Tirapazamine: a hypoxia-activated topoisomerase II poison.

Organization of the higher-order chromatin loop: specific DNA attachment sites on nuclear scaffold

1984 • 1,088 citations

Tumor hypoxia adversely affects the prognosis of carcinoma of the head and neck

1997 • 1,057 citations

Pretreatment oxygenation predicts radiation response in advanced squamous cell carcinoma of the head and neck

1996 • 930 citations

Chromosomal loop anchorage of the kappa immunoglobulin gene occurs next to the enhancer in a region containing topoisomerase II sites

1986 • 922 citations

The hypoxic cell: a target for selective cancer therapy--eighteenth Bruce F. Cain Memorial Award lecture.

1999 • 638 citations

Mechanism of action of eukaryotic topoisomerase II and drugs targeted to the enzyme

1998 • 498 citations

Proliferation- and cell cycle-dependent differences in expression of the 170 kilodalton and 180 kilodalton forms of topoisomerase II in NIH-3T3 cells.

1991 • 450 citations

SR-4233: A new bioreductive agent with high selective toxicity for hypoxic mammalian cells

1986 • 391 citations

Topoisomerase II as a target for anticancer drugs: When enzymes stop being nice

2000 • 359 citations

Preferential, cooperative binding of DNA topoisomerase II to scaffold-associated regions.

1989 • 317 citations

Tirapazamine Plus Cisplatin Versus Cisplatin in Advanced Non–Small-Cell Lung Cancer: A Report of the International CATAPULT I Study Group

2000 • 283 citations

Therapeutic attack of hypoxic cells of solid tumors: presidential address.

1988 • 258 citations

Merbarone Inhibits the Catalytic Activity of Human Topoisomerase IIα by Blocking DNA Cleavage

1998 • 256 citations

Activation of topoisomerase II-mediated excision of chromosomal DNA loops during oxidative stress

1999 • 211 citations

Phase I Trial of Concurrent Tirapazamine, Cisplatin, and Radiotherapy in Patients With Advanced Head and Neck Cancer

2001 • 200 citations

In vitro and intracellular inhibition of topoisomerase II by the antitumor agent merbarone.

1989 • 159 citations

Stimulation of Topoisomerase II-Mediated DNA Damage via a Mechanism Involving Protein Thiolation

2001 • 154 citations

Etoposide Targets Topoisomerase IIα and IIβ in Leukemic Cells: Isoform-Specific Cleavable Complexes Visualized and QuantifiedIn Situby a Novel Immunofluorescence Technique

1998 • 145 citations

Mode of action of topoisomerase II-targeting agents at a specific DNA sequence

1992 • 121 citations

Loss of p21Waf1/Cip1 sensitizes tumors to radiation by an apoptosis-independent mechanism.

1997 • 118 citations

Sequential coexpression of the multidrug resistance genes MRP and mdr1 and their products in VP-16 (etoposide)-selected H69 small cell lung cancer cells.

1995 • 108 citations

Antagonistic effect of aclarubicin on the cytotoxicity of etoposide and 4′-(9-acridinylamino)methanesulfon-m-anisidide in human small cell lung cancer cell lines and on topoisomerase II-mediated DNA cleavage

1991 • 106 citations

The 180-kDa isoform of topoisomerase II is localized in the nucleolus and belongs to the structural elements of the nucleolar remnant

1992 • 98 citations

Sensitivity of human type II topoisomerases to DNA damage: stimulation of enzyme-mediated DNA cleavage by abasic, oxidized and alkylated lesions

2000 • 97 citations

Mapping of DNA topoisomerase II poisons (etoposide, clerocidin) and catalytic inhibitors (aclarubicin, ICRF-187) to four distinct steps in the topoisomerase II catalytic cycle

1996 • 97 citations

Growth state- and cell cycle-dependent fluctuation in the expression of two forms of DNA topoisomerase II and possible specific modification of the higher molecular weight form in the M phase.

1994 • 96 citations

Repair of DNA and chromosome breaks in cells exposed to SR 4233 under hypoxia or to ionizing radiation.

1992 • 88 citations

The response of eukaryotic topoisomerases to DNA damage

1998 • 84 citations

Decreased Mutation Rate for Cellular Resistance to Doxorubicin and Suppression of mdrl Gene Activation by the Cyclosporin PSC 833

1995 • 83 citations

The new paradigm: Integrating genomic function and nuclear architecture

1998 • 81 citations

A phase I/II evaluation of tirapazamine administered intravenously concurrent with cisplatin and radiotherapy in women with locally advanced cervical cancer

2000 • 80 citations

Enzymology of tirapazamine metabolism: a review.

1998 • 79 citations

Direct Evidence for Bimodal DNA Damage Induced by Tirapazamine

1998 • 76 citations

Cisplatin anti-tumour potentiation by tirapazamine results from a hypoxia-dependent cellular sensitization to cisplatin

1999 • 72 citations

ICE Bioassay: Isolating In Vivo Complexes of Enzyme to DNA

2003 • 68 citations

Loss of amino acids 1490Lys-Ser-Lys1492 in the COOH-terminal region of topoisomerase IIalpha in human small cell lung cancer cells selected for resistance to etoposide results in an extranuclear enzyme localization.

1997 • 63 citations

Metabolism of tirapazamine by multiple reductases in the nucleus11Abbreviations: TPZ, tirapazamine; P450 reductase, NADPH:cytochrome P450 reductase; PMSF, phenylmethylsulfonyl fluoride; DTT, dithiothreitol; DHR123, dihydrorhodamine 123; DAPI, 4′,6-diamidino-2-phenylindole, dihydrochloride; SN, supernatant from nuclei; LS, low salt; HS, high salt; and NM, nuclear matrix.

2001 • 63 citations

Discrete Localization of Different DNA Topoisomerases in HeLa and K562 Cell Nuclei and Subnuclear Fractions

1994 • 61 citations

Tirapazamine-induced DNA damage measured using the comet assay correlates with cytotoxicity towards hypoxic tumour cells in vitro

1996 • 59 citations

Spontaneous DNA Damage Stimulates Topoisomerase II-mediated DNA Cleavage

1997 • 59 citations

Tirapazamine is metabolized to its DNA-damaging radical by intranuclear enzymes.

1998 • 56 citations

Dual action of tirapazamine in the induction of DNA strand breaks.

1996 • 48 citations

Detection of hypoxia by measurement of DNA damage in individual cells from spheroids and murine tumours exposed to bioreductive drugs. II. RSU 1069

1995 • 48 citations

Active heterodimers are formed from human DNA topoisomerase II alpha and II beta isoforms.

1996 • 47 citations

Merbarone, a catalytic inhibitor of DNA topoisomerase II, induces apoptosis in CEM cells through activation of ICE/CED-3-like protease.

1999 • 45 citations

Inhibition of DNA replication by tirapazamine.

2001 • 40 citations

Nuclear Distribution of Human DNA Topoisomerase IIβ: A Nuclear Targeting Signal Resides in the 116-Residue C-Terminal Tail

1998 • 39 citations

Metabolism of the bioreductive cytotoxin SR 4233 by tumour cells: enzymatic studies

1993 • 39 citations

Etoposide targets topoisomerase IIα and IIβ in leukemic cells: Isoform-specific cleavable complexes visualized and quantified in situ by a novel immunofluorescence technique

1998 • 30 citations

Detection and quantification of melphalan-DNA adducts at the single cell level in hematopoietic tumor cells

1996 • 24 citations

Initial mechanistic studies with merbarone (NSC 336628)

1985 • 22 citations

Topoisomerase IIα content and topoisomerase II catalytic activity cannot explain drug sensitivities to topoisomerase II inhibitors in lung cancer cell lines

1996 • 18 citations

Characterization of DNA Topoisomerase IIα/β Heterodimers in HeLa Cells

1998 • 10 citations

A Distinct Subnuclear Localization of Mammalian DNA Topoisomerase IIβ in Yeast

2001 • 7 citations