Global ETD Search
Search theses and dissertations gathered from participating repositories worldwide. Every result links back to the library that holds it. No account is needed.
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Showing 1 to 20 of 87 for “"coactivator"”.
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Neuroprotection from the huntingtin-repressed transcriptional coactivator PGC-1α
The transcriptional coactivator PPARgamma coactivator 1alpha (PGC-1α) is a regulator of mitochondrial biogenesis and function and is decreased in the striatum of patients with Huntington’s Disease (HD). HD is an autosomal dominant neurological disorder caused by a polyglutamine repeat in the …
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Design and Synthesis of Estrogen Receptor Coactivator Binding Inhibitors
… series of compounds that could be utilized as coactivator binding inhibitors (CBIs). A fluorescence-based assay was used to evaluate the ability of the CBIs to effectively block the ER-coactivator interaction. The most effective compounds synthesized were amphipathic benzene derivatives with …
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Characterization of Transcription Factor-Coactivator Complexes in Acute Lymphoblastic Leukemia
… by the recruitment of the transcriptional coactivator CBP/p300. Indeed, previous studies have shown that E2A-PBX1-mediated oncogenesis requires direct binding of E2A-PBX1 to CBP/p300. However, the transcriptional targets of this complex remain unknown. Additionally, as t(1;19)-mediated ALL …
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Mechanism of Action of ING4 as a Transcriptional Coactivator of p53
… results establish ING4 as a transcriptional coactivator of p53 and suggest two mechanisms by which p53 affects ING4 complex histone modification and transcriptional activity.</p>
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Chemical Approaches to Inhibiting the Estrogen Receptor-Steroid Receptor Coactivator Interaction
… approach, we have attempted to design de novo coactivator binding inhibitors based on a benzimidazolone scaffold. These molecules, unfortunately, only weakly bind to the estrogen receptor a.
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Identification and Biological Evaluation of Coactivator Binding Inhibitors for the Estrogen Receptor
Finally, the determination of the ER status of a tumor is invaluable in choosing most effective treatment for a breast cancer patient. In Chapter 6 we study the protein product of a highly estrogen-regulated gene, carbonic anhydrase XII and examine the potential for this enzyme to act as an …
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Synthesis and Biological Evaluation of Coactivator Binding Inhibitors and Bivalent Ligands for the Estrogen Receptor
The synthesis of steroidal bivalent ligands for ER is also reported. Two estradiol molecules were connected through a phenylethynyl linkage with chemical tethers of varying composition and length. The binding properties of the bivalent ligands for ER were measured. Moderate relative binding …
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I. Estrogen receptor-mediated inhibition of inflammatory signaling: Implications for treatment of breast cancer II. Small molecule coactivator-binding inhibitors
… inhibit the binding of the estrogen receptor to coactivator proteins that facilitate transcription. We used a peptidomimetic approach to mimic conserved amino acids on the coactivator proteins. Compounds designed in this way did not inhibit the interaction between the estrogen receptor and a …
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A four-and-a-half LIM protein FHL2 acts as a coactivator for the Wilms' tumor suppressor WT1 during gonadal differentiation
… the MIS gene. Importantly, so far no bona fide coactivators for WT1 have been described.
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Design and Synthesis of Small Molecule Regulators of Steroid Receptor Action
… is to prevent transcription via the creation of coactivator binding inhibitors. The estrogen receptor contains a region in the ligand binding domain where coactivator proteins for transcription are able to dock. Using a small molecule specifically designed to bind to this region with a high …
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Regulation of Pyruvate Dehydrogenase Kinase 4 by Thyroid Hormone / Role of Peroxisome Proliferator Activated Receptor Gamma Coactivator-1 alpha and Ccaat Enhancer Binding Protein
… thyroid hormone receptor (TR), transcriptional coactivators especially the peroxisome proliferator activated receptor gamma coactivator-1 (PGC-1α) and other transcription factors that act as accessory factors in T3 actions. </p> <p>Thyroid hormone receptors (TRα or TRβ) are part of the nuclear …
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Second-site inhibitors of the estrogen and androgen hormone receptors
… efforts to directly disrupt the nuclear receptor/coactivator and the nuclear receptor/DNA interactions, and to increase degradation of receptor through binding of small-molecules at non-traditional binding sites. Due to the essential nature of these interactions for estrogen and androgen receptor …
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Interaction of the DNA -Bound Estrogen Receptor With Coregulatory Proteins
… Although the role of ligand in altering coactivator recruitment and transcription has been well documented, the effect of DNA-binding on coregulator recruitment has not been addressed. On binding to the estrogen response elements (EREs) in the target genes the ERs undergo DNA-induced …
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Interactions of Steroid Hormone Receptors With Coactivators and DNA
… response elements (HREs) on DNA, recruiting coactivators and then chromatin remodeling complexes and ultimately the basal transcription machinery. In vivo data suggests that the components of transcription complexes at HREs undergo rapid exchange and replacement. Using our Fluorescence …
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The Dual Role of OCA-B in B Cell Development and Signaling
<p>OCA-B (Oct coactivator from B cells) is a B-cell specific coactivator of transcription that acts in conjunction with the ubiquitously expressed activator, OCT-1 or the B cell-restricted OCT-2. OCT-1 or OCT-2 can bind an upstream octamer element with the consensus sequence 5'-ATGCAAAT-3' in …
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Development and Application of a Fluorescence Anisotropy Microplate Assay for Analyzing the Interaction of Steroid Hormone Receptors With DNA and Coactivators
… transcription is the recruitment of P160 coactivators by ER. The FAMA represents the first reliable in vitro assay for the binding of full-length P160 coactivators to the ERE-ER complex. Binding of full-length SRC1a to the ERE-ERalpha and ERE-ERbeta complex occurred only in the presence of …
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Regulation of SRC-3 localization and dynamics by phosphorylation during ERα-dependent transcriptional activation
… these factors involves either the recruitment of coactivators or corepressors and direct interaction with the basal transcriptional machinery (1). Hormone-activated nuclear receptors (NRs) are well characterized transcriptional factors (2) that bind to the promoters of their target genes and …
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Spatial and temporal coordination of genome segregation with activation of the Mitotic Exit Network
… recruitment of terminal MEN kinase Dbf2 and its coactivator Mob1. We further show that the Hippo-like kinase Cdc15 phosphorylates Nud1. Finally, we present evidence that Mob1 is a novel class of phosphopeptide binding domains. Thus, Cdc15-dependent phosphorylation of the scaffold Nud1 creates a …
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