Search Results - "Hertzberg, Robert P."
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Impact of high-throughput screening in biomedical research
Published in Nature reviews. Drug discovery (01-03-2011)“…Has high-throughput screening (HTS) been unfairly blamed one factor responsible for the decline in productivity in the pharmaceutical industry? This article…”
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High-throughput screening: new technology for the 21st century
Published in Current Opinion in Chemical Biology (01-08-2000)“…New technologies in high-throughput screening have significantly increased throughput and reduced assay volumes. Key advances over the past few years include…”
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Book Review Journal Article -
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Evaluation of Potent and Selective Small-Molecule Antagonists for the CXCR2 Chemokine Receptor
Published in Journal of medicinal chemistry (11-03-2004)“…N,N‘-Diarylureas were prepared, and the structure−activity relationship relative to the CXCR2 receptor was examined. This led to the identification of a potent…”
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Design and Implementation of High Throughput Screening Assays
Published in Molecular biotechnology (01-03-2011)“…High throughput screening (HTS) is at the core of the drug discovery process, and so it is critical to design and implement HTS assays in a comprehensive…”
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5
Design and Implementation of High-Throughput Screening Assays
Published in Methods in molecular biology (Clifton, N.J.) (01-01-2016)“…HTS remains at the core of the drug discovery process, and so it is critical to design and implement HTS assays in a comprehensive fashion involving scientists…”
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6
On the mechanism of topoisomerase I inhibition by camptothecin: evidence for binding to an enzyme-DNA complex
Published in Biochemistry (Easton) (30-05-1989)“…Camptothecin, a cytotoxic antitumor compound, has been shown to produce protein-linked DNA breaks mediated by mammalian topoisomerase I. We have investigated…”
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Synthesis of water-soluble (aminoalkyl)camptothecin analogs: inhibition of topoisomerase I and antitumor activity
Published in Journal of medicinal chemistry (01-01-1991)“…Water-soluble analogues of the antitumor alkaloid camptothecin (1) were prepared in which aminoalkyl groups were introduced into ring A or B. Most of the…”
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8
Design and implementation of high-throughput screening assays
Published in Methods in molecular biology (Clifton, N.J.) (01-01-2009)“…HTS is at the core of the drug discovery process, and so it is critical to design and implement HTS assays in a comprehensive fashion involving scientists from…”
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Identification of a Potent, Selective Non-peptide CXCR2 Antagonist That Inhibits Interleukin-8-induced Neutrophil Migration
Published in The Journal of biological chemistry (24-04-1998)“…Interleukin-8 (IL-8) and closely related Glu-Leu-Arg (ELR) containing CXC chemokines, including growth-related oncogene (GRO)α, GROβ, GROγ, and epithelial…”
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10
Design and implementation of high throughput screening assays
Published in Methods in molecular biology (Clifton, N.J.) (2002)“…HTS is at the core of the drug-discovery process, and so it is critical to design and implement HTS assays in a comprehensive fashion involving scientists from…”
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11
Molecular Cloning and Characterization of the Human Anaphylatoxin C3a Receptor
Published in The Journal of biological chemistry (23-08-1996)“…In a human neutrophil cDNA library, an orphan G-protein-coupled receptor, HNFAG09, with 37% nucleotide identity to the C5a receptor (C5a-R, CD88) was…”
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12
A standard operating procedure for assessing liquid handler performance in high-throughput screening
Published in Journal of biomolecular screening (01-12-2002)“…The thrust of early drug discovery in recent years has been toward the configuration of homogeneous miniaturized assays. This has allowed organizations to…”
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13
Cleavage of DNA with methidiumpropyl-EDTA-iron(II): reaction conditions and product analyses
Published in Biochemistry (Easton) (01-08-1984)“…The synthesis of methidiumpropyl-EDTA (MPE) is described. The binding affinities of MPE, MPE.Ni(II), and MPE.Mg(II) to calf thymus DNA are 2.4 X 10(4) M-1, 1.5…”
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14
In vitro and intracellular inhibition of topoisomerase II by the antitumor agent merbarone
Published in Cancer research (Chicago, Ill.) (15-05-1989)“…Merbarone has previously been shown to have antitumor activity of unknown mechanism in P388 and L1210 tumor models (A. D. Brewer et al., Biochem. Pharmacol.,…”
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15
Automated assay optimization with integrated statistics and smart robotics
Published in Journal of biomolecular screening (01-08-2000)“…The transition from manual to robotic high throughput screening (HTS) in the last few years has made it feasible to screen hundreds of thousands of chemical…”
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16
Camptothecin-resistant mutants of chinese hamster ovary cells containing a resistant form of topoisomerase I
Published in Cancer research (Chicago, Ill.) (15-11-1988)“…In Chinese hamster ovary cells, stable mutants that exhibit 250- to 350-fold resistance to camptothecin (CptR mutants) have been isolated from mutagen-treated…”
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Pyrrolo[1,4]benzodiazepine antitumor antibiotics: relationship of DNA alkylation and sequence specificity to the biological activity of natural and synthetic compounds
Published in Chemical research in toxicology (01-09-1988)“…The DNA alkylation and sequence specificity of a group of natural and synthetic pyrrolo-[1,4]benzodiazepines [P(1,4)Bs] were evaluated by using an exonuclease…”
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18
DNA sequence specificity of the pyrrolo[1,4]benzodiazepine antitumor antibiotics. Methidiumpropyl-EDTA-iron(II) footprinting analysis of DNA binding sites for anthramycin and related drugs
Published in Biochemistry (Easton) (25-03-1986)“…Anthramycin, tomaymycin, and sibiromycin are members of the pyrrolo[1,4]benzodiazepine [P(1,4)B] antitumor antibiotic group. These drugs bind covalently…”
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The role of the anionic groups in the receptor binding of interleukin-8 antagonists
Published in International journal of peptide research and therapeutics (01-05-1998)“…SummaryIn an effort to determine the role of the acidic group in the receptor binding ofN-(2-hydroxy-4-nitrophenyl)-N′-(phenyl) urea, an interleukin-8B…”
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20
Degradation of structurally modified DNAs by bleomycin group antibiotics
Published in Biochemistry (Easton) (03-05-1988)“…Bleomycin-mediated DNA strand scission has been shown to be diminished at certain sequences in proximity to 5-methylcytidines. We have investigated the…”
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