The current status of camptothecin analogues as antitumor agents

Journal of the National Cancer Institute

Volumn 85, Issue 4, 1993, Pages 271-291

  Slichenmyer, William J ^a   Rowinsky, Eric K ^a   Donehower, Ross C ^a   Kaufmann, Scott H ^a  

^a JOHNS HOPKINS UNIVERSITY   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

CAMPTOTHECIN; DNA TOPOISOMERASE; IRINOTECAN; TOPOTECAN;

ANTINEOPLASTIC ACTIVITY; CANCER SCREENING; CANCER THERAPY; CELL CYCLE; COLORECTAL CANCER; DNA REPLICATION; DRUG MECHANISM; DRUG METABOLISM; ENZYME REGULATION; GENETIC TRANSCRIPTION; HUMAN; IMMUNOBLOTTING; LUNG CANCER; NEUTROPENIA; NONHODGKIN LYMPHOMA; OVARY CANCER; PHASE 1 CLINICAL TRIAL; PHASE 2 CLINICAL TRIAL; PRIORITY JOURNAL; RETROSPECTIVE STUDY; REVIEW; STRUCTURE ACTIVITY RELATION; THROMBOCYTOPENIA; UTERINE CERVIX CANCER;

ANIMAL; ANTINEOPLASTIC AGENTS, PHYTOGENIC; CAMPTOTHECIN; CLINICAL TRIALS; COMBINED MODALITY THERAPY; DNA TOPOISOMERASES, TYPE I; FORECASTING; HUMAN; SUPPORT, U.S. GOV'T, P.H.S.; TOPOTECAN;

EID: 0027447420     PISSN: 00278874     EISSN: None     Source Type: Journal    
DOI: 10.1093/jnci/85.4.271     Document Type: Review

References (260)

1. Wall ME, Wani MC, Cook CE, et al: Plant antitumor agents. I. The isolation and structure of camptothecin, a novel alkaloidal leukemia and tumor inhibitor from Camptotheca acuminata. J Am Chem Soc 88:3888-3890, 1966
2. Horwitz SB, Chano CSCK, Grollman AP: Studies on camptothecin: I. Effects on nucleic acid and protein synthesis. Mol Pharmacol 7:632-644, 1971
3. Kessel D: Effects of camptothecin on RNA synthesis in leukemia L1210 cells. Biochim Biophys Acta 246:225-232, 1971
4. Abelson HT, Penman S: Selective interruption of high molecular weight RNA synthesis in HeLa cells by camptothecin. Nature New Biol 237:144-146, 1972
5. Kessel D, Bosmann HB, Lohr K: Camptothecin effects on DNA synthesis in murine leukemia cells. Biochim Biophys Acta 269:210216, 1972
6. Abelson HT, Penman S: Selective interruption of RNA metabolism by chemotherapeutic agents. Handb Exp Pharmakol 38:571-581, 1974
7. Horwttz M, Horwitz S: Intracellular degradation of HeLa and adenovirus type 2 DNA induced by camptothecin. Biochem Biophys Res Commun 45:723-727, 1971
8. Horwttz SB, Horwttz MS: Effects of camptothecin on the breakage and repair of DNA during the cell cycle. Cancer Res 33:2834-2836, 1973
9. Spataro A, Kessel D: The effects of camptothecin on mammalian DNA. Biochim Biophys Acta 331:194-201, 1973
10. Gellert M: DNA topoisomerases. Arm Rev Biochem 50:879-910, 1981
11. Vosbero HP: DNA topoisomerase: Enzymes that control DNA conformation. Curr Top Microbiol Immunol 114:19-102, 1985
12. Wang JC: DNA topoisomerases. Ann Rev Biochem 54:665-697, 1985
13. D’Arpa P, Lru LF: Topoisomerase-targeting antitumor drugs. Biochim Biophys Acta 989:163-177, 1989
14. Schneider E, Hsiang YH, Lru L: DNA topoisomerases as anticancer drug targets. Adv Pharmacol 21:149-183, 1990
15. Osheroff N: Biochemical basis for the interactions of type I and type II topoisomerases with DNA. Pharmacol Ther 41:223-241, 1989
16. Liu LF, Miller KG: Eukaryotic DNA topoisomerases: Two forms of type I DNA topoisomerases from HeLa cell nuclei. Proc Natl Acad Sci USA 78:3487-3491, 1981
17. Schmitt B, Buhre U, Vosbero HP: Characterisation of size variants of type I DNA topoisomerase isolated from calf thymus. Eur J Biochem 144:127-134, 1984
18. Shero J, Bordwell B, Rothfield N, et al: High titers of autoantibodies to topoisomerase I (scl-70) in sera from scleroderma patients. Science 231:737-740, 1986
19. D’Arpa P, Machlin PS, Ratrie H III, et al: cDNA cloning of human DNA topoisomerase I: Catalytic activity of a 67.7 Kda carboyxl-terminal fragment. Proc Natl Acad Sci U S A 85:2543-2547, 1988
20. Juan C, Hwang J, Liu A, et al: Human DNA topoisomerase I is encoded by a single-copy gene that maps to chromosome region 20ql2-13.2. Proc Natl Acad Sci USA 85:8910-8913, 1988
21. Champoux J: Evidence for an intermediate with a single-strand break in the reaction catalyzed by the DNA untwisting enzyme. Proc Naü Acad Sci USA 73:3488-3491, 1976
22. Champoux J: Mechanism of the reaction catalyzed by the DNA untwisting enzyme: Attachment of the enzyme to the 3'-terminus of the nicked DNA. J Mol Biol 118:441-446, 1978
23. Champoux J: DNA is linked to the rat liver DNA nicking-closing enzyme by a phosphodiester bond to tyrosine. J Biol Chem 256:4805-4809, 1981
24. Lynn R, Bjornsti MA, Caron P, et al: Peptide sequencing and site-directed mutagenesis identify tyrosine-727 as the active site tyrosine of Saccharomyces cerevisiae DNA topoisomerase I. Proc Natl Acad Sci U S A 86:3559-3563, 1989
25. Eng WK, Pandit SD, Sternglanz R: Mapping of the active site tyrosine of eukaryotic DNA topoisomerase I. J Biol Chem 264:13373-13376, 1989
26. Liu L, Wang J: Supercoiling of the DNA template during RNA transcription. Proc Natl Acad Sci USA 84:7024-7027, 1987
27. Brill S, Sternglanz R: Transcription-dependent DNA supercoiling in yeast DNA topoisomerase mutants. Cell 54:403-411, 1988
28. Gilmour DS, Pfluofelder G, Wano JC, et al: Topoisomerase I interacts with transcribed regions in Drosophila cells. Cell 44:401407, 1986
29. CAMtLLONt G, Di Marttno E, Caserta M, et al: Eukaryotic DNA topoisomerase I reaction is topology dependent. Nucleic Acids Res 16:7071-7085, 1988
30. Camilloni G, Di Martino E, Di Mauro E, et al: Regulation of the function of eukaryotic DNA topoisomerase I: Topological conditions for inactivity. Proc Natl Acaid Sci USA 86:3080-3084, 1989
31. Muller M: Quantitation of eukaryotic topoisomerase I reactivity with DNA. Preferential cleavage of supercoiled DNA. Biochim Biophys Acta 824:263-267, 1985
32. Fleischmann G, Pfluofelder G, Steiner EK, et al: Drosophila DNA topoisomerase I is associated with transcriptionally active regions of the genome. Proc Natl Acad Sci USA 81:6958-6962, 1984
33. Muller M, Pfund W, Mehta V, et al: Eukaryotic type I topoisomerase is enriched in the nucleolus and catalytically active on ribosomal DNA. EMBO J 4:1237-1243, 1985
34. Zhang H, Wang J, Liu L: Involvement of DNA topoisomerase l in transcription of human ribosomal RNA genes. Proc Natl Acad Sci USA 85:1060-1064, 1988
35. Stewart AF, Schütz G: Camptothecin-induced in vivo topoisomerase I cleavages in the transcriptionally active tyrosine aminotransferase gene. Cell 50:1109-1117, 1987
36. Gilmour DS, Eloin SC: Localization of specific topoisomerase I interactions within the transcribed region of active heat shock genes by using the inhibitor camptothecin. Mol Cell Biol 7:141-148, 1987
37. Kroeoer PE, Rowe TC: Interaction of topoisomerase I with the transcribed region of the Drosophila hsp 70 heat shock gene. Nucleic Acids Res 17:8495-8509, 1989
38. Eoyhazi E, Durban E: Microinjection of anti-topoisomerase I immunoglobulin G into nuclei of chironomus tentans salivary gland cells leads to blockage of transcription elongation. Mol Cell Biol 7:4308-4316, 1987
39. Garo LC, Diangelo S, Jacob ST: Role of DNA topoisomerase 1 in the transcription of supercoiled rRNA gene. Proc Natl Acad Sci USA 84:3185-3188. 1987
40. Uemura T, Yanacida M: Isolation of type I and II DNA mutants from fission yeast: Single and double mutants show different phenotypes in cell growth and chromatin organization. EMBO J 3:1737-1744, 1984
41. Thrash C, Voelkel K, Dinardo S, et al: Identification of Saccharomyces cerevisiae mutants deficient in DNA topoisomerase I activity. J Biol Chem 259:1375-1377, 1984
42. Goto T, Wang JC: Cloning of yeast TOPI, the gene encoding DNA topoisomerase I, and construction of mutants defective in both DNA topoisomerase I and DNA topoisomerase II. Proc Natl Acad Sci USA 82:7178-7182, 1985
43. Naoata K, Guooenheimer R, Hurwitz J: Adenovirus DNA replication in vitro: Synthesis of full-length DNA with purified proteins. Proc Natl Acad Sci USA 80:4266-4270, 1983
44. Yang L, Wold MS, Li JJ, et al: Roles of DNA topoisomerases in simian virus 40 DNA replication in vitro. Proc Natl Acad Sci USA 84:950-954, 1987
45. Kim RA, Wang JC: Function of DNA topoisomerases as replication swivels in Saccharomyces cerevisiae. J Mol Biol 208:257-267, 1989
46. Taudou G, Mirambeau G, Lavenot C, et al: DNA topoisomerase activities in concanavalin A-stimulated lymphocytes. FEBS Lett 176:431-435, 1984
47. Heck MM, Earnshaw WC: Topoisomerase II: A specific marker for cell proliferation. J Cell Biol 103:2569-2581, 1986
48. Kaufmann S, McLaughlin S, Kaštan M, et al: Topoisomerase II levels during granulocytic maturation in vitro and in vivo. Cancer Res 51:3534-3543, 1991
49. Hwang JL, Shyy SH, Chen AY, et al: Studies of topoisomerase-specific antitumor drugs in human lymphocytes using rabbit antisera against recombinant human topoisomerase II polypeptide. Cancer Res 49:958-962, 1989
50. Kaufmann SH: Additional members of the rat liver lamin polypeptide family. J Biol Chem 264:13946-13955, 1989
51. Potměšil M, Hsiang YH, Liu L, et al: Resistance of human leukemic and normal lymphocytes to drug-induced DNA cleavage and low levels of DNA topoisomerase II. Cancer Res 48:3537-3543, 1988
52. Giovanella BC, Stehlin JS, Wall ME, et al: DNA topoisomerase targeted chemotherapy of human colon cancer in xenografts. Science 246:1046-1048, 1989
53. Champoux J: Proteins that affect DNA conformation. Ann Rev Biochem 47:449-479, 1978
54. Champoux J, Youno L, Been M: Studies on the regulation and specificity of the DNA-untwisting enzyme. Cold Spring Harbor Symposium. Quant Mol Biol 43:53-58, 1979
55. Hsiang YH, Wu HY, Liu L: Proliferation-dependent regulation of DNA topoisomerase II in cultured human cells. Cancer Res 48:3230-3235, 1988
56. Romig H, Richter A: Expression of the topoisomerase I gene in serum stimulated human fibroblasts. Biochim Biophys Acta 1048:274-280, 1990
57. Duouet M, Lavenot C, Harper F, et al: DNA topoisomerases from rat liver: Physiological variations. Nucleic Acids Res 11:1059-1075, 1983
58. Kunze N, Yano G, Dolbero M, et al: Structure of the human type I DNA topoisomerase gene. J Biol Chem 266:9610-9616, 1991
59. Hirabayashi N, Kim R, Nishiyama M, et al: Tissue expression of topoisomerase I and II in digestive tract cancers and adjacent normal tissues. Proc Am Assoc Cancer Res 33:436, 1992
60. van der Zee AG, Hollema H, deJong S, et al: 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. Cancer Res 51:5915-5920, 1991
61. Potmesil M, Hsiano Y-H, Liu LF, et al: Topoisomerase I (topo-I) and topoisomerase II (topo-II) levels in high and low grade lymphomas. Proc Am Assoc Cancer Res 29:176, 1988
62. Samuels D, Shimizu Y, Shimizu N: Protein kinase C phosphorylâtes DNA topoisomerase I. FEBS Lett 259:57-60, 1989
63. Pommier Y, Kerrigan D, Hartman KD, et al: Phosphorylation of mammalian DNA topoisomerase I and activation by protein kinase C. J Biol Chem 265:9418-9422, 1990
64. kinase C. J Biol Chem 267:11156-11162, 1992
65. Kerrigan D, Pommier Y: Protein kinase C activity influences camptothecin-mediated DNA strand breaks and cytotoxicity in DC3F/9-OHE, Chinese hamster cells resistant to topoisomerase D inhibitors. Proc Am Assoc Cancer Res 31:437, 1990
66. Utsugi T, Mattern MR, Mirabelu CK, et al: Potentiation of topoisomerase inhibitor-induced DNA strand breakage and cytotoxicity by tumor necrosis factor: Enhancement of topoisomerase activity as a mechanism of potentiation. Cancer Res 50:2636-2640, 1990
67. Nambi P, Mattern M, Bartus JO, et al: Stimulation of intracellular topoisomerase I activity by vasopressin and thrombin. Differential regulation by pertussis toxin. Biochem J 262:485-489, 1989
68. Mattern MR, Mong S, Mono SM, et al: Transient activation of topoisomerase I in leukotriene D4 signal transduction in human cells. Biochem J 265:101-107, 1990
69. Jongstra-Bilen J, Ittel ME, Niedergang C, et al: DNA topoisomerase I from calf thymus is inhibited in vitro by poly(ADP-ribosylation). Eur J Biochem 136:391-396, 1983
70. Ferro A, Olivera B: Poly(ADP-ribosylation) of DNA topoisomerase I from calf thymus. J Biol Chem 259:547-554, 1984
71. Kasid U, Halligan B, Liu L, et al: Poly(ADP-ribose)-mediated post-translational modification of chromatin-associated human topoisomerase I. Inhibitory effects on catalytic activity. J Biol Chem 264:18687-18692, 1989
72. Adamietz P: Poly(ADP-ribose) synthase is the major endogenous nonhistone acceptor for poly(ADP-ribose) in alkylated rat hepatoma cells. Eur J Biochem 169:365-372, 1987
73. Krupitza G, Cerutti P: ADP-ribosylation of ADPR-transferase and topoisomerase 1 in intact mouse epidermal cells JB6. Biochemistry 28:2034-2040, 1989
74. Liu LF: DNA topoisomerase poisons as antitumor drugs. Ann Rev Biochem 58:351-375, 1989
75. Hsiang Y-H, Hertzbero R, Hecht S, et al: Camptothecin induces protein-linked DNA breaks via mammalian DNA topoisomerase I. J Biol Chem 260:14873-14878, 1985
76. Mattern MR, Mono SM, Bartus HF, et al: Relationship between the intracellular effects of camptothecin and the inhibition of DNA topoisomerase I in cultured L1210 cells. Cancer Res 47:1793-1798, 1987
77. Hsiang YH, Liu LF: Identification of mammalian DNA topoisomerase I as an intracellular target of the anticancer drug camptothecin. Cancer Res 48:1722-1726, 1988
78. Covey JM, Jaxel C, Kohn KW, et al: Protein-linked DNA strand breaks induced in mammalian cells by camptothecin, an inhibitor of topoisomerase I. Cancer Res 49:5016-5022, 1989
79. Kaufmann SH: Antagonism between camptothecin and topoisomerase 11-directed chemotherapeutic agents in a human leukemia cell line. Cancer Res 51:1129-1136, 1991
80. Svejstrup J, Christiansen K, Gromova I, et al: New technique for uncoupling the cleavage and religation reactions of eukaryotic topoisomerase I. The mode of action of camptothecin at a specific recognition site. J Mol Biol 222:669-678, 1991
81. Porter SE, Champoux JJ: The basis for camptothecin enhancement of DNA breakage by eukaryotic topoisomerase I. Nucleic Acids Res 17:8521-8532, 1989
82. Jaxel C, Kohn KW, Pommier Y: Topoisomerase I interaction with SV40 DNA in the presence and absence of camptothecin. Nucleic Acids Res 16:11157-11170, 1988
83. Champoux J, Aronoff R: The effects of camptothecin on the reaction and the specificity of the wheat germ type I topoisomerase. J Biol Chem 264:1010-1015, 1989
84. Jaxel C, Capranico G, Kerrigan D, et al: Effect of local DNA sequence on topoisomerase I cleavage in the presence or absence of camptothecin. J Biol Chem 266:20418-20423, 1991
85. Hertzbero RP, Caranfa MJ, Hecht SM: On the mechanism of topoisomerase I inhibition by camptothecin: Evidence for binding to an enzyme-DNA complex. Biochemistry 28:4629-4638, 1989
86. Creasy WA, Richards M, Gil D, et al: Action of (s)-10-hydroxycamptothecin on P388 leukemia and distribution of the drug in mice. Cancer Treat Rep 67:179-182, 1983
87. Hertzbero RP, Caranfa MJ, Holden KG, et al: Modification of the hydroxy lactone ring of camptothecin: Inhibition of mammalian topoisomerase I and biological activity. J Med Chem 32:715-720, 1989
88. Hsiang YH, Liu LF, Wall ME, et al: DNA topoisomerase I-mediated DNA cleavage and cytotoxicity of camptothecin analogues. Cancer Res 49:4385-4389, 1989
89. Jaxel C, Kohn KW, Wani MC, et al: 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. Cancer Res 49:1465-1469, 1989
90. Kingsbury WD, Boehm JC, Jakas DR, et al: Synthesis of water-soluble (aminoalkyl) camptothecin analogues: Inhibition of topoisomerase I and antitumor activity. J Med Chem 34:98-107, 1991
91. Nrnss J, Wang JC: DNA topoisomerase-targeting antitumor drugs can be studied in yeast. Proc Natl Acad Sci U S A 85:7501-7505, 1988
92. Eng W-K, Faucette L, Johnson RK, et al: Evidence that DNA topoisomerase I is necessary for the cytotoxic effects of camptothecin. Mol Pharmacol 34:755-760, 1988
93. Bjornsti MA, Benedetti P, Viguanti GA, et al: Expression of human DNA topoisomerase I in yeast cells lacking yeast DNA topoisomerase I: Restoration of sensitivity of the cells to the antitumor drug camptothecin. Cancer Res 49:6318-6323, 1989
94. Madden KR, Champoux J: Overexpression of human topoisomerase I in baby hamster kidney cells: Hypersensitivity of clonal isolates to camptothecin. Cancer Res 52:525-532, 1992
95. Li LH, Fraser TJ, Olin EJ, et al: Action of camptothecin on mammalian cells in culture. Cancer Res 32:2643-2650, 1972
96. Drewtnko B, Freireich EJ, Gottlieb JA: Lethal activity of camptothecin sodium on human lymphoma cells. Cancer Res 34:747750, 1974
97. D’Arpa P, Beardmore C, Liu LF: Involvement of nucleic acid synthesis in cell killing mechanisms of topoisomerase poisons. Cancer Res 50:6919-6924, 1990
98. Avemann K, Knippers R, Roller T, et al: Camptothecin, a specific inhibitor of type I DNA topoisomerase, induces DNA breakage at replication forks. Mol Cell Biol 8:3026-3034, 1988
99. Shin CG, Snapka RM: Exposure to camptothecin breaks leading and lagging strand simian virus 40 DNA replication forks. Biochem Biophys Res Commun 168:135-140, 1990
100. Ryan AJ, Squires S, Strutt HL, et al: Camptothecin cytotoxicity in mammalian cells is associated with the induction of persistent double strand breaks in replicating DNA. Nucleic Acids Res 19:3295-3300, 1991
101. Hsiang YH, Lihou MG, Liu LF: Arrest of replication forks by drug-stabilized topoisomerase I-DNA cleavable complexes as a mechanism of cell killing by camptothecin. Cancer Res 49:5077-5082, 1989
102. Zhang H, D’Arpa P, Liu L: A model for tumor cell killing by topoisomerase poisons. Cancer Cells 2:23-27, 1990
103. Holm C.-JM, Kerrigan D, et al: Differential requirement of DNA replication for the cytotoxicity of DNA topoisomerase I and II inhibitors in Chinese hamster DC3F cells. Cancer Res 49:6365-6368, 1989
104. Giovanella BC, Hinz HR, Kozielski AJ, et al: Complete growth inhibition of human cancer xenografts in nude mice by treatment with 20-(s)-camptothecin. Cancer Res 51:3052-3055, 1991
105. Chatterjee S, Cheno MF, Trivedi D, et al: Camptothecin hypersensitivity in poly(adenosine diphosphate-ribose) polymerase-deficient cell lines. Cancer Commun 1:389-394, 1989
106. O’Connor PM, Nieves-Neira W, Kerrioan D, et al: S-phase population analysis does not correlate with the cytotoxicity of camptothecin and 10,11 ethylenedioxycamptothecin in human colon carcinoma HT-29 cells. Cancer Commun 3:233-240, 1991
107. Huang C, Han CS, Yue XF, et al: Cytotoxicity and sister chromatid exchanges induced in vitro by six anticancer drugs developed in the People’s Republic of China. JNCI 71:841-847, 1983
108. Degrassi F, De Salvia R, Tanzarella C, et al: Induction of chromosomal aberrations and SCE by camptothecin, an inhibitor of mammalian topoisomerase I. Mutat Res 211:125-130, 1989
109. Been M, Champoux J: DNA breakage and closure by rat liver type 1 topoisomerase: Separation of the half-reactions by using a singlestranded DNA substrate. Proc Natl Acad Sci U S A 78:2883-2887, 1981
110. Halligan B, Davis J, Edwards K, et al: Intra- and intermolecular strand transfer by HeLa DNA topoisomerase I. J Biol Chem 257:3995-4000, 1982
111. Bullock P, Champoux J, Botchan M: Association of crossover points with topoisomerase I cleavage sites: A model for nonhomologous recombination. Science 230:954-958, 1985
112. Shuman S: Vaccinia DNA topoisomerase I promotes illegitimate recombination in Escherichia coli. Proc Natl Acad Sci U S A 86:3489-3493, 1989
113. Bendixen C, Thomsen B, Alsner J, et al: Camptothecin-stabilized topoisomerase I-DNA adducts cause premature termination of transcription. Biochemistry 29:5613-5619, 1990
114. Tobey RA: Effects of cytosine arabinoside, daunomycin, mithra-mycin, azacytidine, adriamycin, and camptothecin on mammalian cell cycle traverse. Cancer Res 32:2720-2725, 1972
115. Zucker RM, Elstein KH: A new action for topoisomerase inhibitors. Chem Biol Interact 79:31-40, 1991
116. Tsao YP, D’Arpa P, Liu L: The involvement of active DNA synthesis in camptothecin-induced G2 arrest: Altered regulation of P34cdc2/cyclin Bl. Cancer Res 52:1823-1829, 1992
117. Tobey R: Different drugs arrest cells at a number of distinct stages in G2. Nature 254:245-247, 1975
118. Lau C, Pardee A: Mechanism by which caffeine potentiates lethality of nitrogen mustard. Proc Natl Acad Sci USA 79:2942-2946, 1982
119. Lock R, Ross W: Inhibition of p34cdc2 kinase activity by etoposide or irradiation as a mechanism of G2 arrest in Chinese hamster ovary cells. Cancer Res 50:3761-3766, 1990
120. O’Connor P, Ferris D, White G, et al: Relationships between cdc2 kinase, DNA cross-linking, and cell cycle perturbations induced by nitrogen mustard. Cell Growth Differ 3:43-52, 1992
121. Lock R: Inhibition of P34cdc2 kinase activation, p34cdc2 dephosphorylation, and mitotic progression in Chinese hamster ovary cells exposed to etoposide. Cancer Res 52:1817-1822, 1992
122. Chou S, Kaneko M, Nakaya K, et al: Induction of differentiation of human and mouse myeloid leukemia cells by camptothecin. Biochem Biophys Res Commun 166:160-167, 1990
123. Ling YH, Tseng MT, Nelson JA: Differentiation induction of human promyelocytic leukemia cells by 10-hydroxycamptothecin, a DNA topoisomerase I inhibitor. Differentiation 46:135-141, 1991
124. McSheehy PM, Gervasoni M, Lampasona V, et al: Studies of the differentiation properties of camptothecin in the human leukaemic cells K562. Eur J Cancer 27:1406-1411, 1991
125. Aller P, Rius C, Mata F, et al: Camptothecin induces differentiation and stimulates the expression of differentiation-related genes in U-937 human promonocytic leukemia cells. Cancer Res 52:1245-1251, 1992
126. Wani MA, Snapka RM: Drug-induced loss of unstably amplified genes. Cancer Invest 8:587-593, 1990
127. Wani MA, Strayer JM, Snapka RM: Hypersensitivity to low level cytotoxic stress in mouse cells with high levels of DHFR gene amplification. Anticancer Drugs 1:67-75, 1990
128. Snapka RM: Gene amplification as a target for cancer chemotherapy. Oncol Res 4:145-150, 1992
129. Von Hoff D, Waddelow T, Forseth B, et al: Hydroxyurea accelerates loss of extrachromosomally amplified genes from tumor cells. Cancer Res 51:6273-6279, 1991
130. Kaufmann SH: Induction of endonucleolytic DNA cleavage in human acute myelogenous leukemia cells by etoposide, camptothecin, and other cytotoxic anticancer drugs. A cautionary note. Cancer Res 49:5870-5878, 1989
131. Del Bino G, Darzynkiewicz Z: 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. Cancer Res 51:1165-1169, 1991
132. Kharbanda S, Rubin E, Gunji H, et al: Camptothecin and its derivatives induce expression of the c-jun protooncogene in human myeloid leukemia cells. Cancer Res 51:6636-6642, 1991
133. Del Bino G, Lassota P, Darzynkiewicz Z: The S-phase cytotoxicity of camptothecin. Exp Cell Res 193:27-35, 1991
134. Sorenson C, Barry M, Eastman A: Analysis of events associated with cell cycle arrest at G2 phase and cell death induced by cisplatinum. J Natl Cancer Inst 82:749-754, 1990
135. Gunji H, Kharbanda S, Kufe D: Induction of intemucleosomal DNA fragmentation in human myeloid leukemia cells by 1-b-d-arabinofuranosylcytosine. Cancer Res 51:741-743, 1991
136. Del Bino G, Skierski JS, Darzynkiewicz Z: The concentration-dependent diversity of effects of DNA topoisomerase I and II inhibitors on the cell cycle of HL-60 cells. Exp Cell Res 195:485-491, 1991
137. Wani MC, Ronman PE, Lindley JT, et al: Plant antitumor agents. 18. Synthesis and biological activity of camptothecin analogues. J Med Chem 23:554-560, 1980
138. Grochow LB, Rowinsky EK, Johnson R, et al: Pharmacokinetics and pharmacodynamics of topotecan in patients with advanced cancer. Drug Metab Dispos 20:706-712, 1992
139. Wall M, Wani M: Antineoplastic agents from plants. Ann Rev Pharmacol Toxicol 17:117-132, 1977
140. Dewys WD, Humphreys SR, Goldin A: Studies on therapeutic effectiveness of drugs with tumor weight and survival time indices of Walker 256 carcinosarcoma. Cancer Chemother Rep 52:229-242, 1968
141. Gallo RC, Whano-Peno J, Adamson RH: Studies on the antitumor activity, mechanism of action, and cell cycle effects of camptothecin. J Natl Cancer Inst 46:789-795, 1971
142. Venditti JM, Abbott BJ: Studies on oncolytic agents from natural sources. Correlation of activity against animal tumors and clinical effectiveness. Lloydia 30:332-348, 1967
143. Venditti JM: Treatment schedule dependency of experimentally active antileukemic (L1210) drugs. Cancer Chemother Rep 2:35-59, 1971
144. Schaeppi U, Fleischman RW, Cooney DA: Toxicity of camptothecin (NSC-100880). Cancer Chemother Rep 5:25-36, 1974
145. Guarino AM, Anderson JB, Starkweather DK, et al: Pharmacologic studies of camptothecin (NSC-100880): Distribution, plasma protein binding, and biliary excretion. Cancer Chemother Rep 57:125-140, 1973
146. Gottlieb JA, Guarino AM, Call JB, et al: Preliminary pharmacologic and clinical evaluation of camptothecin sodium (NSC-100880). Cancer Chemother Rep 54:461-470, 1970
147. Muooia FM, Creaven PJ, Hansen H, et al: Phase I clinical trial of weekly and daily treatment with camptothecin (NSC-100880): Correlation with preclinical studies. Cancer Chemother Rep 56:515-521, 1972
148. Xu B, Jui-ting C, Jin-lono Y, et al: New results in pharmacologic research of some anticancer agents. In Proceedings of US-China Pharmacology Symposium, Committee on Scholarly Communication with the People’s Republic of China (Bums JJ, Tsuchitani PJ, eds). New York, 1979, pp 151-188
149. Gottlieb JA, Luce JK: Treatment of malignant melanoma with camptothecin (NSC-100880). Cancer Chemother Rep 56:103-105, 1972
150. Moertel CG, Schutt AJ, Reitemeier RJ, et al: Phase II study of camptothecin (NSC-100880) in the treatment of advanced gastrointestinal cancer. Cancer Chemother Rep 56:95-101, 1972
151. Hart LG, Call JB, Oliverio VT: A fluorometric method for determination of camptothecin in plasma and urine. Cancer Chemother Rep 53:211-214, 1969
152. Guarino AM, Hart LG, Call JB, et al: Studies of the physiologic disposition of the antitumor agent, camptothecin sodium (NSC-100880), in rodents. Proc Am Assoc Cancer Res 10:33, 1969
153. Creaven PJ, Allen LM, Muggia FM: Plasma camptothecin (NSC-100880) levels during a 5-day course of treatment: Relation to dose and toxicity. Cancer Chemother Rep 56:573-578, 1972
154. Smith PL, Liehr JG, Jacob S, et al: Pharmacokinetics of tritium labeled camptothecin in nude mice. Proc Am Assoc Cancer Res 33:432, 1992
155. Burris HA III, Hanauske A-R, Johnson RK, et al: Activity of topotecan, a new topoisomerase I inhibitor, against human tumor colony-forming units in vitro. J Natl Cancer Inst 84:1816-1820, 1992
156. Johnson RK, Hertzbero RP, Kingsbury WD, et al: Preclinical profile of SK and F 104864, a water-soluble analog of camptothecin. Presented at the Sixth NCI-EORTC Symposium on New Drugs in Cancer Therapy, Amsterdam, March, 1991
157. Johnson RK, McCabe FL, Gallagher G, et al: Comparative efficacy of topotecan, irinotecan, camptothecin and 9-amino-camptothecin in preclinical tumor models. In Proceedings on the Seventh NCI-EORTC Symposium on New Drugs in Cancer Therapy, Amsterdam, 1992, p 85
158. Houghton PJ, Cheshire PJ, Myers L, et al: Evaluation of 9-dimethylaminomethyl-10-hydroxycamptothecin (topotecan) against xenografts derived from adult and childhood tumors. In Proceedings of the Seventh NCI-EORTC Symposium on New Drugs in Cancer Therapy, Amsterdam, 1992, p 84
159. Rowinsky EK, Grochow LB, Hendricks CB, et al: Phase 1 and pharmacologic study of topotecan: A novel topoisomerase I inhibitor. J Clin Oncol 10:647-656, 1992
160. Murphy B, Saltz L, Sirott M, et al: Granulocyte-colony stimulating factor (G-CSF) does not increase the maximum tolerated dose (MTD) in a phase I study of topotecan. Proc ASCO 11:139, 1992
161. Rowinsky EK, Sartorius S, Grochow L: Phase I and pharmacologic study of topotecan, an inhibitor of topoisomerase 1, with granulocyte colony stimulating factor (G-CSF): Toxicologic differences between concurrent and post-treatment G-CSF administration. Proc ASCO 11:116, 1992
162. Verweu J, Lund B, Beynen J, et al: Clinical studies with topotecan: The EORTC Experience. In Proceedings of the Seventh NCI-EORTC Symposium on New Drugs in Cancer Therapy, Amsterdam, 1992, p 118
163. Sirott MN, Saltz L, Young C, et al: Phase 1 and clinical pharmacologic study of intravenous topotecan (T). Proc ASCO 10:104, 1991
164. Haas NB, Lacreta FP, Walczak J, et al: Phase I/pharmacoki-netic trial of topotecan on a weekly 24-hour infusion schedule. Proc Am Assoc Cancer Res 33:523, 1992
165. Beran M, O’Brien S, Estey E, et al: Topotecan (topo) in patients with refractory and relapsed acute leukemia. In Proceedings of the Fourth Conference on DNA Topoisomerases in Therapy, 1992, p 54
166. Recondo G, Abbruzzese J, Newman B, et al: A phase I trial of topotecan (topo) administered by a 24-hr infusion. Proc Am Assoc Cancer Res 32:206, 1991
167. Cole D, Blaney S, Balis F, et al: A phase 1 and pharmacokinetic study of topotecan in pediatric patients. Proc ASCO 11:116, 1992
168. Wall J, Burris H, Rodriguez G, et al: Phase 1 trial of topotecan (SK and F 104864) in patients with refractory solid tumors. Proc ASCO 10:98, 1991
169. Burris H, Kuhn K, Wall J, et al: Early clinical trials of topotecan, a new topoisomerase I inhibitor. In Proceedings of the Seventh NCI-EORTC Symposium on New Drugs in Cancer Therapy, Amsterdam, 1992, p 118
170. Ten Bokkel Huintnk WW, Rodenhuis S, Beunen, J, et al: Phase I study of the topoisomerase I inhibitor topotecan (SK & F 104864). Proc ASCO 11:110, 1992
171. Tong W, Saltz L, Sirott M, et al: Rapid HPLC assay for topotecan (T). Proc Am Assoc Cancer Res 32:433, 1991
172. Kuhn J, Burris S, Wall J, et al: Pharmacokinetics of the topoisomerase I inhibitor, SK and F 104864. Proc ASCO 9:70, 1990
173. Beunen JH, Smith BR, Keuer WJ, et al: High-performance liquid chromatographic analysis of the new antitumour drug SK&F 104864-a (NSC 609699) in plasma. J Pharm Biomed Anal 8:789-794, 1990
174. Kuhn J, Burris H, Irvin R, et al: Pharmacokinetics of topotecan following a 30 minute infusion or 3 day continuous infusion. In Proceedings of the Seventh NCI-EORTC Symposium on New Drugs in Cancer Therapy, Amsterdam, 1992, p 83
175. Staubus AE, Rutherford M, Snuffer P, et al: Kinetics of ring opening of camptothecin analogs and topotecan in plasma and whole blood. Proc Am Assoc Cancer Res 33:531, 1992
176. Kaneda N, Nagata H, Furuta T, et al: Metabolism and pharmacokinetics of the camptothecin analogue CPT-11 in the mouse. Cancer Res 50:1715-1720, 1990
177. Kawato Y, Aonuma M, Hirota Y, et al: Intracellular roles of SN-38, a metabolite of the camptothecin derivative CPT-11, in the antitumor effect of CPT-11. Cancer Res 51:4187-4191, 1991
178. Kunimoto T, Nitta K, Tanaka T, et al: Antitumor activity of 7-ethyl-10-[4-(l-piperidino)-l-piperidino]carbonyloxy-camptothecin, a novel water-soluble derivative of camptothecin, against murine tumors. Cancer Res 47:5944-5947, 1987
179. Furuta T, Yokokura T, Mutai M: Antitumor activity of CPT-11 against rat Walker 256 carcinoma. Jpn J Cancer Chemother 15:2757-2760, 1988
180. Bissery MC, Mathieu-Boue A, Lavelle F: Preclinical evaluation of CPT-11, a camptothecin derivative. Proc Am Assoc Cancer Res 32:402, 1991
181. Bissery MC, Mathieu-Boue A, Lavelle F: Experimental anti-tumor activity of CPT-11 in vitro and in vivo. In Proceedings of the Seventh NCI-EORTC Symposium on New Drugs in Cancer Therapy, Amsterdam, 1992, p 82
182. Matsuzaki T, Yokokura T, Mutai M, et al: Inhibition of spontaneous and experimental metastasis by a new derivative of camptothecin, CPT-11, in mice. Cancer Chemother Pharmacol 21:308-312, 1988
183. Tsuruo T, Matsuzaki T, Matsushita M, et al: Antitumor effect of CPT-11, a new derivative of camptothecin, against pleiotropic drug-resistant tumors in vitro and in vivo. Cancer Chemother Pharmacol 21:71-74, 1988
184. Kawato Y, Furuta T, Aonuma M, et al: Antitumor activity of a camptothecin derivative, CPT-11, against human tumor xenografts in nude mice. Cancer Chemother Pharmacol 28:192-198, 1991
185. Wang Y, Inoue K, Shibata H: Preclinical evaluation of a new camptothecin derivative, CPT-11, on the subrenai capsule assay. Jpn J Cancer Chemother 14:1264-1270, 1987
186. Ohe Y, Sasaki Y, Shinkai T, et al: Pharmacokinetics with a 5-day continuous-infusion of a camptothecin derivative, CPT-11. Proc ASCO 10:117, 1991
187. Negoro S, Fukuoka M, Masuda N, et al: 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. J Natl Cancer Inst 83:1164-1168, 1991
188. Rothenberg ML, Kuhn J, Burris HA: A phase I and pharmacokinetic trial of CPT-11 in patients with refractory solid tumors. Proc ASCO 11:113, 1992
189. Rowinsky E, Grochow L, Ettinger D, et al: Phase I and pharmacologic study of CPT-11, a semisynthetic topoisomerase I-targeting agent, on a single dose schedule. Proc ASCO 11:115, 1992
190. Gandia D, Armand JP, Chabot G, et al: A phase I study of CPT-11 (camptothecin-11) administered every 3 weeks in advanced cancer patients. In Proceedings of the Seventh NCI-EORTC Symposium on New Drugs in Cancer Therapy, Amsterdam, 1992, p 82
191. Gandia D, Armand JP, Chabot G: Phase I study of the new camptothecin analogue CPT-11 administered every 3 weeks. Proc Am Assoc Cancer Res 33:260, 1992
192. Clavel M, Mathieu-Boue A, Dumortier A, et al: Phase I study of CPT-11 administered as a daily infusion for 3 consecutive days. Proc Am Assoc Cancer Res 33:262, 1992
193. Culine S, De Forni M, Extra JM, et al: Phase I study of the camptothecin analogue CPT-11, using a weekly schedule. Proc ASCO 11:110, 1992
194. Tsuri T, Kaneda N, Kado K, et al: CPT-11 converting enzyme from rat serum: Purification and some properties. J Pharmacobiodyn 14:341-349, 1991
195. Fukuoka M, Niitani H, Suzuki A, et al: A phase II study of CPT-11, a new derivative of camptothecin for previously untreated non-small cell lung cancer. J Clin Oncol 10:16-20, 1992
196. Ohno R, Okada K, Masaoka T, et al: An early phase II study of CPT-11: A new derivative of camptothecin, for the treatment of leukemia and lymphoma. J Clin Oncol 8:1907-1912, 1990
197. Masuda N, Fukuoka M, Kusunoki Y, et al: CPT-11: A new derivative of camptothecin for the treatment of refractory or relapsed small cell lung cancer. J Clin Oncol 10:1225-1229, 1992
198. Shimada Y, Yoshino M, Wakui A, et al: Phase II study of CPT-11, a new camptothecin derivative, in patients with metastatic colorectal cancer. Proc ASCO 10:135, 1991
199. Takeuchi S, Takamizawa H, Takeda Y, et al: Clinical study of CPT-11, camptothecin derivative, on gynecological malignancy. Proc ASCO 10:189, 1991
200. Takeuchi S, Noda K, Yakushui M: Late phase II study of CPT-11, topoisomerase I inhibitor, in advanced cervical carcinoma. Proc ASCO 11:224, 1992
201. Neooro S, Fukuoka M, Niitani H, et al: Phase II study of CPT-11, a new camptothecin derivative, in small cell lung cancer (SCLC). Proc ASCO 10:241, 1991
202. Tsuda H, Takatsuki K, Ohno R, et al: A late phase II trial of a potent topoisomerase I inhibitor, CPT-11, in malignant lymphoma. Proc ASCO 11:316, 1992
203. Kanzawa F, Kondoh H, Kwon SJ, et al: Role of carboxylesterase on metabolism of camptothecin analogue (CPT-11) in non-small lung cancer cell line PC-7 cells. Proc Am Assoc Cancer Res 33:427, 1992
204. Rothenbero ML, Kuhn J, Burris HA, et al: CPT-11: Phase I experience using a weekly schedule. In Proceedings of the Seventh NCI-EORTC Symposium on New Drugs in Cancer Therapy, Amsterdam, 1992, p 119
205. Kaneda N, Yokokura T: Nonlinear pharmacokinetics of CPT-11 in rats. Cancer Res 50:1721-1725, 1990
206. Chabot G, Abigerges D, Gandia D, et al: Pharmacokinetic-pharmacodynamic relationships in patients administered with CPT-11, a new camptothecin analogue. Proc Am Assoc Cancer Res 33:266, 1992
207. Chabot G, De Forni M, Gandi D, et al: Comparative pharmacokinetics of the camptothecin analogue CPT-11 and its active metabolite SN-38, using three different schedules in phase I trials. In: Proceedings of NC1-EORTC Symposium on New Drugs in Cancer Therapy, Amsterdam, 1992, p 82
208. Sasaki Y, Morita M, Miya T, et al: Pharmacokinetic and pharmacodynamic analysis of CPT-11 and its active metabolite SN-38. Proc ASCO 11:111, 1992
209. Katz EJ, Vick JS, Kling KM, et al: Effect of topoisomerase modulators on cisplatin cytotoxicity in human ovarian carcinoma cells. Eut J Cancer 26:724-727, 1990
210. Drewinko B, Green C, Loo TL: Combination chemotherapy in vitro with cis-dichlorodiammineplatinum(II). Cancer Treat Rep 60:1619-1625, 1976
211. Kano Y, Suzuki K, Akutsu M, et al: Effects of CPT-11 in combination with other anti-cancer agents in culture. Int J Cancer 50:604-610, 1992
212. Johnson R, McCabe F, Yu Y: Combination regimens with topotecan in animal tumor models. In Proceedings of the Seventh NCI-EORTC Symposium on New Drugs in Cancer Therapy, Amsterdam, 1992, p 85
213. Masuda N, Fukuoka M, Takada M, et al: CPT-11 in combination with cisplatin for advanced non-small cell lung cancer. J Clin Oncol 10:1775-1780, 1992
214. Drewinko B, Loo TL, Freireich EJ: Combination chemotherapy in vitro. III. BCNU. Cancer Treat Rep 63:373-375, 1979
215. Oguro M: A topoisomerase I inhibitor, CPT-11: Its enigmatic antitumor activity in combination with other agents in vitro. In Proceedings of the Third Conference on Topoisomerases, 1990, p 35
216. Bertrand R, O’Connor P, Kerrigan D, et al: Sequential administration of camptothecin and etoposide circumvents the antagonistic cytotoxicity of simultaneous drug administration in slowly growing human colon-carcinoma HT-29 cells. Eur J Cancer 28A:743-748, 1992
217. Anzai H, Frost P, Abbruzzese JL: Synergistic cytotoxicity with combined inhibition of topoisomerase (topo) I and II. Proc Am Assoc Cancer Res 33:431, 1992
218. Tewey K, Rowe T, Yang L, et al: Adriamycin-induced DNA damage mediated by mammalian topoisomerase II. Science 226:466-468, 1984
219. Kim R, Hirabayashi N, Nishiyama M, et al: Experimental studies on biochemical modulation targeting topoisomerase I and II in human tumor xenografts in nude mice. Int J Cancer 50:760-766, 1992
220. Anzai H, Frost P, Abbruzzese JL: Synergistic cytotoxicity with 2'-deoxy-5-azacytidine and topotecan in vitro and in vivo. Cancer Res 52:2180-2185, 1992
221. Chatterjee S, Cheno MF, Beroer NA: Hypersensitivity to clinically useful alkylating agents and radiation in poly(ADP-ribose) polymerase-deficient cell lines. Cancer Commun 2:401-407, 1990
222. Chatterjee S, Cheng MF, Trivedi D, et al: Camptothecin hypersensitivity mediated by interference with poly(adenosine diphosphate-ribose) polymerase. Proc Am Assoc Cancer Res 31:440, 1990
223. Satoh M, Lindahl T: Role of poly(ADP-ribose) formation in DNA repair. Nature 356:356-358, 1992
224. Utsugi T, Demuth S, Hanna N: Synergistic antitumor effects of topoisomerase inhibitors and natural cell-mediated cytotoxicity. Cancer Res 49:1429-1433, 1989
225. Musk SR, Steel G: The inhibition of cellular recovery in human tumour cells by inhibitors of topoisomerase. Br J Cancer 62:364-367, 1990
226. Mattern MR, Hofmann GA, McCabe FL, et al: Synergistic cell killing by ionizing radiation and topoisomerase I inhibitor topotecan (SK&F 104864). Cancer Res 51:5813-5816, 1991
227. Chang AY, Gu Z, Keno R, et al: Radiation (XRT)-sensitizing effects of topoisomerase (topo) I and II inhibitors. Proc Am Assoc Cancer Res 32:389, 1991
228. Chang AY, Gu CZ, Keno P, et al: Topotecan (T) and etoposide (E) inhibit radiation (XRT) repair differently than potential lethal damage (PLD) repair or sublethal damage repair. Proc Am Assoc Cancer Res 33:437, 1992
229. Owens JK, Schea R, Wang M, et al: Camptothecin sensitizes radioresistant human melanoma cells to X-irradiation. Proc Am Assoc Cancer Res 33:437, 1992
230. Kim JH, Kim SH, Kolozsvary A, et al: Potentiation of radiation response in human carcinoma cells in vitro and murine fibrosarcoma in vivo by topotecan, an inhibitor of DNA topoisomerase I. Int J Radiat Oncol Biol Phys 22:515-518, 1992
231. Kastan M, Onyekwere O, Sidransky D, et al: Participation of p53 protein in the cellular response to DNA damage. Cancer Res 51:6304-6311, 1991
232. Hollstein M, Sidransky D, Vogelstein B, et al: p53 Mutations in human cancers. Science 253:49-53, 1991
233. Kroll DJ, Boroert CJ, Wiedmann TW, et al: Drug sensitivity of heat-resistant mouse B16 melanoma variants. Radiat Res 124:15-21, 1990
234. Herman TS, Khandakar V, Korbut T, et al: Cytotoxicity, tumor cell survival and tumor growth delay with camptothecin or topotecan under hyperthermic conditions alone or with cisplatin. Proc Am Assoc Cancer Res 33:499, 1992
235. Kessel D: Some determinants of camptothecin responsiveness in leukemia LI210 cells. Cancer Res 31:1883-1887, 1971
236. Johnson RK, Chitnis MP, Embrey WM, et al: In vivo characteristics of resistance and cross-resistance of an adriamycin-resistant subline of P388 leukemia. Cancer Treat Rep 62:1535-1547, 1978
237. Naito M, Hamada H, Tsuruo T: ATP/Mg2+-dependent binding of vincristine to the plasma membrane of multidrug-resistant k562 cells. J Biol Chem 263:11887-11891, 1988
238. Chen AY, Yu C, Potmesil M, et al' Camptothecin overcomes MDR1-mediated resistance in human KB carcinoma cells. Cancer Res 51:6039-6044, 1991
239. Hendricks CB, Rowtnsky EK, Grochow LB, et al: Effects of P-glycoprotein expression on accumulation and cytotoxicity of topotecan (SK&F 104864), a new camptothecin analog. Cancer Res 52:2268-2278, 1992
240. Lai SL, Goldstein L, Gottesman M, et al: MDR1 gene expression in lung cancer. J Natl Cancer Inst 81:1144-1150, 1989
241. Goldstein L, Galski H, Fojo A, et al: Expression of a multidrug resistance gene in human cancers. J Natl Cancer Inst 81:116-124, 1989
242. Cordon-Cardo C, O’Brien JP: The multidrug resistance phenotype in human cancer. In Important Advances in Oncology 1991 (DeVita VT Jr, Heilman S, Rosenberg SA, eds). Philadelphia: Lippincott, 1991, pp 19-38
243. Fojo A, Ueda K, Slamon D, et al: Expression of a multidrug resistance gene in human tumors and tissues. Proc Natl Acad Sci USA 84:265-269, 1987
244. Niimi S, Nakaûawa K, Suoimoto Y, et al: Mechanism of crossresistance to a camptothecin analogue (CPT-11) in a human ovarian cancer cell line selected by cisplatin. Cancer Res 52:328-333, 1992
245. Kanzawa F, Suoimoto Y, Minato K, et al: Establishment of a camptothecin analogue (CPT-1 l)-resistant cell line of human nonsmall cell lung cancer: Characterization and mechanism of resistance. Cancer Res 50:5919-5924, 1990
246. Chang J-Y, Dethlefsen LA, Barley LR, et al: Characterization of camptothecin-resistant Chinese hamster lung cells. Biochem Pharmacol 43:2443-2452, 1992
247. Suoimoto Y, Tsukahara S, Oh-Hara T, et al: Decreased expression of DNA topoisomerase I in camptothecin-resistant tumor cell lines as determined by a monoclonal antibody. Cancer Res 50:6925-6930, 1990
248. Gupta RS, Gupta R, Eng B, et al: Camptothecin-resistant mutants of Chinese hamster ovary cells containing a resistant form of topoisomerase I. Cancer Res 48:6404-6410, 1988
249. Eng WK, McCabe FL, Tan KB, et al: Development of a stable camptothecin-resistant subline of p388 leukemia with reduced topoisomerase I content. Mol Pharmacol 38:471-480, 1990
250. Tanizawa A, Pommier Y: Topoisomerase I alteration in a camptothecin-resistant cell line derived from Chinese hamster DC3F cells in culture. Cancer Res 52:1848-1854, 1992
251. Andoh T, Ishii K, Suzuki Y, et al: Characterization of a mammalian mutant with a camptothecin-resistant DNA topoisomerase 1. Proc Natl Acad Sci U S A 84:5565-5569, 1987
252. Kjeldsen E, Bonven BJ, Andoh T, et al: Characterization of a camptothecin-resistant human DNA topoisomerase I. J Biol Chem 263:3912-3916, 1988
253. Tamura H, Kohchi C, Yamada R, et al: Molecular cloning of a cDNA of a camptothecin-resistant human DNA topoisomerase I and identification of mutation sites. Nucleic Acids Res 19:69-75, 1991
254. Tan KB, Mattern MR, Eng WK, et al: Nonproductive rearrangement of DNA topoisomerase I and II genes: Correlation with resistance to topoisomerase inhibitors. J Natl Cancer Inst 81:1732-1735, 1989
255. Vaughan W, Karp J, Burke P: Long chemotherapy-free remissions after single-cycle timed-sequential chemotherapy for acute myelocytic leukemia. Cancer 45:859-865, 1980
256. Trask D, Muller M: Stabilization of type I topoisomerase-DNA covalent complexes by actinomycin D. Proc Natl Acad Sci USA 85:1417-1421, 1988
257. Yamashita Y, Kawada S, Fujii N, et al: Induction of mammalian DNA topoisomerase I and II mediated DNA cleavage by saintopin, a new antitumor agent from fungus. Biochemistry 30:5838-5845, 1991
258. Rtou JF, Helissey P, Grondard L, et al: Inhibition of eukaryotic DNA topoisomerase 1 and II activities by indoloquinolinedione derivatives. Mol Pharmacol 40:699-706, 1991
259. Poddevin B, Rtou JF, Lavelle F, et al: Dual topoisomerase 1 and 11 inhibition by RP 60475, an intercalating agent in early clinical trial, Proc Am Assoc Cancer Res 33:437, 1992
260. Taguchi T, Wakui A, Hasegawa K, et al: Phase I clinical study of CPT-11. Jpn J Cancer Chemother 17:115-120, 1990