (3H-PGD2) using CHO cells stably transfected with human CRTH2. In addition, these compounds were assessed for their functional activity in PGD2 driven Ca2+ flux in KB8 cells expre
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br Acknowledgments We would like to thank the
2020-10-27
Acknowledgments We would like to thank the Bloomington Stock Center and the Vienna Drosophila RNAi Center for stocks used in this study. RMG was supported in part by a Professors grant to R. Losick from the HHMI and this work was supported by NSF grant 074578 to A.A.N. Introduction The catabo
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L-690,330 The in vitro cytotoxicity of the prodrugs was
2020-10-27
The in vitro cytotoxicity of the prodrugs was assessed in the LS174T human colon cell line (). The results were found to reflect the stability of the prodrugs, with the unstable urea compounds ( and ) giving relatively poor cytotoxicity differentials between prodrugs and parents (i.e., approximately
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The binding pattern of was
2020-10-27
The binding pattern of 1 was analysed by flexible molecular docking. The (±)-J 113397 receptor inserted into the narrow ATP binding site of CK2 (Fig. 2). As shown the aliphatic chain of 1 was located at the edge of the pocket and established van der Waals interactions with the side chains residues
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LP533401 hcl Although it is well established that estrogen a
2020-10-27
Although it is well established that estrogen and ESR1 mediate numerous reproductive processes, increasing evidence suggests that ESR2 also lays an integral role in reproduction. ESR2 is a mediator in folliculogenesis and may also act by stimulating ovulation and regulating luteinization (Su et al.,
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Recent studies have also uncovered additional roles for
2020-10-27
Recent studies have also uncovered additional roles for E2 enzymes and E2~Ub conjugates in modulating the activity of deubiquitinating enzymes (DUBs), such as OTUB1 (Juang et al., 2012, Wiener et al., 2013, Wiener et al., 2012). Interestingly, OTUB1 has also been shown to associate and modulate the
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The interface between the E ligase and the E enzyme
2020-10-27
The interface between the E3 ligase and the E2 enzyme can vary, and ZNF451 and SP-RING ligases stabilize this interaction via noncovalent binding to a scaffold SUMO (SUMOB) on the backside of the E2 (Cappadocia et al., 2015; Eisenhardt et al., 2015; Streich & Lima, 2016). By contrast, RanBP2 does no
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