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Structures of three classes of anticancer agents bound to the human topoisomerase I-DNA covalent complex.

Staker BL, Feese MD, Cushman M, Pommier Y, Zembower D, Stewart L, Burgin AB
J Med Chem 48 2336-45 (2005)
Related entries: 1sc7, 1seu

Cited: 238 times
EuropePMC logo PMID: 15801827

Abstract

Human topoisomerase I (top1) is the molecular target of a diverse set of anticancer compounds, including the camptothecins, indolocarbazoles, and indenoisoquinolines. These compounds bind to a transient top1-DNA covalent complex and inhibit the resealing of a single-strand nick that the enzyme creates to relieve superhelical tension in duplex DNA. (Hertzberg, R. P.; et al. Biochem. 1989, 28, 4629-4638. Hsiang, Y. H.; et al. J. Biol. Chem 1985, 260, 14873-14878. Champoux, J. J. Annu. Rev. Biochem. 2001, 70, 369-413. Stewart, L.; et al. Science 1998, 729, 1534-1541.) We report the X-ray crystal structures of the human top1-DNA complex bound with camptothecin and representative members of the indenoisoquinoline and indolocarbazole classes of top1 poisons. The planar nature of all three structurally diverse classes allows them to intercalate between DNA base pairs at the site of single-strand cleavage. All three classes of compounds have a free electron pair near Arg364, a residue that if mutated confers resistance to all three classes of drugs. The common intercalative binding mode is augmented by unexpected chemotype-specific contacts with amino acid residues Asn352 and Glu356, which adopt alternative side-chain conformations to accommodate the bound compounds. These new X-ray structures explain how very different molecules can stabilize top1-DNA covalent complexes and will aid the rational design of completely novel structural classes of anticancer drugs.

Reviews - 1t8i mentioned but not cited (8)

  1. DNA topoisomerases and their poisoning by anticancer and antibacterial drugs. Pommier Y, Leo E, Zhang H, Marchand C. Chem Biol 17 421-433 (2010)
  2. Drugging topoisomerases: lessons and challenges. Pommier Y. ACS Chem Biol 8 82-95 (2013)
  3. Interfacial inhibitors: targeting macromolecular complexes. Pommier Y, Marchand C. Nat Rev Drug Discov 11 25-36 (2011)
  4. DNA topoisomerases: Advances in understanding of cellular roles and multi-protein complexes via structure-function analysis. McKie SJ, Neuman KC, Maxwell A. Bioessays 43 e2000286 (2021)
  5. Interfacial inhibitors. Pommier Y, Kiselev E, Marchand C. Bioorg Med Chem Lett 25 3961-3965 (2015)
  6. DNA folds threaten genetic stability and can be leveraged for chemotherapy. Zell J, Rota Sperti F, Britton S, Monchaud D. RSC Chem Biol 2 47-76 (2021)
  7. Indole-Based Tubulin Inhibitors: Binding Modes and SARs Investigations. Tang S, Zhou Z, Jiang Z, Zhu W, Qiao D. Molecules 27 1587 (2022)
  8. Recent advances in the area of plant-based anti-cancer drug discovery using computational approaches. Das AP, Agarwal SM. Mol Divers (2023)

Articles - 1t8i mentioned but not cited (61)

  1. Ligand-based Pharmacophore Modeling, Virtual Screening and Molecular Docking Studies for Discovery of Potential Topoisomerase I Inhibitors. Pal S, Kumar V, Kundu B, Bhattacharya D, Preethy N, Reddy MP, Talukdar A. Comput Struct Biotechnol J 17 291-310 (2019)
  2. Design, synthesis, and biological evaluation of 14-substituted aromathecins as topoisomerase I inhibitors. Cinelli MA, Morrell A, Dexheimer TS, Scher ES, Pommier Y, Cushman M. J Med Chem 51 4609-4619 (2008)
  3. Antiproliferative activities of Amaryllidaceae alkaloids from Lycoris radiata targeting DNA topoisomerase I. Chen GL, Tian YQ, Wu JL, Li N, Guo MQ. Sci Rep 6 38284 (2016)
  4. Exploring DNA topoisomerase I ligand space in search of novel anticancer agents. Drwal MN, Agama K, Wakelin LP, Pommier Y, Griffith R. PLoS One 6 e25150 (2011)
  5. Alcohol-, diol-, and carbohydrate-substituted indenoisoquinolines as topoisomerase I inhibitors: investigating the relationships involving stereochemistry, hydrogen bonding, and biological activity. Peterson KE, Cinelli MA, Morrell AE, Mehta A, Dexheimer TS, Agama K, Antony S, Pommier Y, Cushman M. J Med Chem 54 4937-4953 (2011)
  6. New Discorhabdin Alkaloids from the Antarctic Deep-Sea Sponge Latrunculia biformis. Li F, Peifer C, Janussen D, Tasdemir D. Mar Drugs 17 E439 (2019)
  7. Targeted Isolation of Tsitsikammamines from the Antarctic Deep-Sea Sponge Latrunculia biformis by Molecular Networking and Anticancer Activity. Li F, Janussen D, Peifer C, Pérez-Victoria I, Tasdemir D. Mar Drugs 16 (2018)
  8. Effect of Pterostilbene, a Natural Derivative of Resveratrol, in the Treatment of Colorectal Cancer through Top1/Tdp1-Mediated DNA Repair Pathway. Zhang Y, Li Y, Sun C, Chen X, Han L, Wang T, Liu J, Chen X, Zhao D. Cancers (Basel) 13 4002 (2021)
  9. Identification of Leishmania donovani Topoisomerase 1 inhibitors via intuitive scaffold hopping and bioisosteric modification of known Top 1 inhibitors. Mamidala R, Majumdar P, Jha KK, Bathula C, Agarwal R, Chary MT, Majumder HK, Munshi P, Sen S. Sci Rep 6 26603 (2016)
  10. Molecular docking and dynamics simulation study of bioactive compounds from Ficus carica L. with important anticancer drug targets. Gurung AB, Ali MA, Lee J, Farah MA, Al-Anazi KM. PLoS One 16 e0254035 (2021)
  11. The structure-activity relationships of A-ring-substituted aromathecin topoisomerase I inhibitors strongly support a camptothecin-like binding mode. Cinelli MA, Morrell AE, Dexheimer TS, Agama K, Agrawal S, Pommier Y, Cushman M. Bioorg Med Chem 18 5535-5552 (2010)
  12. Design, Synthesis, Antimicrobial, and Anticancer Activities of Acridine Thiosemicarbazides Derivatives. Chen R, Huo L, Jaiswal Y, Huang J, Zhong Z, Zhong J, Williams L, Xia X, Liang Y, Yan Z. Molecules 24 E2065 (2019)
  13. Design, synthesis, cytotoxic activity and molecular docking studies of new 20(S)-sulfonylamidine camptothecin derivatives. Song ZL, Wang MJ, Li L, Wu D, Wang YH, Yan LT, Morris-Natschke SL, Liu YQ, Zhao YL, Wang CY, Liu H, Goto M, Liu H, Zhu GX, Lee KH. Eur J Med Chem 115 109-120 (2016)
  14. Hybrid topoisomerase I and HDAC inhibitors as dual action anticancer agents. Cincinelli R, Musso L, Artali R, Guglielmi MB, La Porta I, Melito C, Colelli F, Cardile F, Signorino G, Fucci A, Frusciante M, Pisano C, Dallavalle S. PLoS One 13 e0205018 (2018)
  15. Inhibitory effect of DNA topoisomerase inhibitor isoliquiritigenin on the growth of glioma cells. Zhao S, Chang H, Ma P, Gao G, Jin C, Zhao X, Zhou W, Jin B. Int J Clin Exp Pathol 8 12577-12582 (2015)
  16. Antileishmanial activity of terpenylquinones on Leishmania infantum and their effects on Leishmania topoisomerase IB. Pérez-Pertejo Y, Escudero-Martínez JM, Reguera RM, Balaña-Fouce R, García PA, Jambrina PG, San Feliciano A, Castro MÁ. Int J Parasitol Drugs Drug Resist 11 70-79 (2019)
  17. Artemisinin Derivatives with Antimelanoma Activity Show Inhibitory Effect against Human DNA Topoisomerase 1. Botta L, Filippi S, Zippilli C, Cesarini S, Bizzarri BM, Cirigliano A, Rinaldi T, Paiardini A, Fiorucci D, Saladino R, Negri R, Benedetti P. ACS Med Chem Lett 11 1035-1040 (2020)
  18. Mutational study of the "catalytic tetrad" of DNA topoisomerase IB from the hemoflagellate Leishmania donovani: Role of Asp-353 and Asn-221 in camptothecin resistance. Diaz-González R, Pérez-Pertejo Y, Pommier Y, Balaña-Fouce R, Reguera RM. Biochem Pharmacol 76 608-619 (2008)
  19. New 1,2,3-triazole linked ciprofloxacin-chalcones induce DNA damage by inhibiting human topoisomerase I& II and tubulin polymerization. Mohammed HHH, Abd El-Hafeez AA, Ebeid K, Mekkawy AI, Abourehab MAS, Wafa EI, Alhaj-Suliman SO, Salem AK, Ghosh P, Abuo-Rahma GEA, Hayallah AM, Abbas SH. J Enzyme Inhib Med Chem 37 1346-1363 (2022)
  20. Chromenopyrimidinone Controls Stemness and Malignancy by suppressing CD133 Expression in Hepatocellular Carcinoma. Song Y, Kim S, Lee H, No JH, Ryu HC, Kim J, Lim JW, Kim M, Choi I, Seo HR. Cancers (Basel) 12 E1193 (2020)
  21. Phenolic metabolites, biological activities, and isolated compounds of Terminalia muelleri extract. El-Kashak WA, Osman SM, Gaara AH, El-Toumy SA, Mohamed TK, Brouard I. Pharm Biol 55 2277-2284 (2017)
  22. Adaptive laboratory evolution in S. cerevisiae highlights role of transcription factors in fungal xenobiotic resistance. Ottilie S, Luth MR, Hellemann E, Goldgof GM, Vigil E, Kumar P, Cheung AL, Song M, Godinez-Macias KP, Carolino K, Yang J, Lopez G, Abraham M, Tarsio M, LeBlanc E, Whitesell L, Schenken J, Gunawan F, Patel R, Smith J, Love MS, Williams RM, McNamara CW, Gerwick WH, Ideker T, Suzuki Y, Wirth DF, Lukens AK, Kane PM, Cowen LE, Durrant JD, Winzeler EA. Commun Biol 5 128 (2022)
  23. Antitumor Activity and Mechanism of Robustic Acid from Dalbergia benthami Prain via Computational Target Fishing. Huang J, Liang Y, Tian W, Ma J, Huang L, Li B, Chen R, Li D. Molecules 25 E3919 (2020)
  24. Development of purely structure-based pharmacophores for the topoisomerase I-DNA-ligand binding pocket. Drwal MN, Agama K, Pommier Y, Griffith R. J Comput Aided Mol Des 27 1037-1049 (2013)
  25. Lignin Nanoparticles Deliver Novel Thymine Biomimetic Photo-Adducts with Antimelanoma Activity. Gabellone S, Piccinino D, Filippi S, Castrignanò T, Zippilli C, Del Buono D, Saladino R. Int J Mol Sci 23 915 (2022)
  26. Machine Learning Models Combined with Virtual Screening and Molecular Docking to Predict Human Topoisomerase I Inhibitors. Li B, Kang X, Zhao D, Zou Y, Huang X, Wang J, Zhang C. Molecules 24 E2107 (2019)
  27. Natural Product Evodiamine with Borate Trigger Unit: Discovery of Potent Antitumor Agents against Colon Cancer. Li X, Wu S, Dong G, Chen S, Ma Z, Liu D, Sheng C. ACS Med Chem Lett 11 439-444 (2020)
  28. Newly Synthesized Imino-Derivatives Analogues of Resveratrol Exert Inhibitory Effects in Breast Tumor Cells. Iacopetta D, Lappano R, Mariconda A, Ceramella J, Sinicropi MS, Saturnino C, Talia M, Cirillo F, Martinelli F, Puoci F, Rosano C, Longo P, Maggiolini M. Int J Mol Sci 21 E7797 (2020)
  29. Structure-Based Drug Design and Identification of H2O-Soluble and Low Toxic Hexacyclic Camptothecin Derivatives with Improved Efficacy in Cancer and Lethal Inflammation Models in Vivo. Pan P, Chen J, Li X, Li M, Yu H, Zhao JJ, Ni J, Wang X, Sun H, Tian S, Zhu F, Liu F, Huang Y, Hou T. J Med Chem 61 8613-8624 (2018)
  30. TOP1-DNA Trapping by Exatecan and Combination Therapy with ATR Inhibitor. Jo U, Murai Y, Agama KK, Sun Y, Saha LK, Yang X, Arakawa Y, Gayle S, Jones K, Paralkar V, Sundaram RK, Van Doorn J, Vasquez JC, Bindra RS, Choi WS, Pommier Y. Mol Cancer Ther 21 1090-1102 (2022)
  31. In Vitro and In Silico Characterization of an Antimalarial Compound with Antitumor Activity Targeting Human DNA Topoisomerase IB. Soren BC, Babu Dasari J, Ottaviani A, Messina B, Andreotti G, Romeo A, Iacovelli F, Falconi M, Desideri A, Fiorani P. Int J Mol Sci 22 7455 (2021)
  32. topIb, a phylogenetic hallmark gene of Thaumarchaeota encodes a functional eukaryote-like topoisomerase IB. Dahmane N, Gadelle D, Delmas S, Criscuolo A, Eberhard S, Desnoues N, Collin S, Zhang H, Pommier Y, Forterre P, Sezonov G. Nucleic Acids Res 44 2795-2805 (2016)
  33. A Novel Benzocoumarin-Stilbene Hybrid as a DNA ligase I inhibitor with in vitro and in vivo anti-tumor activity in breast cancer models. Hussain MK, Singh DK, Singh A, Asad M, Ansari MI, Shameem M, Krishna S, Valicherla GR, Makadia V, Meena S, Deshmukh AL, Gayen JR, Imran Siddiqi M, Datta D, Hajela K, Banerjee D. Sci Rep 7 10715 (2017)
  34. Dual Topoisomerase I/II Inhibition-Induced Apoptosis and Necro-Apoptosis in Cancer Cells by a Novel Ciprofloxacin Derivative via RIPK1/RIPK3/MLKL Activation. Alaaeldin R, Abdel-Rahman IM, Ali FEM, Bekhit AA, Elhamadany EY, Zhao QL, Cui ZG, Fathy M. Molecules 27 7993 (2022)
  35. Exploring Multifunctional Bioactive Components from Podophyllum sinense Using Multi-Target Ultrafiltration. Feng H, Chen G, Zhang Y, Guo M. Front Pharmacol 12 749189 (2021)
  36. Hybrid Quinolinyl Phosphonates as Heterocyclic Carboxylate Isosteres: Synthesis and Biological Evaluation against Topoisomerase 1B (TOP1B). Selas A, Fuertes M, Melcón-Fernández E, Pérez-Pertejo Y, Reguera RM, Balaña-Fouce R, Knudsen BR, Palacios F, Alonso C. Pharmaceuticals (Basel) 14 784 (2021)
  37. Network pharmacology and RNA sequencing studies on triterpenoid saponins from Bupleurum chinense for the treatment of breast cancer. Li D, Liu D, Yue D, Gao P, Du C, Liu X, Zhang L. RSC Adv 9 41088-41098 (2019)
  38. Bioactive fluorenes. Part III: 2,7-dichloro-9H-fluorene-based thiazolidinone and azetidinone analogues as anticancer and antimicrobial against multidrug resistant strains agents. Hussein EM, Alsantali RI, Morad M, Obaid RJ, Altass HM, Sayqal A, Abourehab MAS, Elkhawaga AA, Aboraia ASM, Ahmed SA. BMC Chem 14 42 (2020)
  39. Molecular docking elucidates the plausible mechanisms underlying the anticancer properties of acetyldigitoxigenin from Adenium obesum. Gurung AB, Ali MA, Lee J, Al-Hemaid F, Farah MA, Al-Anazi KM. Saudi J Biol Sci 27 1907-1911 (2020)
  40. Novel Sophoridine Derivatives Bearing Phosphoramide Mustard Moiety Exhibit Potent Antitumor Activities In Vitro and In Vivo. Li D, Dai L, Zhao X, Zhi S, Shen H, Yang Z. Molecules 23 E1960 (2018)
  41. Novel α, β-Unsaturated Sophoridinic Derivatives: Design, Synthesis, Molecular Docking and Anti-Cancer Activities. Xu Y, Wu L, Dai H, Gao M, Ur Rashid H, Wang H, Xie P, Liu X, Jiang J, Wang L. Molecules 22 E1967 (2017)
  42. Synthesis and Evaluation of Anticancer Activity of New 4-Acyloxy Derivatives of Robustic Acid. Chen R, Huo L, Jaiswal Y, Wei J, Li D, Zhong J, Williams L, Xia X, Liang Y. Int J Mol Sci 20 E5336 (2019)
  43. The dipeptidyl peptidase IV inhibitors vildagliptin and K-579 inhibit a phospholipase C: a case of promiscuous scaffolds in proteins. Chakraborty S, Rendón-Ramírez A, Ásgeirsson B, Dutta M, Ghosh AS, Oda M, Venkatramani R, Rao BJ, Dandekar AM, Goñi FM. F1000Res 2 286 (2013)
  44. Characterization of Caerulomycin A as a dual-targeting anticancer agent. Tong L, Sun W, Wu S, Han Y. Eur J Pharmacol 922 174914 (2022)
  45. Characterization of Promising Cytotoxic Metabolites from Tabebuia guayacan Hemsl.: Computational Prediction and In Vitro Testing. El-Hawary SS, Mohammed R, Taher MA, AbouZid SF, Mansour MA, Almahmoud SA, Huwaimel B, Amin E. Plants (Basel) 11 888 (2022)
  46. Design and Synthesis of Acridine-Triazole and Acridine-Thiadiazole Derivatives and Their Inhibitory Effect against Cancer Cells. Huo L, Liu X, Jaiswal Y, Xu H, Chen R, Lu R, Nong Y, Williams L, Liang Y, Jia Z. Int J Mol Sci 24 64 (2022)
  47. Evodiamine and Rutaecarpine as Potential Anticancer Compounds: A Combined Computational Study. Liu J, Guo H, Zhou J, Wang Y, Yan H, Jin R, Tang Y. Int J Mol Sci 23 11513 (2022)
  48. Insight on the Interaction between the Camptothecin Derivative and DNA Oligomer Mimicking the Target of Topo I Inhibitors. Bocian W, Naumczuk B, Urbanowicz M, Sitkowski J, Bednarek E, Wiktorska K, Pogorzelska A, Wielgus E, Kozerski L. Molecules 27 6946 (2022)
  49. Molecular Docking and Dynamics Simulation Revealed the Potential Inhibitory Activity of New Drugs against Human Topoisomerase I Receptor. Madeddu F, Di Martino J, Pieroni M, Del Buono D, Bottoni P, Botta L, Castrignanò T, Saladino R. Int J Mol Sci 23 14652 (2022)
  50. Novel bivalent securinine mimetics as topoisomerase I inhibitors. Hou W, Lin H, Wang ZY, Banwell MG, Zeng T, Sun PH, Lin J, Chen WM. Medchemcomm 8 320-328 (2017)
  51. Potential Multifunctional Bioactive Compounds from Dysosma versipellis Explored by Bioaffinity Ultrafiltration-HPLC/MS with Topo I, Topo II, COX-2 and ACE2. Feng H, Chen G, Zhang Y, Guo M. J Inflamm Res 15 4677-4692 (2022)
  52. Synthesis, anticancer evaluation and molecular docking studies of new benzimidazole- 1,3,4-oxadiazole derivatives as human topoisomerase types I poison. Acar Çevik U, Sağlık BN, Osmaniye D, Levent S, Kaya Çavuşoğlu B, Karaduman AB, Atlıd Ö, Atlı Eklioğlu Ö, Kaplancıklı ZA. J Enzyme Inhib Med Chem 35 1657-1673 (2020)
  53. Combination of bioaffinity ultrafiltration-UFLC-ESI-Q/TOF-MS/MS, in silico docking and multiple complex networks to explore antitumor mechanism of topoisomerase I inhibitors from Artemisiae Scopariae Herba. Chen T, Hu J, Wang H, Tan N, Qi J, Wang X, Wang L. BMC Complement Med Ther 23 317 (2023)
  54. Design and synthesis of new spirooxindole candidates and their selenium nanoparticles as potential dual Topo I/II inhibitors, DNA intercalators, and apoptotic inducers. El-Kalyoubi S, Khalifa MM, Abo-Elfadl MT, El-Sayed AA, Elkamhawy A, Lee K, Al-Karmalawy AA. J Enzyme Inhib Med Chem 38 2242714 (2023)
  55. Dimethylmyricacene: An In Vitro and In Silico Study of a Semisynthetic Non-Camptothecin Derivative Compound, Targeting Human DNA Topoisomerase 1B. Ottaviani A, Iacovelli F, Welsch J, Morozzo Della Rocca B, Desideri A, Falconi M, Calcul L, Baker BJ, Fiorani P. Cells 11 3486 (2022)
  56. MD-Ligand-Receptor: A High-Performance Computing Tool for Characterizing Ligand-Receptor Binding Interactions in Molecular Dynamics Trajectories. Pieroni M, Madeddu F, Di Martino J, Arcieri M, Parisi V, Bottoni P, Castrignanò T. Int J Mol Sci 24 11671 (2023)
  57. Molecular Dynamics Investigations of Human DNA-Topoisomerase I Interacting with Novel Dewar Valence Photo-Adducts: Insights into Inhibitory Activity. Di Martino J, Arcieri M, Madeddu F, Pieroni M, Carotenuto G, Bottoni P, Botta L, Castrignanò T, Gabellone S, Saladino R. Int J Mol Sci 25 234 (2023)
  58. New 5-Substituted SN38 Derivatives: A Stability Study and Interaction with Model Nicked DNA by NMR and Molecular Modeling Methods. Bednarek E, Bocian W, Sitkowski J, Urbanowicz M, Kozerski L. Int J Mol Sci 24 17445 (2023)
  59. Novel 3,9-Disubstituted Acridines with Strong Inhibition Activity against Topoisomerase I: Synthesis, Biological Evaluation and Molecular Docking Study. Krochtová K, Halečková A, Janovec L, Blizniaková M, Kušnírová K, Kožurková M. Molecules 28 1308 (2023)
  60. Synthesis of novel amidines via one-pot three component reactions: Selective topoisomerase I inhibitors with antiproliferative properties. El-Sheref EM, Tawfeek HN, Hassan AA, Bräse S, Elbastawesy MAI, Gomaa HAM, Mostafa YA, Youssif BGM. Front Chem 10 1039176 (2022)
  61. The binding proximity of methyl β-lilacinobioside isolated from Caralluma retrospiciens with topoisomerase II attributes apoptosis in breast cancer cell line. Alallah MI, Alhemaid F, Bai F, Mothana RA, Elshikh MS, Abul Farah M, Ali MA, Lee J, Al-Anazi KM. Saudi J Biol Sci 25 1826-1833 (2018)


Reviews citing this publication (20)

  1. Topoisomerase I inhibitors: camptothecins and beyond. Pommier Y. Nat Rev Cancer 6 789-802 (2006)
  2. DNA topoisomerase I inhibitors: chemistry, biology, and interfacial inhibition. Pommier Y. Chem Rev 109 2894-2902 (2009)
  3. New mechanistic and functional insights into DNA topoisomerases. Chen SH, Chan NL, Hsieh TS. Annu Rev Biochem 82 139-170 (2013)
  4. Repair of topoisomerase I-mediated DNA damage. Pommier Y, Barcelo JM, Rao VA, Sordet O, Jobson AG, Thibaut L, Miao ZH, Seiler JA, Zhang H, Marchand C, Agama K, Nitiss JL, Redon C. Prog Nucleic Acid Res Mol Biol 81 179-229 (2006)
  5. Topoisomerases as anticancer targets. Delgado JL, Hsieh CM, Chan NL, Hiasa H. Biochem J 475 373-398 (2018)
  6. Indolocarbazole natural products: occurrence, biosynthesis, and biological activity. Sánchez C, Méndez C, Salas JA. Nat Prod Rep 23 1007-1045 (2006)
  7. Cancer therapies utilizing the camptothecins: a review of the in vivo literature. Venditto VJ, Simanek EE. Mol Pharm 7 307-349 (2010)
  8. Structural studies of type I topoisomerases. Baker NM, Rajan R, Mondragón A. Nucleic Acids Res 37 693-701 (2009)
  9. Targeting topoisomerase I: molecular mechanisms and cellular determinants of response to topoisomerase I inhibitors. Beretta GL, Perego P, Zunino F. Expert Opin Ther Targets 12 1243-1256 (2008)
  10. Novel camptothecin derivatives as topoisomerase I inhibitors. Basili S, Moro S. Expert Opin Ther Pat 19 555-574 (2009)
  11. Small molecule intercalation with double stranded DNA: implications for normal gene regulation and for predicting the biological efficacy and genotoxicity of drugs and other chemicals. Hendry LB, Mahesh VB, Bransome ED, Ewing DE. Mutat Res 623 53-71 (2007)
  12. Targeting atypical trypanosomatid DNA topoisomerase I. Balaña-Fouce R, Redondo CM, Pérez-Pertejo Y, Díaz-González R, Reguera RM. Drug Discov Today 11 733-740 (2006)
  13. The effects of camptothecin on RNA polymerase II transcription: roles of DNA topoisomerase I. Capranico G, Ferri F, Fogli MV, Russo A, Lotito L, Baranello L. Biochimie 89 482-489 (2007)
  14. Biomarkers for enhancing the radiosensitivity of nasopharyngeal carcinoma. Chen W, Hu GH. Cancer Biol Med 12 23-32 (2015)
  15. Topoisomerase inhibitors as anticancer agents: a patent update. Khadka DB, Cho WJ. Expert Opin Ther Pat 23 1033-1056 (2013)
  16. Relevance of extracellular and intracellular interactions of camptothecins as determinants of antitumor activity. Beretta GL, Zunino F. Biochem Pharmacol 74 1437-1444 (2007)
  17. Recent Advances in Improved Anticancer Efficacies of Camptothecin Nano-Formulations: A Systematic Review. Ghanbari-Movahed M, Kaceli T, Mondal A, Farzaei MH, Bishayee A. Biomedicines 9 480 (2021)
  18. Topoisomerase 1B poisons: Over a half-century of drug leads, clinical candidates, and serendipitous discoveries. Cinelli MA. Med Res Rev 39 1294-1337 (2019)
  19. Analyses of anticancer drugs by capillary electrophoresis: a review. Ali I, Haque A, Wani WA, Saleem K, Al Za'abi M. Biomed Chromatogr 27 1296-1311 (2013)
  20. Oligonucleotide-Recognizing Topoisomerase Inhibitors (OTIs): Precision Gene Editors for Neurodegenerative Diseases? Bax BD, Sutormin D, McDonald NQ, Burley GA, Shelkovnikova T. Int J Mol Sci 23 11541 (2022)

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  1. Optimal function of the DNA repair enzyme TDP1 requires its phosphorylation by ATM and/or DNA-PK. Das BB, Antony S, Gupta S, Dexheimer TS, Redon CE, Garfield S, Shiloh Y, Pommier Y. EMBO J 28 3667-3680 (2009)
  2. Rational design of human DNA ligase inhibitors that target cellular DNA replication and repair. Chen X, Zhong S, Zhu X, Dziegielewska B, Ellenberger T, Wilson GM, MacKerell AD, Tomkinson AE. Cancer Res 68 3169-3177 (2008)
  3. The indenoisoquinoline noncamptothecin topoisomerase I inhibitors: update and perspectives. Pommier Y, Cushman M. Mol Cancer Ther 8 1008-1014 (2009)
  4. DNA cleavage assay for the identification of topoisomerase I inhibitors. Dexheimer TS, Pommier Y. Nat Protoc 3 1736-1750 (2008)
  5. A novel norindenoisoquinoline structure reveals a common interfacial inhibitor paradigm for ternary trapping of the topoisomerase I-DNA covalent complex. Marchand C, Antony S, Kohn KW, Cushman M, Ioanoviciu A, Staker BL, Burgin AB, Stewart L, Pommier Y. Mol Cancer Ther 5 287-295 (2006)
  6. Synthesis and evaluation of indenoisoquinoline topoisomerase I inhibitors substituted with nitrogen heterocycles. Nagarajan M, Morrell A, Ioanoviciu A, Antony S, Kohlhagen G, Agama K, Hollingshead M, Pommier Y, Cushman M. J Med Chem 49 6283-6289 (2006)
  7. Crystallographic trapping in the rebeccamycin biosynthetic enzyme RebC. Ryan KS, Howard-Jones AR, Hamill MJ, Elliott SJ, Walsh CT, Drennan CL. Proc Natl Acad Sci U S A 104 15311-15316 (2007)
  8. Structural basis for specificity in the poxvirus topoisomerase. Perry K, Hwang Y, Bushman FD, Van Duyne GD. Mol Cell 23 343-354 (2006)
  9. Synergistic targeting of cell membrane, cytoplasm, and nucleus of cancer cells using rod-shaped nanoparticles. Barua S, Mitragotri S. ACS Nano 7 9558-9570 (2013)
  10. Early effects of topoisomerase I inhibition on RNA polymerase II along transcribed genes in human cells. Khobta A, Ferri F, Lotito L, Montecucco A, Rossi R, Capranico G. J Mol Biol 357 127-138 (2006)
  11. A systematic study of nitrated indenoisoquinolines reveals a potent topoisomerase I inhibitor. Morrell A, Antony S, Kohlhagen G, Pommier Y, Cushman M. J Med Chem 49 7740-7753 (2006)
  12. Cloning and characterization of an environmental DNA-derived gene cluster that encodes the biosynthesis of the antitumor substance BE-54017. Chang FY, Brady SF. J Am Chem Soc 133 9996-9999 (2011)
  13. Immunodetection of human topoisomerase I-DNA covalent complexes. Patel AG, Flatten KS, Peterson KL, Beito TG, Schneider PA, Perkins AL, Harki DA, Kaufmann SH. Nucleic Acids Res 44 2816-2826 (2016)
  14. Thr729 in human topoisomerase I modulates anti-cancer drug resistance by altering protein domain communications as suggested by molecular dynamics simulations. Chillemi G, D'Annessa I, Fiorani P, Losasso C, Benedetti P, Desideri A. Nucleic Acids Res 36 5645-5651 (2008)
  15. 7-azaindenoisoquinolines as topoisomerase I inhibitors and potential anticancer agents. Kiselev E, DeGuire S, Morrell A, Agama K, Dexheimer TS, Pommier Y, Cushman M. J Med Chem 54 6106-6116 (2011)
  16. Investigation of the lactam side chain length necessary for optimal indenoisoquinoline topoisomerase I inhibition and cytotoxicity in human cancer cell cultures. Morrell A, Placzek MS, Steffen JD, Antony S, Agama K, Pommier Y, Cushman M. J Med Chem 50 2040-2048 (2007)
  17. Using 3'-bridging phosphorothiolates to isolate the forward DNA cleavage reaction of human topoisomerase IIalpha. Deweese JE, Burgin AB, Osheroff N. Biochemistry 47 4129-4140 (2008)
  18. Synthesis of benz[d]indeno[1,2-b]pyran-5,11-diones: versatile intermediates for the design and synthesis of topoisomerase I inhibitors. Morrell A, Antony S, Kohlhagen G, Pommier Y, Cushman M. Bioorg Med Chem Lett 16 1846-1849 (2006)
  19. The anticancer multi-kinase inhibitor dovitinib also targets topoisomerase I and topoisomerase II. Hasinoff BB, Wu X, Nitiss JL, Kanagasabai R, Yalowich JC. Biochem Pharmacol 84 1617-1626 (2012)
  20. γH2AX assay as DNA damage biomarker for human population studies: defining experimental conditions. Sánchez-Flores M, Pásaro E, Bonassi S, Laffon B, Valdiglesias V. Toxicol Sci 144 406-413 (2015)
  21. Synthesis and biological evaluation of new carbohydrate-substituted indenoisoquinoline topoisomerase I inhibitors and improved syntheses of the experimental anticancer agents indotecan (LMP400) and indimitecan (LMP776). Beck DE, Agama K, Marchand C, Chergui A, Pommier Y, Cushman M. J Med Chem 57 1495-1512 (2014)
  22. Synthesis and Biological Evaluation of the First Triple Inhibitors of Human Topoisomerase 1, Tyrosyl-DNA Phosphodiesterase 1 (Tdp1), and Tyrosyl-DNA Phosphodiesterase 2 (Tdp2). Wang P, Elsayed MSA, Plescia CB, Ravji A, Redon CE, Kiselev E, Marchand C, Zeleznik O, Agama K, Pommier Y, Cushman M. J Med Chem 60 3275-3288 (2017)
  23. Molecular drug design, synthesis and structure elucidation of a new specific target peptide based metallo drug for cancer chemotherapy as topoisomerase I inhibitor. Tabassum S, Al-Asbahy WM, Afzal M, Afzal M, Arjmand F, Bagchi V. Dalton Trans 41 4955-4964 (2012)
  24. Targeted metagenomics: finding rare tryptophan dimer natural products in the environment. Chang FY, Ternei MA, Calle PY, Brady SF. J Am Chem Soc 137 6044-6052 (2015)
  25. Anthracyclines as effective anticancer drugs. Nadas J, Sun D. Expert Opin Drug Discov 1 549-568 (2006)
  26. Design, synthesis, and evaluation of dibenzo[c,h][1,6]naphthyridines as topoisomerase I inhibitors and potential anticancer agents. Kiselev E, Dexheimer TS, Pommier Y, Cushman M. J Med Chem 53 8716-8726 (2010)
  27. Molecular and cellular pharmacology of the novel noncamptothecin topoisomerase I inhibitor Genz-644282. Sooryakumar D, Dexheimer TS, Teicher BA, Pommier Y. Mol Cancer Ther 10 1490-1499 (2011)
  28. Cytotoxicity of the traditional chinese medicine (TCM) plumbagin in its copper chemistry. Chen ZF, Tan MX, Liu LM, Liu YC, Wang HS, Yang B, Peng Y, Liu HG, Liang H, Orvig C. Dalton Trans 10824-10833 (2009)
  29. Design and synthesis of C3-pyrazole/chalcone-linked beta-carboline hybrids: antitopoisomerase I, DNA-interactive, and apoptosis-inducing anticancer agents. Kamal A, Srinivasulu V, Nayak VL, Sathish M, Shankaraiah N, Bagul C, Reddy NV, Rangaraj N, Nagesh N. ChemMedChem 9 2084-2098 (2014)
  30. Identification, synthesis, and biological evaluation of metabolites of the experimental cancer treatment drugs indotecan (LMP400) and indimitecan (LMP776) and investigation of isomerically hydroxylated indenoisoquinoline analogues as topoisomerase I poisons. Cinelli MA, Reddy PV, Lv PC, Liang JH, Chen L, Agama K, Pommier Y, van Breemen RB, Cushman M. J Med Chem 55 10844-10862 (2012)
  31. Potential new inorganic antitumour agents from combining the anticancer traditional Chinese medicine (TCM) matrine with Ga(III), Au(III), Sn(IV) ions, and DNA binding studies. Chen ZF, Mao L, Liu LM, Liu YC, Peng Y, Hong X, Wang HH, Liu HG, Liang H. J Inorg Biochem 105 171-180 (2011)
  32. Crystal structure of a bacterial type IB DNA topoisomerase reveals a preassembled active site in the absence of DNA. Patel A, Shuman S, Mondragón A. J Biol Chem 281 6030-6037 (2006)
  33. Synthesis and biological evaluation of 14-(aminoalkyl-aminomethyl)aromathecins as topoisomerase I inhibitors: investigating the hypothesis of shared structure-activity relationships. Cinelli MA, Cordero B, Dexheimer TS, Pommier Y, Cushman M. Bioorg Med Chem 17 7145-7155 (2009)
  34. Investigating the correlations among the chemical structures, bioactivity profiles and molecular targets of small molecules. Cheng T, Wang Y, Bryant SH. Bioinformatics 26 2881-2888 (2010)
  35. Molecular design, synthesis and docking study of benz[b]oxepines and 12-oxobenzo[c]phenanthridinones as topoisomerase 1 inhibitors. Lee SH, Van HT, Yang SH, Lee KT, Kwon Y, Cho WJ. Bioorg Med Chem Lett 19 2444-2447 (2009)
  36. Total synthesis and biological evaluation of 22-hydroxyacuminatine. Xiao X, Antony S, Pommier Y, Cushman M. J Med Chem 49 1408-1412 (2006)
  37. Tryptophane-205 of human topoisomerase I is essential for camptothecin inhibition of negative but not positive supercoil removal. Frøhlich RF, Veigaard C, Andersen FF, McClendon AK, Gentry AC, Andersen AH, Osheroff N, Stevnsner T, Knudsen BR. Nucleic Acids Res 35 6170-6180 (2007)
  38. Identification of C10 biotinylated camptothecin (CPT-10-B) binding peptides using T7 phage display screen on a QCM device. Takakusagi Y, Takakusagi K, Kuramochi K, Kobayashi S, Sugawara F, Sakaguchi K. Bioorg Med Chem 15 7590-7598 (2007)
  39. Simulations of DNA topoisomerase 1B bound to supercoiled DNA reveal changes in the flexibility pattern of the enzyme and a secondary protein-DNA binding site. D'Annessa I, Coletta A, Sutthibutpong T, Mitchell J, Chillemi G, Harris S, Desideri A. Nucleic Acids Res 42 9304-9312 (2014)
  40. Synthesis and topoisomerase poisoning activity of A-ring and E-ring substituted luotonin A derivatives. Nacro K, Zha CC, Guzzo PR, Jason Herr R, Peace D, Friedrich TD. Bioorg Med Chem 15 4237-4246 (2007)
  41. Design, docking, and synthesis of novel indeno[1,2-c]isoquinolines for the development of antitumor agents as topoisomerase I inhibitors. Cho WJ, Le QM, My Van HT, Youl Lee K, Kang BY, Lee ES, Lee SK, Kwon Y. Bioorg Med Chem Lett 17 3531-3534 (2007)
  42. Discovery, Synthesis, and Evaluation of Oxynitidine Derivatives as Dual Inhibitors of DNA Topoisomerase IB (TOP1) and Tyrosyl-DNA Phosphodiesterase 1 (TDP1), and Potential Antitumor Agents. Zhang XR, Wang HW, Tang WL, Zhang Y, Yang H, Hu DX, Ravji A, Marchand C, Kiselev E, Ofori-Atta K, Agama K, Pommier Y, An LK. J Med Chem 61 9908-9930 (2018)
  43. Molecular mechanism of the camptothecin resistance of Glu710Gly topoisomerase IB mutant analyzed in vitro and in silico. Tesauro C, Morozzo della Rocca B, Ottaviani A, Coletta A, Zuccaro L, Arnò B, D'Annessa I, Fiorani P, Desideri A. Mol Cancer 12 100 (2013)
  44. Mutation of Gly721 alters DNA topoisomerase I active site architecture and sensitivity to camptothecin. van der Merwe M, Bjornsti MA. J Biol Chem 283 3305-3315 (2008)
  45. Optimization of the lactam side chain of 7-azaindenoisoquinoline topoisomerase I inhibitors and mechanism of action studies in cancer cells. Kiselev E, Sooryakumar D, Agama K, Cushman M, Pommier Y. J Med Chem 57 1289-1298 (2014)
  46. Azaindenoisoquinolines as topoisomerase I inhibitors and potential anticancer agents: a systematic study of structure-activity relationships. Kiselev E, Agama K, Pommier Y, Cushman M. J Med Chem 55 1682-1697 (2012)
  47. Convenient synthesis of indeno[1,2-c]isoquinolines as constrained forms of 3-arylisoquinolines and docking study of a topoisomerase I inhibitor into DNA-topoisomerase I complex. Van HT, Le QM, Lee KY, Lee ES, Kwon Y, Kim TS, Le TN, Lee SH, Cho WJ. Bioorg Med Chem Lett 17 5763-5767 (2007)
  48. Design and Synthesis of Chlorinated and Fluorinated 7-Azaindenoisoquinolines as Potent Cytotoxic Anticancer Agents That Inhibit Topoisomerase I. Elsayed MSA, Su Y, Wang P, Sethi T, Agama K, Ravji A, Redon CE, Kiselev E, Horzmann KA, Freeman JL, Pommier Y, Cushman M. J Med Chem 60 5364-5376 (2017)
  49. Differential modulation of BRCA1 and BARD1 nuclear localisation and foci assembly by DNA damage. Brodie KM, Henderson BR. Cell Signal 22 291-302 (2010)
  50. Discovery of potent indenoisoquinoline topoisomerase I poisons lacking the 3-nitro toxicophore. Beck DE, Abdelmalak M, Lv W, Reddy PV, Tender GS, O'Neill E, Agama K, Marchand C, Pommier Y, Cushman M. J Med Chem 58 3997-4015 (2015)
  51. Gold(III) macrocycles: nucleotide-specific unconventional catalytic inhibitors of human topoisomerase I. Akerman KJ, Fagenson AM, Cyril V, Taylor M, Muller MT, Akerman MP, Munro OQ. J Am Chem Soc 136 5670-5682 (2014)
  52. Quinoline alkaloids as intercalative topoisomerase inhibitors. Byler KG, Wang C, Setzer WN. J Mol Model 15 1417-1426 (2009)
  53. Activity of indenoisoquinolines against African trypanosomes. Bakshi RP, Sang D, Morrell A, Cushman M, Shapiro TA. Antimicrob Agents Chemother 53 123-128 (2009)
  54. Characterization and structure-activity relationships of indenoisoquinoline-derived topoisomerase I inhibitors in unsilencing the dormant Ube3a gene associated with Angelman syndrome. Lee HM, Clark EP, Kuijer MB, Cushman M, Pommier Y, Philpot BD. Mol Autism 9 45 (2018)
  55. Design, synthesis, and biological evaluation of O-2-modified indenoisoquinolines as dual topoisomerase I-tyrosyl-DNA phosphodiesterase I inhibitors. Lv PC, Agama K, Marchand C, Pommier Y, Cushman M. J Med Chem 57 4324-4336 (2014)
  56. Evaluation of indenoisoquinoline topoisomerase I inhibitors using a hollow fiber assay. Morrell A, Jayaraman M, Nagarajan M, Fox BM, Meckley MR, Ioanoviciu A, Pommier Y, Antony S, Hollingshead M, Cushman M. Bioorg Med Chem Lett 16 4395-4399 (2006)
  57. Rational design and synthesis of topoisomerase I and II inhibitors based on oleanolic acid moiety for new anti-cancer drugs. Ashour A, El-Sharkawy S, Amer M, Abdel Bar F, Katakura Y, Miyamoto T, Toyota N, Bang TH, Kondo R, Shimizu K. Bioorg Med Chem 22 211-220 (2014)
  58. Role of the protein in the DNA sequence specificity of the cleavage site stabilized by the camptothecin topoisomerase IB inhibitor: a metadynamics study. Coletta A, Desideri A. Nucleic Acids Res 41 9977-9986 (2013)
  59. The different cleavage DNA sequence specificity explains the camptothecin resistance of the human topoisomerase I Glu418Lys mutant. Fiorani P, Chillemi G, Losasso C, Castelli S, Desideri A. Nucleic Acids Res 34 5093-5100 (2006)
  60. Synthesis of β-carboline-benzimidazole conjugates using lanthanum nitrate as a catalyst and their biological evaluation. Kamal A, Rao MP, Swapna P, Srinivasulu V, Bagul C, Shaik AB, Mullagiri K, Kovvuri J, Reddy VS, Vidyasagar K, Nagesh N. Org Biomol Chem 12 2370-2387 (2014)
  61. The binding orientation of a norindenoisoquinoline in the topoisomerase I-DNA cleavage complex is primarily governed by pi-pi stacking interactions. Song Y, Cushman M. J Phys Chem B 112 9484-9489 (2008)
  62. WRN protects against topo I but not topo II inhibitors by preventing DNA break formation. Christmann M, Tomicic MT, Gestrich C, Roos WP, Bohr VA, Kaina B. DNA Repair (Amst) 7 1999-2009 (2008)
  63. Replacement of the human topoisomerase linker domain with the plasmodial counterpart renders the enzyme camptothecin resistant. Arnò B, D'Annessa I, Tesauro C, Zuccaro L, Ottaviani A, Knudsen B, Fiorani P, Desideri A. PLoS One 8 e68404 (2013)
  64. Structure-based design, synthesis, and biological studies of new anticancer norindenoisoquinoline topoisomerase I inhibitors. Song Y, Shao Z, Dexheimer TS, Scher ES, Pommier Y, Cushman M. J Med Chem 53 1979-1989 (2010)
  65. Synthesis, biological evaluation, and molecular modeling studies of rebeccamycin analogues modified in the carbohydrate moiety. Animati F, Berettoni M, Bigioni M, Binaschi M, Felicetti P, Gontrani L, Incani O, Madami A, Monteagudo E, Olivieri L, Resta S, Rossi C, Cipollone A. ChemMedChem 3 266-279 (2008)
  66. Allosteric inhibition of topoisomerase I by pinostrobin: Molecular docking, spectroscopic and topoisomerase I activity studies. Jadaun A, Subbarao N, Dixit A. J Photochem Photobiol B 167 299-308 (2017)
  67. Discovery of DNA Topoisomerase I Inhibitors with Low-Cytotoxicity Based on Virtual Screening from Natural Products. Xin LT, Liu L, Shao CL, Yu RL, Chen FL, Yue SJ, Wang M, Guo ZL, Fan YC, Guan HS, Wang CY. Mar Drugs 15 E217 (2017)
  68. Molecular docking approach on the Topoisomerase I inhibitors series included in the NCI anti-cancer agents mechanism database. Lauria A, Ippolito M, Almerico AM. J Mol Model 13 393-400 (2007)
  69. Synthesis and biological evaluation of new fluorinated and chlorinated indenoisoquinoline topoisomerase I poisons. Beck DE, Lv W, Abdelmalak M, Plescia CB, Agama K, Marchand C, Pommier Y, Cushman M. Bioorg Med Chem 24 1469-1479 (2016)
  70. Attenuation of cytogenetic effects by erythropoietin in human lymphocytes in vitro and P388 ascites tumor cells in vivo treated with irinotecan (CPT-11). Digkas E, Kareli D, Chrisafi S, Passadaki T, Mantadakis E, Hatzimichail A, Vargemezis V, Lialiaris T. Food Chem Toxicol 48 242-249 (2010)
  71. Binding of topotecan to a nicked DNA oligomer in solution. Bocian W, Kawecki R, Bednarek E, Sitkowski J, Williamson MP, Hansen PE, Kozerski L. Chemistry 14 2788-2794 (2008)
  72. Biochemical characterization and substrate specificity of the gene cluster for biosyntheses of K-252a and its analogs by in vitro heterologous expression system of Escherichia coli. Chiu HT, Lin YC, Lee MN, Chen YL, Wang MS, Lai CC. Mol Biosyst 5 1192-1203 (2009)
  73. Discovery of 4-alkoxy-2-aryl-6,7-dimethoxyquinolines as a new class of topoisomerase I inhibitors endowed with potent in vitro anticancer activity. Elbadawi MM, Eldehna WM, Wang W, Agama KK, Pommier Y, Abe M. Eur J Med Chem 215 113261 (2021)
  74. Genomic profiling in CEPH cell lines distinguishes between the camptothecins and indenoisoquinolines. Watson VG, Hardison NE, Harris T, Motsinger-Reif A, McLeod HL. Mol Cancer Ther 10 1839-1845 (2011)
  75. Novel imidazo[1,2-a]naphthyridinic systems (part 1): synthesis, antiproliferative and DNA-intercalating activities. Andaloussi M, Moreau E, Masurier N, Lacroix J, Gaudreault RC, Chezal JM, El Laghdach A, Canitrot D, Debiton E, Teulade JC, Chavignon O. Eur J Med Chem 43 2505-2517 (2008)
  76. Peptide Inhibition of Topoisomerase IB from Plasmodium falciparum. Roy A, D'Annessa I, Nielsen CJ, Tordrup D, Laursen RR, Knudsen BR, Desideri A, Andersen FF. Mol Biol Int 2011 854626 (2011)
  77. Potential new inorganic antitumour agents from combining the anticancer traditional Chinese medicine (TCM) liriodenine with metal ions, and DNA binding studies. Chen ZF, Liu YC, Liu LM, Wang HS, Qin SH, Wang BL, Bian HD, Yang B, Fun HK, Liu HG, Liang H, Orvig C. Dalton Trans 262-272 (2009)
  78. Synthesis and cytotoxic activity of a new series of topoisomerase I inhibitors. Dallavalle S, Gattinoni S, Mazzini S, Scaglioni L, Merlini L, Tinelli S, Beretta GL, Zunino F. Bioorg Med Chem Lett 18 1484-1489 (2008)
  79. 20-(S)-camptothecin analogues as DNA topoisomerase I inhibitors: a QSAR study. Hansch C, Verma RP. ChemMedChem 2 1807-1813 (2007)
  80. Design, Synthesis, and Biological Evaluation of Potential Prodrugs Related to the Experimental Anticancer Agent Indotecan (LMP400). Lv PC, Elsayed MS, Agama K, Marchand C, Pommier Y, Cushman M. J Med Chem 59 4890-4899 (2016)
  81. Divalent later transition metal complexes of the traditional chinese medicine (TCM) liriodenine: coordination chemistry, cytotoxicity and DNA binding studies. Liu YC, Chen ZF, Liu LM, Peng Y, Hong X, Yang B, Liu HG, Liang H, Orvig C. Dalton Trans 10813-10823 (2009)
  82. Induction of cell cycle arrest and apoptosis by copper complex Cu(SBCM)2 towards oestrogen-receptor positive MCF-7 breast cancer cells. Foo JB, Ng LS, Lim JH, Tan PX, Lor YZ, Loo JSE, Low ML, Chan LC, Beh CY, Leong SW, Saiful Yazan L, Tor YS, How CW. RSC Adv 9 18359-18370 (2019)
  83. Sequence selectivity of the cleavage sites induced by topoisomerase I inhibitors: a molecular dynamics study. Siu FM, Pommier Y. Nucleic Acids Res 41 10010-10019 (2013)
  84. Topoisomerase I (TOP1) dynamics: conformational transition from open to closed states. Takahashi DT, Gadelle D, Agama K, Kiselev E, Zhang H, Yab E, Petrella S, Forterre P, Pommier Y, Mayer C. Nat Commun 13 59 (2022)
  85. Binding of an Indenoisoquinoline to the topoisomerase-DNA complex induces reduction of linker mobility and strengthening of protein-DNA interaction. Mancini G, D'Annessa I, Coletta A, Chillemi G, Pommier Y, Cushman M, Desideri A. PLoS One 7 e51354 (2012)
  86. Cytogenetic evaluation of pre-pregnancy smoking in maternal and newborn lymphocytes. Kareli DE, Pouliliou SE, Nikas IH, Psillaki AN, Galazios GC, Liberis VA, Lialiaris TS. Eur J Obstet Gynecol Reprod Biol 165 205-209 (2012)
  87. Exploring DNA topoisomerase I inhibition by the benzo[c]phenanthridines fagaronine and ethoxidine using steered molecular dynamics. Clark RL, Deane FM, Anthony NG, Johnston BF, McCarthy FO, Mackay SP. Bioorg Med Chem 15 4741-4752 (2007)
  88. Synthesis and biological evaluation of novel homocamptothecins conjugating with dihydropyrimidine derivatives as potent topoisomerase I inhibitors. Zhu L, Cheng P, Lei N, Yao J, Sheng C, Zhuang C, Guo W, Liu W, Zhang Y, Dong G, Wang S, Miao Z, Zhang W. Arch Pharm (Weinheim) 344 726-734 (2011)
  89. TCH-1030 targeting on topoisomerase I induces S-phase arrest, DNA fragmentation, and cell death of breast cancer cells. Liu YP, Chen HL, Tzeng CC, Lu PJ, Lo CW, Lee YC, Tseng CH, Chen YL, Yang CN. Breast Cancer Res Treat 138 383-393 (2013)
  90. The human topoisomerase 1B Arg634Ala mutation results in camptothecin resistance and loss of inter-domain motion correlation. D'Annessa I, Tesauro C, Wang Z, Arnò B, Zuccaro L, Fiorani P, Desideri A. Biochim Biophys Acta 1834 2712-2721 (2013)
  91. Electron paramagnetic resonance (EPR) study of spin-labeled camptothecin derivatives: a different look of the ternary complex. Ricci A, Marinello J, Bortolus M, Sánchez A, Grandas A, Pedroso E, Pommier Y, Capranico G, Maniero AL, Zagotto G. J Med Chem 54 1003-1009 (2011)
  92. Pyrrolo[2,3-α]carbazole derivatives as topoisomerase I inhibitors that affect viability of glioma and endothelial cells in vitro and angiogenesis in vivo. Lampropoulou E, Manioudaki M, Fousteris M, Koutsourea A, Nikolaropoulos S, Papadimitriou E. Biomed Pharmacother 65 142-150 (2011)
  93. Synthesis and anticancer activity of new [(Indolyl)pyrazolyl]-1,3,4-oxadiazole thioglycosides and acyclic nucleoside analogs. El-Sayed WA, El-Sofany WI, Hussein HAR, Fathy NM. Nucleosides Nucleotides Nucleic Acids 36 474-495 (2017)
  94. Synthesis and biological evaluation of 7-alkenyl homocamptothecins as potent topoisomerase I inhibitors. Zhu L, Zhang X, Lei N, Liu W, Miao Z, Zhuang C, Sheng C, Guo W, Dong G, Yao J, Cheng P, Zhang W. Chem Biodivers 9 1084-1094 (2012)
  95. Synthesis and biological research of novel azaacridine derivatives as potent DNA-binding ligands and topoisomerase II inhibitors. Li D, Yuan Z, Chen S, Zhang C, Song L, Gao C, Chen Y, Tan C, Jiang Y. Bioorg Med Chem 25 3437-3446 (2017)
  96. Topoisomerase I-mediated DNA cleavage induced by the minor groove-directed binding of bibenzimidazoles to a distal site. Khan QA, Pilch DS. J Mol Biol 365 561-569 (2007)
  97. Design and synthesis of 4-amino-2-phenylquinazolines as novel topoisomerase I inhibitors with molecular modeling. Le TN, Yang SH, Khadka DB, Van HT, Cho SH, Kwon Y, Lee ES, Lee KT, Cho WJ. Bioorg Med Chem 19 4399-4404 (2011)
  98. Electrochemical investigation of the interaction between topotecan and DNA at disposable graphite electrodes. Congur G, Erdem A, Mese F. Bioelectrochemistry 102 21-28 (2015)
  99. Human topoisomerase I C-terminal domain fragment containing the active site tyrosine is a molten globule: implication for the formation of competent productive complex. Punchihewa C, Dai J, Carver M, Yang D. J Struct Biol 159 111-121 (2007)
  100. Investigation of the Structure-Activity Relationships of Aza-A-Ring Indenoisoquinoline Topoisomerase I Poisons. Beck DE, Reddy PV, Lv W, Abdelmalak M, Tender GS, Lopez S, Agama K, Marchand C, Pommier Y, Cushman M. J Med Chem 59 3840-3853 (2016)
  101. Novel antitumor L-arabinose derivative of indolocarbazole with high affinity to DNA. Kaluzhny DN, Tatarskiy VV, Dezhenkova LG, Plikhtyak IL, Miniker TD, Shchyolkina AK, Strel'tsov SA, Chilov GG, Novikov FN, Kubasova IY, Smirnova ZS, Mel'nik SY, Livshits MA, Borisova OF, Shtil AA. ChemMedChem 4 1641-1648 (2009)
  102. On the selective detection of duplex deoxyribonucleic acids by 2,1,3-benzothiadiazole fluorophores. Neto BA, Lapis AA, Mancilha FS, Batista EL, Netz PA, Rominger F, Basso LA, Santos DS, Dupont J. Mol Biosyst 6 967-975 (2010)
  103. Recovery of the poisoned topoisomerase II for DNA religation: coordinated motion of the cleavage core revealed with the microsecond atomistic simulation. Huang NL, Lin JH. Nucleic Acids Res 43 6772-6786 (2015)
  104. Synthesis and biological evaluation of 5-aminoethyl benzophenanthridone derivatives as DNA topoisomerase IB inhibitors. Tang WL, Zhang Y, Hu DX, Yang H, Yu Q, Chen JW, Agama K, Pommier Y, An LK. Eur J Med Chem 178 81-92 (2019)
  105. Synthesis and biological evaluation of 6-fluoro-3-phenyl-7-piperazinyl quinolone derivatives as potential topoisomerase I inhibitors. Ge R, Zhao Q, Xie Z, Lu L, Guo Q, Li Z, Zhao L. Eur J Med Chem 122 465-474 (2016)
  106. Design and synthesis of some β-carboline derivatives as multi-target anticancer agents. Abdelsalam MA, AboulWafa OM, Badawey EA, El-Shoukrofy MS, El-Miligy MM, Gouda N. Future Med Chem 10 2791-2814 (2018)
  107. Evaluation of two models for human topoisomerase I interaction with dsDNA and camptothecin derivatives. Laco GS. PLoS One 6 e24314 (2011)
  108. Mechanism and specificity of DNA strand exchange catalyzed by vaccinia DNA topoisomerase type I. Stahley MR, Stivers JT. Biochemistry 49 2786-2795 (2010)
  109. Minor groove dimeric bisbenzimidazoles inhibit in vitro DNA binding to eukaryotic DNA topoisomerase I. Susova OY, Ivanov AA, Morales Ruiz SS, Lesovaya EA, Gromyko AV, Streltsov SA, Zhuze AL. Biochemistry (Mosc) 75 695-701 (2010)
  110. Mutations in the proteolipid subunits of the vacuolar H+-ATPase provide resistance to indolotryptoline natural products. Chang FY, Kawashima SA, Brady SF. Biochemistry 53 7123-7131 (2014)
  111. The antitumor activity of CYB-L10, a human topoisomerase IB catalytic inhibitor. Yu Q, Chen Y, Yang H, Zhang HL, Agama K, Pommier Y, An LK. J Enzyme Inhib Med Chem 34 818-822 (2019)
  112. Topoisomerase IB poisons induce histone H2A phosphorylation as a response to DNA damage in Leishmania infantum. Gutiérrez-Corbo C, Álvarez-Velilla R, Reguera RM, García-Estrada C, Cushman M, Balaña-Fouce R, Pérez-Pertejo Y. Int J Parasitol Drugs Drug Resist 11 39-48 (2019)
  113. α-Glucosidase Inhibitory and Antimicrobial Benzoylphloroglucinols from Garcinia schomburgakiana Fruits: In Vitro and In Silico Studies. Nguyen HT, Nguyen TT, Duong TH, Tran NM, Nguyen CH, Nguyen TH, Sichaem J. Molecules 27 2574 (2022)
  114. Binding mode analysis of topoisomerase inhibitors, 6-arylamino-7-chloro-quinazoline-5,8-diones, within the cleavable complex of human topoisomerase I and DNA. Choi I, Kim C, Choi S. Arch Pharm Res 30 1526-1535 (2007)
  115. Design, synthesis and evaluation of 4-substituted anthra[2,1-c][1,2,5]thiadiazole-6,11-dione derivatives as novel non-camptothecin topoisomerase I inhibitors. Dong G, Fang Y, Liu Y, Liu N, Wu S, Zhang W, Sheng C. Bioorg Med Chem Lett 27 1929-1933 (2017)
  116. Dissecting and predicting different types of binding sites in nucleic acids based on structural information. Jiang Z, Xiao SR, Liu R. Brief Bioinform 23 bbab411 (2022)
  117. Diterpenoids from Roots of Salvia lachnocalyx; In-silico and In-vitro Toxicity against Human Cancer Cell Lines. Hadavand Mirzaei H, Firuzi O, Jassbi AR. Iran J Pharm Res 19 85-94 (2020)
  118. Phenotype Screening of an Azole-bisindole Chemical Library Identifies URB1483 as a New Antileishmanial Agent Devoid of Toxicity on Human Cells. Diotallevi A, Scalvini L, Buffi G, Pérez-Pertejo Y, De Santi M, Verboni M, Favi G, Magnani M, Lodola A, Lucarini S, Galluzzi L. ACS Omega 6 35699-35710 (2021)
  119. Solvent dependency of the UV-Vis spectrum of indenoisoquinolines: role of keto-oxygens as polarity interaction probes. Coletta A, Castelli S, Chillemi G, Sanna N, Cushman M, Pommier Y, Desideri A. PLoS One 8 e73881 (2013)
  120. Structure-activity relationship study of 16 a-thiocamptothecins: an integrated in vitro and in silico approach. Samorì C, Beretta GL, Varchi G, Guerrini A, Di Micco S, Basili S, Bifulco G, Riccio R, Moro S, Bombardelli E, Zunino F, Fontana G. ChemMedChem 5 2006-2015 (2010)
  121. The regio-selective synthesis of 10-hydroxy camptothecin norcantharidin conjugates and their biological activity evaluation in vitro. Zhao CK, Li C, Wang XH, Bao YJ, Yang FH, Huang M. R Soc Open Sci 5 172317 (2018)
  122. Three-Component Synthesis of 2-Amino-3-cyano-4H-chromenes, In Silico Analysis of Their Pharmacological Profile, and In Vitro Anticancer and Antifungal Testing. Feliciano A, Gómez-García O, Escalante CH, Rodríguez-Hernández MA, Vargas-Fuentes M, Andrade-Pavón D, Villa-Tanaca L, Álvarez-Toledano C, Ramírez-Apan MT, Vázquez MA, Tamariz J, Delgado F. Pharmaceuticals (Basel) 14 1110 (2021)
  123. Total and semisynthesis and in vitro studies of both enantiomers of 20-fluorocamptothecin. Tangirala RS, Dixon R, Yang D, Ambrus A, Antony S, Agama K, Pommier Y, Curran DP. Bioorg Med Chem Lett 15 4736-4740 (2005)
  124. A gold-catalyzed cycloisomerization/aerobic oxidation cascade strategy for 2-aryl indenones from 1,5-enynes. Guo J, Peng X, Wang X, Xie F, Zhang X, Liang G, Sun Z, Liu Y, Cheng M, Liu Y. Org Biomol Chem 16 9147-9151 (2018)
  125. Advantages of an optical nanosensor system for the mechanistic analysis of a novel topoisomerase I targeting drug: a case study. Andersen MB, Tesauro C, Gonzalez M, Kristoffersen EL, Alonso C, Rubiales G, Coletta A, Frøhlich R, Stougaard M, Ho YP, Palacios F, Knudsen BR. Nanoscale 9 1886-1895 (2017)
  126. Design, synthesis, anticancer screening, docking studies and in silico ADME prediction of some β-carboline derivatives. Abdelsalam MA, AboulWafa OM, M Badawey EA, El-Shoukrofy MS, El-Miligy MM, Gouda N, Elaasser MM. Future Med Chem 10 1159-1175 (2018)
  127. Inhibition of DNA-Topoisomerase I by Acylated Triterpene Saponins from Pittosporum angustifolium Lodd. Bäcker C, Drwal MN, Preissner R, Lindequist U. Nat Prod Bioprospect 6 141-147 (2016)
  128. Microscopic Modes and Free Energies for Topoisomerase I-DNA Covalent Complex Binding with Non-campothecin Inhibitors by Molecular Docking and Dynamics Simulations. Wei NN, Hamza A, Hao C, Xiu Z, Zhan CG. Theor Chem Acc 132 (2013)
  129. Molecular Mechanisms of Anticancer Activity of N-Glycosides of Indolocarbazoles LCS-1208 and LCS-1269. Zenkov RG, Vlasova OA, Maksimova VP, Fetisov TI, Karpechenko NY, Ektova LV, Eremina VA, Popova VG, Usalka OG, Lesovaya EA, Belitsky GA, Yakubovskaya MG, Kirsanov KI. Molecules 26 7329 (2021)
  130. Novel 20(S)-sulfonylamidine derivatives of camptothecin and the use thereof as a potent antitumor agent: a patent evaluation of WO2015048365 (A1). Beretta GL, Zaffaroni N, Varchi G. Expert Opin Ther Pat 26 637-642 (2016)
  131. Position-Selective Synthesis and Biological Evaluation of Four Isomeric A-Ring Amino Derivatives of the Alkaloid Luotonin A. Ibric A, Eckerstorfer S, Eder M, Louko I, Tunjic L, Heffeter P, Schueffl HH, Marian B, Haider N. Molecules 24 E716 (2019)
  132. Synthesis of a peptide-universal nucleotide antigen: towards next-generation antibodies to detect topoisomerase I-DNA covalent complexes. Perkins AL, Peterson KL, Beito TG, Flatten KS, Kaufmann SH, Harki DA. Org Biomol Chem 14 4103-4109 (2016)
  133. Synthesis, structure, and biological evaluation of a platinum-carbazole conjugate. Cheun Y, Koag MC, Naguib YW, Ouzon-Shubeita H, Cui Z, Pakotiprapha D, Lee S. Chem Biol Drug Des 91 116-125 (2018)
  134. Total synthesis of (S)-14-azacamptothecin. Liu F, Li C. Org Biomol Chem 12 637-642 (2014)
  135. Use of double-stranded DNA mini-circles to characterize the covalent topoisomerase-DNA complex. Millet A, Strauss F, Delagoutte E. Sci Rep 5 13154 (2015)
  136. In vitro anti-inflammatory, in silico molecular docking and molecular dynamics simulation of oleanane-type triterpenes from aerial parts of Mussaenda recurvata. Tri MD, Phat NT, Minh PN, Chi MT, Hao BX, Minh An TN, Alam M, Van Kieu N, Dang VS, Mai TTN, Duong TH. RSC Adv 13 5324-5336 (2023)
  137. A Novel Generalized 3D-QSAR Model of Camptothecin Analogs. Bacilieri M, Paoletta S, Basili S, Fanton M, Moro S. Mol Inform 30 927-938 (2011)
  138. An Efficient Synthesis of 1-(1,3-Dioxoisoindolin-2-yl)-3-aryl Urea Analogs as Anticancer and Antioxidant Agents: An Insight into Experimental and In Silico Studies. Afzal O, Ahsan MJ. Molecules 29 67 (2023)
  139. Anti-Colorectal Cancer Effects of a Novel Camptothecin Derivative PCC0208037 In Vitro and In Vivo. Li M, Wang L, Wei Y, Wang W, Liu Z, Zuo A, Liu W, Tian J, Wang H. Pharmaceuticals (Basel) 16 53 (2022)
  140. Bio-guided isolation of alpha-glucosidase inhibitory compounds from Vietnamese Garcinia schomburgkiana fruits: in vitro and in silico studies. Nguyen NH, Vu YT, Nguyen TD, Cao TT, Nguyen HT, Le TK, Sichaem J, Mai DT, Minh An TN, Duong TH. RSC Adv 13 35408-35421 (2023)
  141. Characteristics of the microbial community in rhizosphere of Camptotheca acuminata cultured with exotic invasive plant Eupatorium adenophorum. Zu Y, Gao C, Wang W, Yang F, Liu Y, Wang M, Zhao Y. Sci China C Life Sci 50 22-30 (2007)
  142. DNA polymerase ε harmonizes topological states and R-loops formation to maintain genome integrity in Arabidopsis. Li Q, Zhou J, Li S, Zhang W, Du Y, Li K, Wang Y, Sun Q. Nat Commun 14 7763 (2023)
  143. Design, Synthesis, and Antiproliferative Activity of Novel Neocryptolepine-Rhodanine Hybrids. El-Bahnsawye M, Hussein MKA, Elmongy EI, Awad HM, Tolan AAE, Moemen YS, El-Shaarawy A, El-Sayed IE. Molecules 27 7599 (2022)
  144. Diphenyl ditelluride anticancer activity and DNA topoisomerase I poisoning in human colon cancer HCT116 cells. Juchem ALM, Trindade C, da Silva JB, Machado MDS, Guecheva TN, Rocha JC, Saffi J, de Oliveira IM, Henriques JAP, Escargueil A. Oncotarget 14 637-649 (2023)
  145. Effect of maternal smoking during pregnancy on fetus: a cytogenetic perspective. Kareli D, Pouliliou S, Nikas I, Psillaki A, Karelis A, Nikolettos N, Galazios G, Liberis V, Lialiaris T. J Matern Fetal Neonatal Med 27 127-131 (2014)
  146. Evaluation of the Anticancer and Biological Activities of Istaroxime via Ex Vivo Analyses, Molecular Docking and Conceptual Density Functional Theory Computations. Gok E, Unal N, Gungor B, Karakus G, Kaya S, Canturk P, Katin KP. Molecules 28 7458 (2023)
  147. Genomic and transcriptomic analysis of camptothecin producing novel fungal endophyte: Alternaria burnsii NCIM 1409. Natarajan S, Pucker B, Srivastava S. Sci Rep 13 14614 (2023)
  148. Single protein encapsulated SN38 for tumor-targeting treatment. Yu C, Huang F, Wang K, Liu M, Chow WA, Ling X, Li F, Causey JL, Huang X, Cook-Wiens G, Cui X. J Transl Med 21 897 (2023)
  149. Supercritical CO2 assisted extraction of essential oil and naringin from Citrus grandis peel: in vitro antimicrobial activity and docking study. Mai TC, Tran NT, Mai DT, Ngoc Mai TT, Thuc Duyen NH, Minh An TN, Alam M, Dang CH, Nguyen TD, Nguyen TD. RSC Adv 12 25962-25976 (2022)


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