Target Information
Target General Infomation | |||||
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Target ID |
T09826
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Former ID |
TTDNC00422
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Target Name |
Toposisomerase-1
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Gene Name |
TOP1
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Synonyms |
DNA topoisomerase 1; DNA topoisomerase I; TOP1
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Target Type |
Clinical Trial
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Disease | Acquired immune deficiency syndrome [ICD9: 42; ICD10: B20] | ||||
Advanced ovarian cancer; Lung cancer [ICD9:183, 162; ICD10: C56, C33-C34] | |||||
Acute lymphoblastic leukemia [ICD9: 204.0, 556; ICD10: C91.0] | |||||
Breast cancer [ICD9: 174, 175; ICD10: C50] | |||||
Bladder cancer [ICD9: 188; ICD10: C67] | |||||
Colorectal cancer [ICD9: 153, 154; ICD10: C18-C21] | |||||
Cancer [ICD9: 140-229; ICD10: C00-C96] | |||||
Esophageal cancer [ICD9: 150; ICD10: C15] | |||||
Gastric cancer [ICD9: 151; ICD10: C16] | |||||
Glioblastoma multiforme; Myelodysplastic syndrome [ICD9:191, 238.7; ICD10: C71, D46] | |||||
Human immunodeficiency virus infection [ICD9: 279.3; ICD10: B20-B26] | |||||
Lymphoma [ICD9: 202.8, 208.9; ICD10: C81-C86] | |||||
Late-stage solid tumors [ICD9: 140-199, 210-229; ICD10: C00-C75, C7A, C7B, D10-D36, D3A] | |||||
Metastatic breast cancer; Metastatic colorectal cancer [ICD9:153, 154; ICD10: C50, C18-C21] | |||||
Metastatic breast cancer [ICD10: C50] | |||||
Ovarian cancer [ICD9: 183; ICD10: C56] | |||||
Solid tumours [ICD9: 140-199, 210-229; ICD10: C00-D48] | |||||
Unspecified [ICD code not available] | |||||
Function |
Releases the supercoiling and torsional tension of DNA introduced during the DNA replication and transcription by transiently cleaving and rejoining one strand of the DNA duplex. Introduces a single-strand break via transesterification at a target site in duplex DNA. The scissile phosphodiester is attacked by the catalytic tyrosine of the enzyme, resulting in the formation of a DNA-(3'-phosphotyrosyl)-enzyme intermediate and the expulsion ofa 5'-OH DNA strand. The free DNA strand then undergoes passage around the unbroken strand thus removing DNA supercoils. Finally, in the religation step, the DNA 5'-OH attacks the covalent intermediate to expel the active-site tyrosine and restore the DNA phosphodiester backbone (By similarity). Regulates the alternative splicing of tissue factor (F3) pre-mRNA in endothelial cells. .
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BioChemical Class |
DNA topoisomerase
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UniProt ID | |||||
EC Number |
EC 5.99.1.2
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Sequence |
MSGDHLHNDSQIEADFRLNDSHKHKDKHKDREHRHKEHKKEKDREKSKHSNSEHKDSEKK
HKEKEKTKHKDGSSEKHKDKHKDRDKEKRKEEKVRASGDAKIKKEKENGFSSPPQIKDEP EDDGYFVPPKEDIKPLKRPRDEDDADYKPKKIKTEDTKKEKKRKLEEEEDGKLKKPKNKD KDKKVPEPDNKKKKPKKEEEQKWKWWEEERYPEGIKWKFLEHKGPVFAPPYEPLPENVKF YYDGKVMKLSPKAEEVATFFAKMLDHEYTTKEIFRKNFFKDWRKEMTNEEKNIITNLSKC DFTQMSQYFKAQTEARKQMSKEEKLKIKEENEKLLKEYGFCIMDNHKERIANFKIEPPGL FRGRGNHPKMGMLKRRIMPEDIIINCSKDAKVPSPPPGHKWKEVRHDNKVTWLVSWTENI QGSIKYIMLNPSSRIKGEKDWQKYETARRLKKCVDKIRNQYREDWKSKEMKVRQRAVALY FIDKLALRAGNEKEEGETADTVGCCSLRVEHINLHPELDGQEYVVEFDFLGKDSIRYYNK VPVEKRVFKNLQLFMENKQPEDDLFDRLNTGILNKHLQDLMEGLTAKVFRTYNASITLQQ QLKELTAPDENIPAKILSYNRANRAVAILCNHQRAPPKTFEKSMMNLQTKIDAKKEQLAD ARRDLKSAKADAKVMKDAKTKKVVESKKKAVQRLEEQLMKLEVQATDREENKQIALGTSK LNYLDPRITVAWCKKWGVPIEKIYNKTQREKFAWAIDMADEDYEF |
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Structure |
1A31; 1A35; 1A36; 1EJ9; 1K4S; 1K4T; 1LPQ; 1NH3; 1R49; 1RR8; 1RRJ; 1SC7; 1SEU; 1T8I; 1TL8
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Drugs and Mode of Action | |||||
Drug(s) | Camptothecin | Drug Info | Phase 3 | Solid tumours | [528447] |
Edotecarin | Drug Info | Phase 3 | Gastric cancer | [527575] | |
Etirinotecan pegol | Drug Info | Phase 3 | Metastatic breast cancer | [523725] | |
Exatecan | Drug Info | Phase 3 | Solid tumours | [521494] | |
Karenitecin | Drug Info | Phase 3 | Advanced ovarian cancer; Lung cancer | [522031] | |
Rubitecan | Drug Info | Phase 3 | Human immunodeficiency virus infection | [521474] | |
9-AMINOCAMPTOTHECIN | Drug Info | Phase 2 | Acquired immune deficiency syndrome | [521423] | |
Anthracycline | Drug Info | Phase 2 | Solid tumours | [526964] | |
AR-67 | Drug Info | Phase 2 | Glioblastoma multiforme; Myelodysplastic syndrome | [523046] | |
Beta-Lapachone | Drug Info | Phase 2 | Solid tumours | [526407] | |
CRLX101 | Drug Info | Phase 2 | Late-stage solid tumors | [524225] | |
DIFLOMOTECAN | Drug Info | Phase 2 | Solid tumours | [521592] | |
EQ-917 | Drug Info | Phase 2 | Cancer | [532274] | |
Gimatecan | Drug Info | Phase 2 | Breast cancer | [532152] | |
LE-SN38 | Drug Info | Phase 2 | Colorectal cancer | [532503] | |
PEG-SN38 | Drug Info | Phase 2 | Metastatic breast cancer; Metastatic colorectal cancer | [522902], [532503] | |
Pegamotecan | Drug Info | Phase 2 | Esophageal cancer | [521591] | |
Polyglutamate camptothecin | Drug Info | Phase 2 | Solid tumours | [521802] | |
SN-38 | Drug Info | Phase 2 | Cancer | [532503], [541970] | |
TLC-388 | Drug Info | Phase 2 | Solid tumours | [534814] | |
XR-5000 | Drug Info | Phase 2 | Colorectal cancer | [526364] | |
ABI-011 | Drug Info | Phase 1 | Solid tumours | [523113] | |
Afeletecan | Drug Info | Phase 1 | Breast cancer | [547154] | |
CZ-48 | Drug Info | Phase 1 | Cancer | [522742] | |
Daniquidone | Drug Info | Phase 1 | Lymphoma | [521991] | |
DRF-1042 | Drug Info | Phase 1 | Solid tumours | [547222] | |
ELOMOTECAN HYDROCHLORIDE | Drug Info | Phase 1 | Solid tumours | [523624] | |
Genz-644282 | Drug Info | Phase 1 | Solid tumours | [522733] | |
GZ402674 | Drug Info | Phase 1 | Solid tumours | [549434] | |
INTOPLICINE | Drug Info | Phase 1 | Solid tumours | [521454] | |
MLN-576 | Drug Info | Phase 1 | Acute lymphoblastic leukemia | [526301] | |
Namitecan | Drug Info | Phase 1 | Solid tumours | [524157] | |
Tafluposide | Drug Info | Phase 1 | Cancer | [547025] | |
XMT-1001 | Drug Info | Phase 1 | Solid tumours | [521999] | |
(S)-DRF-1042 | Drug Info | Clinical trial | Bladder cancer | [543018] | |
BECATECARIN | Drug Info | Discontinued in Phase 3 | Solid tumours | [549905] | |
Atiratecan | Drug Info | Discontinued in Phase 2 | Colorectal cancer | [548306] | |
Lurtotecan | Drug Info | Discontinued in Phase 2 | Ovarian cancer | [545826] | |
S-16020-2 | Drug Info | Discontinued in Phase 2 | Solid tumours | [545682] | |
DE-310 | Drug Info | Discontinued in Phase 1 | Cancer | [547221] | |
BE-13793C | Drug Info | Terminated | Cancer | [545869] | |
BN-80245 | Drug Info | Terminated | Cancer | [546946] | |
CZ-112 | Drug Info | Terminated | Solid tumours | [546939] | |
ED-110 | Drug Info | Terminated | Cancer | [545230] | |
PIROXANTRONE | Drug Info | Terminated | Cancer | [545671] | |
TAN-1496 | Drug Info | Terminated | Cancer | [545717] | |
Inhibitor | (S)-DRF-1042 | Drug Info | [543672] | ||
9-AMINOCAMPTOTHECIN | Drug Info | [525970] | |||
A35566-A | Drug Info | [543672] | |||
Afeletecan | Drug Info | [544231] | |||
AR-67 | Drug Info | [532769] | |||
ATI-1150 | Drug Info | [543672] | |||
Atiratecan | Drug Info | [531647] | |||
BN-80245 | Drug Info | [551651] | |||
CZ-112 | Drug Info | [525971] | |||
CZ-48 | Drug Info | [525971] | |||
DE-310 | Drug Info | [527636] | |||
DIFLOMOTECAN | Drug Info | [529845] | |||
DRF-1042 | Drug Info | [525970], [527487] | |||
DTS-108 | Drug Info | [543672] | |||
Edotecarin | Drug Info | [527575] | |||
EQ-917 | Drug Info | [530982] | |||
Etirinotecan pegol | Drug Info | [532960] | |||
Exatecan | Drug Info | [526228] | |||
Genz-644282 | Drug Info | [531401] | |||
Gimatecan | Drug Info | [532255] | |||
IDN-5174 | Drug Info | [543672] | |||
IDN-6384 | Drug Info | [543672] | |||
Karenitecin | Drug Info | [525703] | |||
LE-SN38 | Drug Info | [532122] | |||
Lurtotecan | Drug Info | [543672] | |||
MEN-14295 | Drug Info | [543672] | |||
Namitecan | Drug Info | [531937] | |||
PEG-SN38 | Drug Info | [532064] | |||
Pegamotecan | Drug Info | [529412] | |||
Polyglutamate camptothecin | Drug Info | [528447] | |||
Rubitecan | Drug Info | [527937] | |||
TLC-388 | Drug Info | [534814] | |||
XMT-1001 | Drug Info | [531833] | |||
Modulator | ABI-011 | Drug Info | |||
Anthracycline | Drug Info | ||||
BE-13793C | Drug Info | ||||
BECATECARIN | Drug Info | [1572591] | |||
Beta-Lapachone | Drug Info | [526407] | |||
Camptothecin | Drug Info | [528447] | |||
CRISNATOL MESILATE | Drug Info | [1572605] | |||
CRLX101 | Drug Info | ||||
Daniquidone | Drug Info | ||||
ED-110 | Drug Info | [525422] | |||
ELOMOTECAN HYDROCHLORIDE | Drug Info | ||||
GZ402674 | Drug Info | [543672] | |||
INTOPLICINE | Drug Info | ||||
MLN-576 | Drug Info | [526301] | |||
PIROXANTRONE | Drug Info | ||||
S-16020-2 | Drug Info | ||||
SN-38 | Drug Info | ||||
Tafluposide | Drug Info | [526671] | |||
TAN-1496 | Drug Info | [533845] | |||
TH-1320 | Drug Info | [543672] | |||
XR-5000 | Drug Info | [526364] | |||
Stimulator | SER-203 | Drug Info | [543672] | ||
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM) | |||||
DRM | DRM Info | ||||
Pathways | |||||
NetPath Pathway | IL2 Signaling Pathway | ||||
PANTHER Pathway | DNA replication | ||||
Pathway Interaction Database | Caspase Cascade in Apoptosis | ||||
WikiPathways | Integrated Pancreatic Cancer Pathway | ||||
References | |||||
Ref 521423 | ClinicalTrials.gov (NCT00001427) A Phase II Trial of 72-Hour Continuous IV Infusion of 9-Aminocamptothecin With G-CSF Support in Patients With Advanced Ovarian Cancer Previously Treated With Paclitaxel and Cisplatin. U.S. National Institutes of Health. | ||||
Ref 521454 | ClinicalTrials.gov (NCT00003713) Chemotherapy in Treating Patients With Advanced or Metastatic Solid Tumors. U.S. National Institutes of Health. | ||||
Ref 521474 | ClinicalTrials.gov (NCT00005869) Nitrocamptothecin Compared With Gemcitabine in Treating Patients With Unresectable Locally Advanced or Metastatic Pancreatic Cancer. U.S. National Institutes of Health. | ||||
Ref 521494 | ClinicalTrials.gov (NCT00023972) Gemcitabine With or Without Exatecan Mesylate in Treating Patients With Locally Advanced or Metastatic Pancreatic Cancer. U.S. National Institutes of Health. | ||||
Ref 521591 | ClinicalTrials.gov (NCT00080002) Efficacy of Pegamotecan (PEG-Camptothecin) in Localized or Metastatic Cancer of the Stomach or Gastroesophageal Junction. U.S. National Institutes of Health. | ||||
Ref 521592 | ClinicalTrials.gov (NCT00080015) Diflomotecan (BN80915) Administered Once Every 3 Weeks in Treating Patients With Sensitive Small Cell Lung Cancer (SCLC). U.S. National Institutes of Health. | ||||
Ref 521802 | ClinicalTrials.gov (NCT00291837) CT-2106 for the Second Line Treatment of Ovarian Cancer. U.S. National Institutes of Health. | ||||
Ref 521991 | ClinicalTrials.gov (NCT00450502) Safety of Batracylin in Patients With Solid Tumors and Lymphomas. U.S. National Institutes of Health. | ||||
Ref 521999 | ClinicalTrials.gov (NCT00455052) A Study of Intravenous XMT-1001 in Patients With Advanced Solid Tumors. U.S. National Institutes of Health. | ||||
Ref 522031 | ClinicalTrials.gov (NCT00477282) Karenitecin Versus Topotecan in Patients With Advanced Epithelial Ovarian Cancer. U.S. National Institutes of Health. | ||||
Ref 522733 | ClinicalTrials.gov (NCT00942799) Dose Escalation Study to Assess the Safety and Tolerability of Genz-644282 in Patients With Solid Tumors. U.S. National Institutes of Health. | ||||
Ref 522742 | ClinicalTrials.gov (NCT00947739) Phase I and Pharmacology Study of Camptothecin-20-O-Propionate Hydrate (CZ48) in Patients With Solid Tumors or Lymphoma. U.S. National Institutes of Health. | ||||
Ref 522902 | ClinicalTrials.gov (NCT01036113) A Phase 2 Study of EZN-2208 in Patients With Metastatic Breast Cancer. U.S. National Institutes of Health. | ||||
Ref 523046 | ClinicalTrials.gov (NCT01124539) Study of AR-67 in Adult Patients With Recurrence of Glioblastoma Multiforme (GBM) or Gliosarcoma. U.S. National Institutes of Health. | ||||
Ref 523113 | ClinicalTrials.gov (NCT01163071) A Phase 1 Trial of ABI-011 in Patients With Advanced Solid Tumors or Lymphomas. U.S. National Institutes of Health. | ||||
Ref 523624 | ClinicalTrials.gov (NCT01435096) BN80927 in Patients With Advanced Malignant Solid Tumors. U.S. National Institutes of Health. | ||||
Ref 523725 | ClinicalTrials.gov (NCT01492101) The BEACON Study (Breast Cancer Outcomes With NKTR-102). U.S. National Institutes of Health. | ||||
Ref 524157 | ClinicalTrials.gov (NCT01748019) ST1968 Intravenous (Weekly) in Solid Tumors. U.S. National Institutes of Health. | ||||
Ref 524225 | ClinicalTrials.gov (NCT01803269) Topotecan Hydrochloride or Cyclodextrin-Based Polymer-Camptothecin CRLX101 in Treating Patients With Recurrent Small Cell Lung Cancer. U.S. National Institutes of Health. | ||||
Ref 526301 | In vitro and in vivo characterization of XR11576, a novel, orally active, dual inhibitor of topoisomerase I and II. Anticancer Drugs. 2002 Jan;13(1):15-28. | ||||
Ref 526364 | Phase II study of XR5000 (DACA) administered as a 120-h infusion in patients with recurrent glioblastoma multiforme. Ann Oncol. 2002 May;13(5):777-80. | ||||
Ref 526964 | Multicentre, phase II study evaluating capecitabine monotherapy in patients with anthracycline- and taxane-pretreated metastatic breast cancer. Eur J Cancer. 2004 Mar;40(4):536-42. | ||||
Ref 527575 | Edotecarin: a novel topoisomerase I inhibitor. Clin Colorectal Cancer. 2005 May;5(1):27-36. | ||||
Ref 528447 | Topoisomerase I inhibitors: camptothecins and beyond. Nat Rev Cancer. 2006 Oct;6(10):789-802. | ||||
Ref 532152 | A phase II trial of oral gimatecan for recurrent glioblastoma. J Neurooncol. 2013 Feb;111(3):347-53. | ||||
Ref 532274 | Phase II study of camtobell inj. (belotecan) in combination with cisplatin in patients with previously untreated, extensive stage small cell lung cancer. Lung Cancer. 2013 Jun;80(3):313-8. | ||||
Ref 532503 | Randomized phase 2 study of pegylated SN-38 (EZN-2208) or irinotecan plus cetuximab in patients with advanced colorectal cancer. Cancer. 2013 Dec 15;119(24):4223-30. | ||||
Ref 534814 | Topotecan - A novel topoisomerase I inhibitor: pharmacology and clinical experience. Oncology. 1999;56(1):1-12. | ||||
Ref 541970 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 6925). | ||||
Ref 543018 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 8261). | ||||
Ref 545230 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002530) | ||||
Ref 545671 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800004116) | ||||
Ref 545682 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800004159) | ||||
Ref 545717 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800004359) | ||||
Ref 545826 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800004939) | ||||
Ref 545869 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800005130) | ||||
Ref 546939 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800011353) | ||||
Ref 546946 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800011416) | ||||
Ref 547025 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800012192) | ||||
Ref 547154 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800013469) | ||||
Ref 547221 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800014192) | ||||
Ref 547222 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800014200) | ||||
Ref 548306 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800024385) | ||||
Ref 525422 | Indolocarbazole poisons of human topoisomerase I: regioisomeric analogues of ED-110. Bioorg Med Chem Lett. 1999 Jan 18;9(2):145-50. | ||||
Ref 525703 | Characterization of protein kinase chk1 essential for the cell cycle checkpoint after exposure of human head and neck carcinoma A253 cells to a novel topoisomerase I inhibitor BNP1350. Mol Pharmacol.2000 Mar;57(3):453-9. | ||||
Ref 525970 | Intraperitoneal topoisomerase-I inhibitors. Preliminary findings with 9-aminocamptothecin. Ann N Y Acad Sci. 2000;922:178-87. | ||||
Ref 526228 | Phase I study of topoisomerase I inhibitor exatecan mesylate (DX-8951f) given as weekly 24-hour infusions three of every four weeks. Clin Cancer Res. 2001 Dec;7(12):3963-70. | ||||
Ref 526301 | In vitro and in vivo characterization of XR11576, a novel, orally active, dual inhibitor of topoisomerase I and II. Anticancer Drugs. 2002 Jan;13(1):15-28. | ||||
Ref 526364 | Phase II study of XR5000 (DACA) administered as a 120-h infusion in patients with recurrent glioblastoma multiforme. Ann Oncol. 2002 May;13(5):777-80. | ||||
Ref 526671 | Ex vivo effects of the dual topoisomerase inhibitor tafluposide (F 11782) on cells isolated from fresh tumor samples taken from patients with cancer. Anticancer Drugs. 2003 Jul;14(6):467-73. | ||||
Ref 527487 | Safety, tolerability, and pharmacokinetics of a capsule formulation of DRF-1042, a novel camptothecin analog, in refractory cancer patients in a bridging phase I study. J Clin Pharmacol. 2005 Apr;45(4):453-60. | ||||
Ref 527575 | Edotecarin: a novel topoisomerase I inhibitor. Clin Colorectal Cancer. 2005 May;5(1):27-36. | ||||
Ref 527636 | DE-310, a macromolecular prodrug of the topoisomerase-I-inhibitor exatecan (DX-8951), in patients with operable solid tumors. Invest New Drugs. 2005 Aug;23(4):339-47. | ||||
Ref 528447 | Topoisomerase I inhibitors: camptothecins and beyond. Nat Rev Cancer. 2006 Oct;6(10):789-802. | ||||
Ref 529412 | A phase II study of pegylated-camptothecin (pegamotecan) in the treatment of locally advanced and metastatic gastric and gastro-oesophageal junction adenocarcinoma. Cancer Chemother Pharmacol. 2009 Jan;63(2):363-70. | ||||
Ref 529845 | Diflomotecan, a promising homocamptothecin for cancer therapy. Expert Opin Investig Drugs. 2009 Jan;18(1):69-75. | ||||
Ref 530982 | The efficacy and toxicity of belotecan (CKD-602), a camptothericin analogue topoisomerase I inhibitor, in patients with recurrent or refractory epithelial ovarian cancer. J Chemother. 2010 Jun;22(3):197-200. | ||||
Ref 531401 | Genz-644282, a novel non-camptothecin topoisomerase I inhibitor for cancer treatment. Clin Cancer Res. 2011 May 1;17(9):2777-87. | ||||
Ref 531647 | Method development and validation of the simultaneous determination of a novel topoisomerase 1 inhibitor, the prodrug, and the active metabolite in human plasma using column-switching LC-MS/MS, and its application in a clinical trial. J Chromatogr B Analyt Technol Biomed Life Sci. 2011 Nov 15;879(30):3415-22. | ||||
Ref 531833 | Pharmacokinetics and antitumor efficacy of XMT-1001, a novel, polymeric topoisomerase I inhibitor, in mice bearing HT-29 human colon carcinoma xenografts. Clin Cancer Res. 2012 May 1;18(9):2591-602. | ||||
Ref 531937 | Namitecan: a hydrophilic camptothecin with a promising preclinical profile. Curr Med Chem. 2012;19(21):3488-501. | ||||
Ref 532064 | EZN-2208 (PEG-SN38) overcomes ABCG2-mediated topotecan resistance in BRCA1-deficient mouse mammary tumors. PLoS One. 2012;7(9):e45248. | ||||
Ref 532122 | Analysis of type of cell death induced by topoisomerase inhibitor SN-38 in human oral squamous cell carcinoma cell lines. Anticancer Res. 2012 Nov;32(11):4823-32. | ||||
Ref 532255 | Gimatecan and other camptothecin derivatives poison Leishmania DNA-topoisomerase IB leading to a strong leishmanicidal effect. Biochem Pharmacol. 2013 May 15;85(10):1433-40. | ||||
Ref 532769 | Protracted dosing of the lipophilic camptothecin analogue AR-67 in non-small cell lung cancer xenografts and humans. Cancer Chemother Pharmacol. 2014 Jul;74(1):45-54. | ||||
Ref 532960 | Nonclinical pharmacokinetics and activity of etirinotecan pegol (NKTR-102), a long-acting topoisomerase 1 inhibitor, in multiple cancer models. Cancer Chemother Pharmacol. 2014 Dec;74(6):1125-37. | ||||
Ref 533845 | TAN-1496 A, C and E, diketopiperazine antibiotics with inhibitory activity against mammalian DNA topoisomerase I. J Antibiot (Tokyo). 1994 Nov;47(11):1202-18. | ||||
Ref 534814 | Topotecan - A novel topoisomerase I inhibitor: pharmacology and clinical experience. Oncology. 1999;56(1):1-12. | ||||
Ref 543672 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 2636). | ||||
Ref 544231 | The fate of camptothecin glycoconjugate: report of a clinical hold during a phase II study of BAY 56-3722 (formerly BAY 38-3441), in patients with recurrent or metastatic colorectal cancer resistant/refractory to irinotecan. Invest New Drugs. 2012 June; 30(3): 1208-1210. | ||||
Ref 551651 | BN 80245: An E-ring modified camptothecin with potent antiproliferative and topoisomerase I inhibitory activities. Bioorganic & Medicinal Chemistry Letters Volume 7, Issue 17, 9 September 1997, Pages2235-2238. |
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