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An estrogen receptor chimera senses ligands by nuclear translocation
TLDR
A fluorescently tagged chimera between the glucocorticoid and the estrogen receptors, unlike the constitutively nuclear estrogen receptor, is cytoplasmic in the absence of hormone and translocates to the nucleus in response to estradiol, providing a clean system for drug discovery. Expand
Characterization of the phosphorylation status of the hepatitis B virus X-associated protein 2.
TLDR
Serine residues 43,53,131-2, and 329 on XAP2-FLAG were identified as putative phosphorylation sites using site-directed mutagenesis followed by two-dimensional phosphopeptide mapping analysis and all of these serine mutants were able to sequester murine AhR-YFP into the cytoplasm as well as wild-type X AP2. Expand
High-content fluorescence-based screening for epigenetic modulators.
TLDR
This chapter describes the development of mammalian cell-based fluorescent assays to screen for epigenetic modulators using an innovative combination of approaches and options for evaluating the mechanism of action are presented. Expand
Identification of Four Potential Epigenetic Modulators from the NCI Structural Diversity Library Using a Cell-Based Assay
TLDR
The characterization of a locus derepression assay is described, a fluorescence-based mammalian cellular system which was used to screen the NCI structural diversity library for novel epigenetic modulators using an automated imaging platform and four structurally unique compounds were uncovered that, when further investigated, showed distinct activities. Expand
Identification of Compounds by High-Content Screening That Induce Cytoplasmic to Nuclear Localization of a Fluorescent Estrogen Receptor α Chimera and Exhibit Agonist or Antagonist Activity In Vitro
We have completed a robust high-content imaging screen for novel estrogen receptor α (ERα) agonists and antagonists by quantitation of cytoplasmic to nuclear translocation of an estrogen receptorExpand
Development of an image analysis screen for estrogen receptor alpha (ERα) ligands through measurement of nuclear translocation dynamics
TLDR
The GFP-GRER nuclear translocation assay was very robust, with z' values >0.7, CVs <5%, and has been validated with known ER ligands, and inclusion of cytotoxicity filters will facilitate screening of natural product extracts. Expand
A phase 1 trial of TRC102 (methoxyamine HCl) with temozolomide (TMZ) in patients with solid tumors and lymphomas.
TLDR
TRC102 efficiently enhanced the antitumor effect of TMZ regardless of cell line genetic characteristics, e.g., O6-methylguanine DNA-methyltransferase, mismatch repair (MMR), or p53 status in xenograft studies. Expand
Development of a quantitative pharmacodynamic assay for apoptosis in fixed tumor tissue and its application in distinguishing cytotoxic drug—induced DNA double strand breaks from DNA double strand
TLDR
An immunofluorescence assay is described that distinguishes between apoptosis and drug-induced DSBs by measuring coexpression of γH2AX and membrane blebbing−associated CC3 to indicate apoptosis, and γ H2AX in the absence of CC3 bleBbing to indicate drug- induced DNA damage. Expand
Evaluation of Pharmacodynamic Responses to Cancer Therapeutic Agents Using DNA Damage Markers
TLDR
The clinical utility of this DDR multiplex IFA has been demonstrated in preclinical models and clinical specimens following exposure to multiple classes of cytotoxic agents, DNA repair protein inhibitors, and molecularly targeted agents, in both homologous recombination–proficient and -deficient contexts. Expand
Abstract 4678: Pilot trial of talazoparib (BMN 673), an oral PARP inhibitor, in patients with advanced solid tumors carrying deleterious BRCA mutations
TLDR
In summary, talazoparib demonstrated significant clinical activity as a single agent in patients with BRCA-deficient tumors and produced substantial reductions in tumor PAR levels in matched pre and post-treatment tumor biopsies. Expand
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