Molecular, cellular, and clinical aspects of the pharmacology of 20(S)camptothecin and its derivatives

Plant Antitumor Agents. I. The Isolation and Structure of Camptothecin, a Novel Alkaloidal Leukemia and Tumor Inhibitor from Camptotheca acuminata^1,2

1966 • 2,159 citations

DNA TOPOISOMERASE POISONS AS ANTITUMOR DRUGS

1989 • 1,799 citations

Arrest of replication forks by drug-stabilized topoisomerase I-DNA cleavable complexes as a mechanism of cell killing by camptothecin.

1989 • 1,030 citations

Intracellular roles of SN-38, a metabolite of the camptothecin derivative CPT-11, in the antitumor effect of CPT-11.

1991 • 855 citations

Identification of mammalian DNA topoisomerase I as an intracellular target of the anticancer drug camptothecin.

1988 • 843 citations

DNA Topoisomerases: Essential Enzymes and Lethal Targets

1994 • 722 citations

DNA Topoisomerase I—Targeted Chemotherapy of Human Colon Cancer in Xenografts

1989 • 645 citations

The Current Status of Camptothecin Analogues as Antitumor Agents

1993 • 614 citations

On the mechanism of topoisomerase I inhibition by camptothecin: evidence for binding to an enzyme-DNA complex

1989 • 533 citations

Synthesis of water-soluble (aminoalkyl)camptothecin analogs: inhibition of topoisomerase I and antitumor activity

1991 • 513 citations

Metabolic fate of irinotecan in humans: correlation of glucuronidation with diarrhea.

1994 • 503 citations

A kinetic and Mechanistic Study of the Hydrolysis of Camptothecin and Some Analogues

1992 • 456 citations

Structure-activity study of the actions of camptothecin derivatives on mammalian topoisomerase I: evidence for a specific receptor site and a relation to antitumor activity.

1989 • 445 citations

Isolation of type I and II DNA topoisomerase mutants from fission yeast: single and double mutants show different phenotypes in cell growth and chromatin organization.

1984 • 444 citations

Topoisomerase-targeting antitumor drugs

1989 • 441 citations

Drug-target interactions: only the first step in the commitment to a programmed cell death?

1991 • 412 citations

DNA topoisomerases: why so many?

1991 • 375 citations

Differential requirement of DNA replication for the cytotoxicity of DNA topoisomerase I and II inhibitors in Chinese hamster DC3F cells.

1989 • 368 citations

Induction of Multidrug Resistance in Human Cells by Transient Exposure to Different Chemotherapeutic Drugs

1993 • 366 citations

Phase I and pharmacologic study of topotecan: a novel topoisomerase I inhibitor.

1992 • 363 citations

Eukaryotic DNA topoisomerases: two forms of type I DNA topoisomerases from HeLa cell nuclei.

1981 • 350 citations

Recent studies of DNA topoisomerases

1987 • 323 citations

The structural basis of camptothecin interactions with human serum albumin: impact on drug stability

1994 • 316 citations

Phase I clinical trial of weekly and daily treatment with camptothecin (NSC-100880): correlation with preclinical studies.

1972 • 315 citations

Camptothecins: from bench research to hospital wards.

1994 • 314 citations

Phase I and pharmacokinetic trial of weekly CPT-11.

1993 • 300 citations

Metabolism and pharmacokinetics of the camptothecin analogue CPT-11 in the mouse.

1990 • 292 citations

Characterization of a mammalian mutant with a camptothecin-resistant DNA topoisomerase I.

1987 • 291 citations

Comparison of Topoisomerase I Inhibition, DNA Damage, and Cytotoxicity of Camptothecin Derivatives Presently in Clinical Trials

1994 • 291 citations

Phase I Study of Weekly Intravenous Infusions of CPT-11, a New Derivative of Camptothecin, in the Treatment of Advanced Non-Small-Cell Lung Cancer

1991 • 275 citations

Constitutive expression of human Bcl-2 modulates nitrogen mustard and camptothecin induced apoptosis.

1993 • 275 citations

Phase II study of camptothecin (NSC-100880) in the treatment of advanced gastrointestinal cancer.

1972 • 271 citations

A high affinity topoisomerase I binding sequence is clustered at DNAase I hypersensitive sites in tetrahymena R-chromatin

1985 • 256 citations

Preliminary pharmacologic and clinical evaluation of camptothecin sodium (NSC-100880).

1970 • 246 citations

Proliferation-dependent regulation of DNA topoisomerase II in cultured human cells.

1988 • 244 citations

Elevation of topoisomerase I messenger RNA, protein, and catalytic activity in human tumors: demonstration of tumor-type specificity and implications for cancer chemotherapy.

1994 • 243 citations

Protein-linked DNA strand breaks induced in mammalian cells by camptothecin, an inhibitor of topoisomerase I.

1989 • 243 citations

Plant antitumor agents. 18. Synthesis and biological activity of camptothecin analogs

1980 • 232 citations

Synthesis and Antitumor Activity of 20(S)-Camptothecin Derivatives: Carbamate-Linked, Water-Soluble Derivatives of 7-Ethyl-10-hydroxycamptothecin.

1991 • 231 citations

Camptothecin cytotoxicity in mammalian cells is associated with the induction of persistent double strand breaks in replicating DNA

1991 • 228 citations

Decreased expression of DNA topoisomerase I in camptothecin-resistant tumor cell lines as determined by a monoclonal antibody.

1990 • 226 citations

Antitumor effect of CPT-11, a new derivative of camptothecin, against pleiotropic drug-resistant tumors in vitro and in vivo

1988 • 213 citations

Studies on the Antitumor Activity, Mechanism of Action, and Cell Cycle Effects of Camptothecin

1971 • 213 citations

beta-Lapachone, a novel DNA topoisomerase I inhibitor with a mode of action different from camptothecin.

1993 • 212 citations

Effect of P-glycoprotein expression on the accumulation and cytotoxicity of topotecan (SK&F 104864), a new camptothecin analogue.

1992 • 212 citations

Nucleotide sequence preference at rat liver and wheat germ type 1 DNA topoisomerase breakage sites in duplex SV40 DNA

1984 • 208 citations

Interaction between replication forks and topoisomerase I-DNA cleavable complexes: studies in a cell-free SV40 DNA replication system.

1993 • 207 citations

Effect of local DNA sequence on topoisomerase I cleavage in the presence or absence of camptothecin.

1991 • 199 citations

Phase I and pharmacological study of the novel topoisomerase I inhibitor 7-ethyl-10-[4-(1-piperidino)-1-piperidino]carbonyloxycamptothecin (CPT-11) administered as a ninety-minute infusion every 3 weeks.

1994 • 195 citations

Action of camptothecin on mammalian cells in culture.

1972 • 190 citations

The S-phase cytotoxicity of camptothecin

1991 • 190 citations

DNA is linked to the rat liver DNA nicking-closing enzyme by a phosphodiester bond to tyrosine.

1981 • 188 citations

Complete growth inhibition of human cancer xenografts in nude mice by treatment with 20-(S)-camptothecin.

1991 • 179 citations

Metabolic Activation of CPT-11, 7-Ethyl-10-(4-(1-piperidino)-1-piperidino)carbonyloxycamptothecin, a Novel Antitumor Agent, by Carboxylesterase.

1994 • 170 citations

Preferential Binding of the Carboxylate Form of Camptothecin by Human Serum Albumin

1993 • 168 citations

Establishment of a camptothecin analogue (CPT-11)-resistant cell line of human non-small cell lung cancer: Characterization and mechanism of resistance

1991 • 168 citations

Phase I trial of low-dose continuous topotecan infusion in patients with cancer: an active and well-tolerated regimen.

1994 • 166 citations

Antagonism between camptothecin and topoisomerase II-directed chemotherapeutic agents in a human leukemia cell line.

1991 • 165 citations

Antitumor activity of a camptothecin derivative, CPT-11, against human tumor xenografts in nude mice

1991 • 163 citations

Therapeutic efficacy of the topoisomerase I inhibitor 7-ethyl-10-(4-[1-piperidino]-1-piperidino)-carbonyloxy-camptothecin against human tumor xenografts: lack of cross-resistance in vivo in tumors with acquired resistance to the topoisomerase I inhibitor 9-dimethylaminomethyl-10-hydroxycamptothecin.

1993 • 161 citations

Camptothecin overcomes MDR1-mediated resistance in human KB carcinoma cells.

1991 • 159 citations

Synergistic cell killing by ionizing radiation and topoisomerase I inhibitor topotecan (SK&F 104864).

1991 • 154 citations

Phase I and pharmacokinetic study of the camptothecin derivative irinotecan, administered on a weekly schedule in cancer patients.

1994 • 151 citations

Strand breakage by the DNA untwisting enzyme results in covalent attachment of the enzyme to DNA.

1977 • 150 citations

Poly(ADP-ribosylation) of a DNA topoisomerase.

1983 • 145 citations

Molecular cloning of a cDNA of a camptothecin-resistant human DNA topoisomerase I and identification of mutation sites

1991 • 144 citations

Phosphorylation of mammalian DNA topoisomerase I and activation by protein kinase C.

1990 • 143 citations

Relationship between Development of Diarrhea and the Concentration of SN‐38, an Active Metabolite of CPT‐11, in the Intestine and the Blood Plasma of Athymic Mice Following Intraperitoneal Administration of CPT‐11

1993 • 142 citations

Relationship between the intracellular effects of camptothecin and the inhibition of DNA topoisomerase I in cultured L1210 cells.

1987 • 141 citations

CPT-11 Converting Enzyme from Rat Serum: Purification and Some Properties.

1991 • 139 citations

Phase I Clinical and Pharmacology Study of Topotecan Given Daily for 5 Consecutive Days to Patients With Advanced Solid Tumors, With Attempt at Dose Intensification Using Recombinant Granulocyte Colony-Stimulating Factor

1993 • 135 citations

Elevated expression of DNA topoisomerase II in camptothecin-resistant human tumor cell lines.

1990 • 133 citations

Phase I study of topotecan for pediatric patients with malignant solid tumors.

1994 • 132 citations

Identification and kinetics of a ?-glucuronide metabolite of SN-38 in human plasma after administration of the camptothecin derivative irinotecan

1995 • 128 citations

Camptothecin-resistant mutants of Chinese hamster ovary cells containing a resistant form of topoisomerase I.

1988 • 125 citations

Development of a stable camptothecin-resistant subline of P388 leukemia with reduced topoisomerase I content.

1990 • 124 citations

Phase I and pharmacokinetics study of topotecan, a new topoisomerase I inhibitor

1993 • 123 citations

Phase I Study and Pharmacokinetics of CPT-11 With 5-Day Continuous Infusion

1992 • 122 citations

DNA topoisomerase I and II as targets for rational design of new anticancer drugs

1993 • 121 citations

P-glycoprotein expression and DNA topoisomerase I and II activity in benign tumors of the ovary and in malignant tumors of the ovary, before and after platinum/cyclophosphamide chemotherapy.

1991 • 120 citations

Identification of a mutant human topoisomerase I with intact catalytic activity and resistance to 9-nitro-camptothecin.

1994 • 119 citations

Overexpression of human topoisomerase I in baby hamster kidney cells: hypersensitivity of clonal isolates to camptothecin.

1992 • 114 citations

Experimental studies on biochemical modulation targeting topoisomerase I and II in human tumor xenografts in nude mice

1992 • 112 citations

A phase I clinical and pharmacokinetic study of the topoisomerase I inhibitor topotecan (SK&F 104864) given as an intravenous bolus every 21 days

1992 • 112 citations

Reversed-phase high-performance liquid chromatographic method for the simultaneous quantitation of the carboxylate and lactone forms of the camptothecin derivative irinotecan, CPT-11, and its metabolite SN-38 in plasma

1994 • 110 citations

Sequential administration of camptothecin and etoposide circumvents the antagonistic cytotoxicity of simultaneous drug administration in slowly growing human colon carcinoma HT-29 cells

1992 • 109 citations

Camptothecin, teniposide, or 4'-(9-acridinylamino)-3-methanesulfon-m-anisidide, but not mitoxantrone or doxorubicin, induces degradation of nuclear DNA in the S phase of HL-60 cells.

1991 • 109 citations

Nonlinear pharmacokinetics of CPT-11 in rats.

1990 • 109 citations

High-performance liquid chromatographic analysis of the new antitumour drug SK&F 104864-A (NSC 609699) in plasma

1990 • 104 citations

Identification of the metabolites of irinotecan, a new derivative of camptothecin, in rat bile and its biliary excretion

1991 • 101 citations

Camptothecin resistance from a single mutation changing glycine 363 of human DNA topoisomerase I to cysteine.

1993 • 101 citations

Detection of topoisomerase I gene point mutation in CPT-11 resistant lung cancer cell line

1992 • 100 citations

Kinetics of the in vivo interconversion of the carboxylate and lactone forms of irinotecan (CPT-11) and of its metabolite SN-38 in patients.

1994 • 100 citations

Posttreatment exposure to camptothecin enhances the lethal effects of x-rays on radioresistant human malignant melanoma cells

1992 • 97 citations

Plasma and cerebrospinal fluid pharmacokinetic study of topotecan in nonhuman primates.

1993 • 96 citations

Phase I and pharmacologic study of irinotecan in combination with cisplatin for advanced lung cancer

1993 • 94 citations

Mapping of the Active Site Tyrosine of Eukaryotic DNA Topoisomerase I

1989 • 94 citations

Pediatric phase I trial and pharmacokinetic study of topotecan administered as a 24-hour continuous infusion.

1993 • 93 citations

Antineoplastic Agents from Plants

1977 • 93 citations

Identification of an N-terminal domain of eukaryotic DNA topoisomerase I dispensable for catalytic activity but essential for in vivo function.

1992 • 93 citations

Sequence specificity of DNA topoisomerase I in the presence and absence of camptothecin.

1987 • 93 citations

Diverse effects of camptothecin, an inhibitor of topoisomerase I, on the cell cycle of lymphocytic (L1210, MOLT-4) and myelogenous (HL-60, KG1) leukemic cells.

1990 • 93 citations

Mechanisms of camptothecin resistance in yeast DNA topoisomerase I mutants.

1993 • 91 citations

Complete inhibition of growth followed by death of human malignant melanoma cells in vitro and regression of human melanoma xenografts in immunodeficient mice induced by camptothecins.

1992 • 89 citations

Ethyl substitution at the 7 position extends the half-life of 10-hydroxycamptothecin in the presence of human serum albumin

1993 • 87 citations

Cloning of Chinese hamster DNA topoisomerase I cDNA and identification of a single point mutation responsible for camptothecin resistance.

1993 • 86 citations

Phase I/pharmacokinetic study of topotecan by 24-hour continuous infusion weekly.

1994 • 86 citations

Sequence-dependent effect of camptothecin on human topoisomerase I DNA cleavage

1988 • 85 citations

Minimal DNA duplex requirements for topoisomerase I-mediated cleavage in vitro.

1990 • 83 citations

Eukaryotic topoisomerase I-mediated cleavage requires bipartite DNA interaction. Cleavage of DNA substrates containing strand interruptions implicates a role for topoisomerase I in illegitimate recombination

1993 • 82 citations

Characterization of camptothecin-resistant chinese hamster lung cells

1992 • 81 citations

Simultaneous determination of the camptothecin analogue CPT-11 and its active metabolite SN-38 by high-performance liquid chromatography: application to plasma pharmacokinetic studies in cancer patients

1992 • 76 citations

Camptothecin hyper-resistant P388 cells: drug-dependent reduction in topoisomerase I content.

1992 • 74 citations

Increased expression of DNA topoisomerase I gene and collateral sensitivity to camptothecin in human cisplatin-resistant bladder cancer cells.

1994 • 74 citations

Topoisomerase I alteration in a camptothecin-resistant cell line derived from Chinese hamster DC3F cells in culture.

1992 • 71 citations

Regression of human breast carcinoma tumors in immunodeficient mice treated with 9-nitrocamptothecin: differential response of nontumorigenic and tumorigenic human breast cells in vitro.

1993 • 66 citations

Camptothecin and its derivatives induce expression of the c-jun protooncogene in human myeloid leukemia cells.

1991 • 66 citations

Preferential relaxation of supercoiled DNA containing a hexadecameric recognition sequence for topoisomerase I

1987 • 64 citations

Sequential modifications of topoisomerase I activity in a camptothecin-resistant cell line established by progressive adaptation

1993 • 63 citations

Plasma pharmacokinetics of lactone and carboxylate forms of 20(S)-camptothecin in anesthetized rats.

1993 • 63 citations

Camptothecin derivatives induce regression of human ovarian carcinomas grown in nude mice and distinguish between non‐tumorigenic and tumorigenic cells in vitro

1993 • 60 citations

Induction of cleavage in topoisomerase I c-DNA by topoisomerase I enzymes from calf thymus and wheat germ in the presence and absence of camptothecin

1993 • 58 citations

Pharmacokinetics of the in vivo and in vitro conversion of 9-nitro-20(S)-camptothecin to 9-amino-20(S)-camptothecin in humans, dogs, and mice.

1994 • 58 citations

Topoisomerase I Interaction with SV4O DNA in the presence and absence of camptothecin

1988 • 57 citations

Analysis of the active lactone form of 9-aminocamptothecin in plasma using solid-phase extraction and high-performance liquid chromatography

1994 • 57 citations

Camptothecin induces differentiation and stimulates the expression of differentiation-related genes in U-937 human promonocytic leukemia cells.

1992 • 57 citations

Potentiation of radioimmunotherapy by inhibition of topoisomerase I.

1994 • 50 citations

Mechanism of cross-resistance to a camptothecin analogue (CPT-11) in a human ovarian cancer cell line selected by cisplatin.

1992 • 50 citations

Structural modifications of camptothecin and effects on topoisomerase I inhibition

1992 • 46 citations

Phase I and pharmacokinetic studies of topotecan administered as a 72 or 120 h continuous infusion

1994 • 43 citations

Pharmacokinetics of the 9-amino and 10,11-methylenedioxy derivatives of camptothecin in mice.

1993 • 41 citations

Inhibitory Activity of Camptothecin Derivatives Against Acetylcholinesterase in Dogs and Their Binding Activity to Acetylcholine Receptors in Rats

1993 • 40 citations

Expression of the topoisomerase I gene in serum stimulated human fibroblasts

1990 • 39 citations

Characterization of an altered DNA catalysis of a camptothecin-resistant eukaryotic topoisomerase I

1993 • 37 citations

Cytotoxic efficacy of 9-nitrocamptothecin in the treatment of human malignant melanoma cells in vitro.

1994 • 37 citations

Camptothecin analogues: studies from The Johns Hopkins Oncology Center

1994 • 37 citations

Clinical studies of irinotecan alone and in combination with cisplatin

1994 • 35 citations

Preclinical and phase I trials of topoisomerase I inhibitors

1994 • 34 citations

S-Phase Population Analysis Does Not Correlate with the Cytotoxicity of Camptothecin and 10,11-Methylenedioxycamptothecin in Human Colon Carcinoma HT-29 Cells

1991 • 34 citations

Collateral drug sensitivity induced in CPT-11 (a novel derivative of camptothecin)-resistant cell lines

1990 • 34 citations

Phosphorylation of human topoisomerase I by protein kinase C in vitro and in phorbol 12-myristate 13-acetate-activated HL-60 promyelocytic leukaemia cells

1993 • 32 citations

YeastSaccharomyces cerevisiae as a model system to study the cytotoxic activity of the antitumor drug camptothecin

1994 • 31 citations

A Reversed-Phase HPLC Method For Determining Camptothecin In Plasma With Specificity For the Intact Lactone Form of the Drug

1991 • 30 citations

Differential expression of DNA topoisomerase I gene between CPT-11 acquired-and native-resistant human pancreatic tumor cell lines: Detected by RNAPCR-based quantitation assay

1992 • 30 citations

Importance of replication fork progression for the induction of chromosome damage and SCE by inhibitors of DNA topoisomerases

1993 • 29 citations

Clinical, pharmacokinetic and biological studies of topotecan

1994 • 27 citations

High-performance liquid chromatographic analysis of the antitumour drug camptothecin and its lactone ring-opened form in rat plasma

1993 • 25 citations

Limited sampling models for topotecan pharmacokinetics

1994 • 25 citations

Synergistic effect of inhibitors of topoisomerase I and II on chromosome damage and cell killing in cultured Chinese hamster ovary cells

1994 • 23 citations

Quantitative analysis of DNA topoisomerase I activity in human and rat glioma: Characterization and mechanism of resistance to antitopoisomerase chemical, camptothecin‐11

1993 • 23 citations

9‐nitro‐camptothecin delays growth of U‐937 leukemia tumors in nude mice and is cytotoxic or cytostatic for human myelomonocytic leukemia lines in vitro

1993 • 22 citations

Higher G2 sensitivity to the induction of chromosomal damage in the CHO mutant EM9 than in its parental line AA8 by camptothecin, an inhibitor of DNA topoisomerase I

1993 • 22 citations

Establishment of a CPT-11-resistant human ovarian cancer cell line.

1994 • 19 citations

Topoisomerase expression in cancer cell lines and clinical samples

1994 • 16 citations

Studies of the differentiation properties of camptothecin in the human leukaemic cells K562

1991 • 13 citations

7-Ethyl-10-[4-(1-piperidino)-1-piperidino] carbonyloxy camptothecin: mechanism of resistance and clinical trials

1994 • 13 citations

Characterization of a camptothecin‐resistant human DNA topoisomerase I in an in vitro system for Simian virus 40 DNA replication

1991 • 12 citations

The DNA topoisomerase I inhibitor camptothecin blocks postmitotic reformation of nucleoli in mammalian cells.

1993 • 11 citations

Effect of CPT on the calf thymus Topoisomerase I-mediated DNA breakage-reunion reaction: Optimal conditions for the formation and reversal of the CPT trapped Topoisomerase I cleavable complex

1993 • 8 citations

Development of resistance to 9-nitro-camptothecin by human leukemia U-937 cells in vitro correlates with altered sensitivities to several anticancer drugs

1994 • 8 citations

Some pharmacological properties of a new antitumor drug, CPT-11, in isolated muscle preparations

1989 • 6 citations

Semi‐quantitative Analysis of DNA Topoisomerase‐I mRNA Level Using Reverse Transcription‐Polymerase Chain Reaction in Cancer Cell Lines: Its Relation to Cytotoxicity against Camptothecin Derivative

1994 • 6 citations

A NEW DERIVATIVE OF CAMPTOTHECIN, IRINOTECAN HYDROCHLORIDE (CPT-11) INDUCES PROGRAMMED CELL-DEATH IN LEUKEMIA-LYMPHOMA CELL-LINES

1993 • 2 citations

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