Page last updated: 2024-08-07 15:54:47
DNA topoisomerase 2-alpha
A DNA topoisomerase 2-alpha that is encoded in the genome of human. [PRO:DNx, UniProtKB:P11388]
Synonyms
EC 5.6.2.2;
DNA topoisomerase II, alpha isozyme
Research
Bioassay Publications (79)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 19 (24.05) | 18.2507 |
| 2000's | 16 (20.25) | 29.6817 |
| 2010's | 35 (44.30) | 24.3611 |
| 2020's | 9 (11.39) | 2.80 |
Compounds (236)
Drugs with Inhibition Measurements
Drugs with Activation Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| amsacrine | Homo sapiens (human) | EC50 | 0.7200 | 2 | 2 |
| fasudil | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| 4-(4'-hydroxyphenyl)-amino-6,7-dimethoxyquinazoline | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| imatinib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| etoposide | Homo sapiens (human) | EC50 | 28.4050 | 2 | 2 |
| triciribine phosphate | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| picropodophyllin | Homo sapiens (human) | Kd | 0.4860 | 1 | 1 |
| cp 115953 | Homo sapiens (human) | EC50 | 1.2000 | 1 | 1 |
| pd-117596 | Homo sapiens (human) | EC50 | 340.0000 | 1 | 1 |
| gefitinib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| lestaurtinib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| vatalanib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| cyc 202 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| erlotinib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| lapatinib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| sorafenib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| s 1033 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| xl147 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| bms 387032 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| win 33377 | Homo sapiens (human) | EC50 | 3.0000 | 1 | 1 |
| sf 2370 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| ha 1100 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| 7-epi-hydroxystaurosporine | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| zd 6474 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| imd 0354 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| sirolimus | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| alvocidib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| bosutinib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| orantinib | Homo sapiens (human) | Kd | 30.0000 | 1 | 2 |
| su 11248 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| palbociclib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| vx680 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| cyc 116 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| everolimus | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| ekb 569 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| axitinib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| temsirolimus | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| on 01910 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| av 412 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| telatinib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| edotecarin | Homo sapiens (human) | EC50 | 50.0000 | 1 | 1 |
| y-39983 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| cp 547632 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| lenvatinib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| pd 0325901 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| midostaurin | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| osi 930 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| cp 724714 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| hmn-214 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| sr 271425 | Homo sapiens (human) | EC50 | 480.0000 | 1 | 1 |
| tivozanib | Homo sapiens (human) | Kd | 30.0000 | 1 | 2 |
| hki 272 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| tofacitinib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| cediranib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| masitinib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| ly-2157299 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| pazopanib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| azd 6244 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| su 14813 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| bibw 2992 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| binimetinib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| sotrastaurin | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| aee 788 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| saracatinib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| vx 702 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| crenolanib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| tg100-115 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| cc 401 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| exel-7647 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| volasertib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| azd 7762 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| regorafenib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| 6-[[5-fluoro-2-(3,4,5-trimethoxyanilino)-4-pyrimidinyl]amino]-2,2-dimethyl-4H-pyrido[3,2-b][1,4]oxazin-3-one | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| mp470 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| rgb 286638 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| np 031112 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| at 7519 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| bi 2536 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| kw 2449 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| danusertib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| arq 197 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| azd 1152 | Homo sapiens (human) | Kd | 30.0000 | 1 | 2 |
| ridaforolimus | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| ch 4987655 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| 6-(5-((cyclopropylamino)carbonyl)-3-fluoro-2-methylphenyl)-n-(2,2-dimethylprpyl)-3-pyridinecarboxamide | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| cc-930 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| idelalisib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| crizotinib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| trametinib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| mln8054 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| jnj-26483327 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| ly2603618 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| dactolisib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| bgt226 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| gsk 461364 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| enmd 2076 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| e 7050 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| 2-amino-8-ethyl-4-methyl-6-(1H-pyrazol-5-yl)-7-pyrido[2,3-d]pyrimidinone | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| gdc-0973 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| azd 1480 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| azd8330 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| ro5126766 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| fedratinib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| gsk690693 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| 14-methyl-20-oxa-5,7,14,26-tetraazatetracyclo(19.3.1.1(2,6).1(8,12))heptacosa-1(25),2(26),3,5,8(27),9,11,16,21,23-decaene | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| azd5438 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| pf 04217903 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| gdc 0941 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| icotinib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| kx-01 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| mk 5108 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| cudc 101 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| arry-614 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| tak 593 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| mln 8237 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| sgx 523 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| bms 754807 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| sgi 1776 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| pci 32765 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| ponatinib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| amg 900 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| mk-1775 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| AMG-208 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| quizartinib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| at13148 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| tak 733 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| mk 2206 | Homo sapiens (human) | Kd | 30.0000 | 1 | 2 |
| sns 314 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| lucitanib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| pf-04691502 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| n-(cyanomethyl)-4-(2-((4-(4-morpholinyl)phenyl)amino)-4-pyrimidinyl)benzamide | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| dcc-2036 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| defactinib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| poziotinib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| asp3026 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| entrectinib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| pexidartinib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| TAK-580 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| gsk 2126458 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| pf 3758309 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| gdc 0980 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| (5-(2,4-bis((3s)-3-methylmorpholin-4-yl)pyrido(2,3-d)pyrimidin-7-yl)-2-methoxyphenyl)methanol | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| plx4032 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| gsk 1363089 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| arry-334543 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| kin-193 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| mk 2461 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| as 703026 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| baricitinib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| dabrafenib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| pki 587 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| n-(3-fluoro-4-((1-methyl-6-(1h-pyrazol-4-yl)-1h-indazol-5 yl)oxy)phenyl)-1-(4-fluorophenyl)-6-methyl-2-oxo-1,2-dihydropyridine-3-carboxamide | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| ribociclib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| pha 793887 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| abemaciclib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| afuresertib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| gsk 1070916 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| jnj38877605 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| dinaciclib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| gilteritinib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| alectinib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| encorafenib | Homo sapiens (human) | Kd | 30.0000 | 1 | 2 |
| gsk2141795 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| azd8186 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| byl719 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| cep-32496 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| rociletinib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| ceritinib | Homo sapiens (human) | Kd | 30.0000 | 1 | 2 |
| azd1208 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| vx-509 | Homo sapiens (human) | Kd | 0.0640 | 1 | 1 |
| debio 1347 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| volitinib | Homo sapiens (human) | Kd | 30.0000 | 1 | 2 |
| osimertinib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| at 9283 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| otssp167 | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
| osi 027 | Homo sapiens (human) | Kd | 30.0000 | 1 | 2 |
| nintedanib | Homo sapiens (human) | Kd | 30.0000 | 1 | 1 |
Drugs with Other Measurements
[no title available]RSC medicinal chemistry, , Mar-01, Volume: 11, Issue:3, 2020
Novel trifluoromethylated 9-amino-3,4-dihydroacridin-1(2H)-ones act as covalent poisons of human topoisomerase IIα.Bioorganic & medicinal chemistry letters, , 02-01, Volume: 27, Issue:3, 2017
New derivatives of 11-methyl-6-[2-(dimethylamino)ethyl]-6H-indolo[2,3-b]quinoline as cytotoxic DNA topoisomerase II inhibitors.Bioorganic & medicinal chemistry letters, , Oct-01, Volume: 22, Issue:19, 2012
Synthesis, cytotoxic activity, DNA topoisomerase-II inhibition, molecular modeling and structure-activity relationship of 9-anilinothiazolo[5,4-b]quinoline derivatives.Bioorganic & medicinal chemistry, , May-01, Volume: 17, Issue:9, 2009
Synthesis and antitumor activity of 4-aminomethylthioxanthenone and 5-aminomethylbenzothiopyranoindazole derivatives.Journal of medicinal chemistry, , Sep-10, Volume: 41, Issue:19, 1998
Topoisomerase II-mediated DNA cleavage by adocia- and xestoquinones from the Philippine sponge Xestospongia sp.Journal of medicinal chemistry, , Oct-27, Volume: 38, Issue:22, 1995
9-substituted acridine derivatives with long half-life and potent antitumor activity: synthesis and structure-activity relationships.Journal of medicinal chemistry, , Aug-18, Volume: 38, Issue:17, 1995
Inhibition of topoisomerase II catalytic activity by pyridoacridine alkaloids from a Cystodytes sp. ascidian: a mechanism for the apparent intercalator-induced inhibition of topoisomerase II.Journal of medicinal chemistry, , Oct-28, Volume: 37, Issue:22, 1994
Mammalian topoisomerase II inhibitory activity of 1-cyclopropyl-6,8- difluoro-1,4-dihydro-7-(2,6-dimethyl-4-pyridinyl)-4-oxo-3-quinolinecarb oxylic acid and related derivatives.Journal of medicinal chemistry, , Sep-17, Volume: 36, Issue:19, 1993
Discovery and structure-activity relationships of a novel oxazolidinone class of bacterial type II topoisomerase inhibitors.Bioorganic & medicinal chemistry letters, , 06-01, Volume: 65, 2022
[no title available]Journal of medicinal chemistry, , 03-28, Volume: 62, Issue:6, 2019
Discovery and Optimization of Isoquinoline Ethyl Ureas as Antibacterial Agents.Journal of medicinal chemistry, , 05-11, Volume: 60, Issue:9, 2017
Development of a Dual-Acting Antibacterial Agent (TNP-2092) for the Treatment of Persistent Bacterial Infections.Journal of medicinal chemistry, , 07-28, Volume: 59, Issue:14, 2016
7-((4-Substituted)piperazin-1-yl) derivatives of ciprofloxacin: synthesis and in vitro biological evaluation as potential antitumor agents.Bioorganic & medicinal chemistry, , Aug-01, Volume: 17, Issue:15, 2009
Isothiazoloquinolones with enhanced antistaphylococcal activities against multidrug-resistant strains: effects of structural modifications at the 6-, 7-, and 8-positions.Journal of medicinal chemistry, , Jan-25, Volume: 50, Issue:2, 2007
The structure-based design, synthesis and biological evaluation of DNA-binding bisintercalating bisanthrapyrazole anticancer compounds.Bioorganic & medicinal chemistry, , Apr-01, Volume: 16, Issue:7, 2008
Topoisomerase II-mediated DNA cleavage by adocia- and xestoquinones from the Philippine sponge Xestospongia sp.Journal of medicinal chemistry, , Oct-27, Volume: 38, Issue:22, 1995
Inhibition of topoisomerase II catalytic activity by pyridoacridine alkaloids from a Cystodytes sp. ascidian: a mechanism for the apparent intercalator-induced inhibition of topoisomerase II.Journal of medicinal chemistry, , Oct-28, Volume: 37, Issue:22, 1994
Targeting topoisomerase II with trypthantrin derivatives: Discovery of 7-((2-(dimethylamino)ethyl)amino)indolo[2,1-b]quinazoline-6,12-dione as an antiproliferative agent and to treat cancer.European journal of medicinal chemistry, , Sep-15, Volume: 202, 2020
[no title available]RSC medicinal chemistry, , Mar-01, Volume: 11, Issue:3, 2020
Novel, Potent, and Druglike Tetrahydroquinazoline Inhibitor That Is Highly Selective for Human Topoisomerase II α over β.Journal of medicinal chemistry, , 11-12, Volume: 63, Issue:21, 2020
Design, Synthesis, Dynamic Docking, Biochemical Characterization, and Journal of medicinal chemistry, , 04-09, Volume: 63, Issue:7, 2020
Pharmacophore Hybridization To Discover Novel Topoisomerase II Poisons with Promising Antiproliferative Activity.Journal of medicinal chemistry, , 02-08, Volume: 61, Issue:3, 2018
Discovery of Novel Topoisomerase II Inhibitors by Medicinal Chemistry Approaches.Journal of medicinal chemistry, , 10-25, Volume: 61, Issue:20, 2018
Polyamine-containing etoposide derivatives as poisons of human type II topoisomerases: Differential effects on topoisomerase IIα and IIβ.Bioorganic & medicinal chemistry letters, , 09-15, Volume: 28, Issue:17, 2018
Synthesis and biological evaluation of histone deacetylase and DNA topoisomerase II-Targeted inhibitors.Bioorganic & medicinal chemistry, , 05-01, Volume: 26, Issue:8, 2018
Design, synthesis, and evaluation of DNA topoisomerase II-targeted nucleosides.Bioorganic & medicinal chemistry, , 08-01, Volume: 25, Issue:15, 2017
Novel trifluoromethylated 9-amino-3,4-dihydroacridin-1(2H)-ones act as covalent poisons of human topoisomerase IIα.Bioorganic & medicinal chemistry letters, , 02-01, Volume: 27, Issue:3, 2017
Design, synthesis, cytotoxicity, HuTopoIIα inhibitory activity and molecular docking studies of pyrazole derivatives as potential anticancer agents.Bioorganic chemistry, , Volume: 69, 2016
Imine/amide-imidazole conjugates derived from 5-amino-4-cyano-N1-substituted benzyl imidazole: Microwave-assisted synthesis and anticancer activity via selective topoisomerase-II-α inhibition.Bioorganic & medicinal chemistry, , Sep-01, Volume: 23, Issue:17, 2015
Cytotoxicity and topoisomerase I/II inhibition activity of novel 4-aryl/alkyl-1-(piperidin-4-yl)-carbonylthiosemicarbazides and 4-benzoylthiosemicarbazides.Journal of enzyme inhibition and medicinal chemistry, , Volume: 29, Issue:2, 2014
Monocyclic 4-amino-6-(phenylamino)-1,3,5-triazines as inhibitors of human DNA topoisomerase IIα.Bioorganic & medicinal chemistry letters, , Dec-15, Volume: 24, Issue:24, 2014
3-(3-Butylamino-2-hydroxy-propoxy)-1-hydroxy-xanthen-9-one acts as a topoisomerase IIα catalytic inhibitor with low DNA damage.European journal of medicinal chemistry, , Volume: 69, 2013
Synthesis of imine-pyrazolopyrimidinones and their mechanistic interventions on anticancer activity.Bioorganic & medicinal chemistry, , Sep-15, Volume: 21, Issue:18, 2013
Synthesis and evaluation of 2-[2-(phenylthiomethyl)-1H-benzo[d] imidazol-1-yl)acetohydrazide derivatives as antitumor agents.Bioorganic & medicinal chemistry letters, , May-01, Volume: 22, Issue:9, 2012
Synthesis and evaluation of mansonone F derivatives as topoisomerase inhibitors.European journal of medicinal chemistry, , Volume: 46, Issue:8, 2011
A diazirine-based photoaffinity etoposide probe for labeling topoisomerase II.Bioorganic & medicinal chemistry, , Jan-15, Volume: 18, Issue:2, 2010
Synthesis of 1-/2-substituted-[1,2,3]triazolo[4,5-g]phthalazine-4,9-diones and evaluation of their cytotoxicity and topoisomerase II inhibition.Bioorganic & medicinal chemistry, , Apr-15, Volume: 16, Issue:8, 2008
Synthesis and antitumor characterization of pyrazolic analogues of the marine pyrroloquinoline alkaloids: wakayin and tsitsikammamines.Journal of medicinal chemistry, , May-18, Volume: 49, Issue:10, 2006
Synthetic lanostane-type triterpenoids as inhibitors of DNA topoisomerase II.Bioorganic & medicinal chemistry letters, , Jun-15, Volume: 15, Issue:12, 2005
Current developments in the discovery and design of new drug candidates from plant natural product leads.Journal of natural products, , Volume: 67, Issue:2, 2004
Triterpenoid constituents isolated from the bark of Abies sachalinensis.Journal of natural products, , Volume: 65, Issue:11, 2002
Screening of triterpenoids isolated from Phyllanthus flexuosus for DNA topoisomerase inhibitory activity.Journal of natural products, , Volume: 64, Issue:12, 2001
Antitumor agents. 194. Synthesis and biological evaluations of 4-beta-mono-, -di-, and -trisubstituted aniline-4'-O-demethyl-podophyllotoxin and related compounds with improved pharmacological profiles.Journal of medicinal chemistry, , Jul-01, Volume: 42, Issue:13, 1999
Synthesis and antitumor activity of new glycosides of epipodophyllotoxin, analogues of etoposide, and NK 611.Journal of medicinal chemistry, , Nov-05, Volume: 41, Issue:23, 1998
Antitumor agents. 185. Synthesis and biological evaluation of tridemethylthiocolchicine analogues as novel topoisomerase II inhibitors.Journal of medicinal chemistry, , May-21, Volume: 41, Issue:11, 1998
Topoisomerase II-mediated DNA cleavage by adocia- and xestoquinones from the Philippine sponge Xestospongia sp.Journal of medicinal chemistry, , Oct-27, Volume: 38, Issue:22, 1995
Inhibition of topoisomerase II catalytic activity by pyridoacridine alkaloids from a Cystodytes sp. ascidian: a mechanism for the apparent intercalator-induced inhibition of topoisomerase II.Journal of medicinal chemistry, , Oct-28, Volume: 37, Issue:22, 1994
Antitumor agents. 144. New gamma-lactone ring-modified arylamino etoposide analogs as inhibitors of human DNA topoisomerase II.Journal of medicinal chemistry, , Jan-21, Volume: 37, Issue:2, 1994
Antitumor agents. 148. Synthesis and biological evaluation of novel 4 beta-amino derivatives of etoposide with better pharmacological profiles.Journal of medicinal chemistry, , Feb-18, Volume: 37, Issue:4, 1994
Mammalian topoisomerase II inhibitory activity of 1-cyclopropyl-6,8- difluoro-1,4-dihydro-7-(2,6-dimethyl-4-pyridinyl)-4-oxo-3-quinolinecarb oxylic acid and related derivatives.Journal of medicinal chemistry, , Sep-17, Volume: 36, Issue:19, 1993
Antitumor agents. 123. Synthesis and human DNA topoisomerase II inhibitory activity of 2'-chloro derivatives of etoposide and 4 beta-(arylamino)-4'-O-demethylpodophyllotoxins.Journal of medicinal chemistry, , Mar-06, Volume: 35, Issue:5, 1992
Antitumor agents. 124. New 4 beta-substituted aniline derivatives of 6,7-O,O-demethylene-4'-O-demethylpodophyllotoxin and related compounds as potent inhibitors of human DNA topoisomerase II.Journal of medicinal chemistry, , Mar-06, Volume: 35, Issue:5, 1992
Antitumor agents, 130, Novel 4 beta-arylamino derivatives of 3',4'-didemethoxy-3',4'-dioxo-4-deoxypodophyllotoxin as potent inhibitors of human DNA topoisomerase II.Journal of natural products, , Volume: 55, Issue:8, 1992
Antitumor agents. 120. New 4-substituted benzylamine and benzyl ether derivatives of 4'-O-demethylepipodophyllotoxin as potent inhibitors of human DNA topoisomerase II.Journal of medicinal chemistry, , Volume: 34, Issue:12, 1991
Antitumor agents. 113. New 4 beta-arylamino derivatives of 4'-O-demethylepipodophyllotoxin and related compounds as potent inhibitors of human DNA topoisomerase II.Journal of medicinal chemistry, , Volume: 33, Issue:9, 1990
Antitumor agents. 111. New 4-hydroxylated and 4-halogenated anilino derivatives of 4'-demethylepipodophyllotoxin as potent inhibitors of human DNA topoisomerase II.Journal of medicinal chemistry, , Volume: 33, Issue:5, 1990
Antitumor agents, 107. New cytotoxic 4-alkylamino analogues of 4'-demethyl-epipodophyllotoxin as inhibitors of human DNA topoisomerase II.Journal of natural products, , Volume: 52, Issue:3
Current developments in the discovery and design of new drug candidates from plant natural product leads.Journal of natural products, , Volume: 67, Issue:2, 2004
Antitumor agents. 144. New gamma-lactone ring-modified arylamino etoposide analogs as inhibitors of human DNA topoisomerase II.Journal of medicinal chemistry, , Jan-21, Volume: 37, Issue:2, 1994
Antitumor agents. 123. Synthesis and human DNA topoisomerase II inhibitory activity of 2'-chloro derivatives of etoposide and 4 beta-(arylamino)-4'-O-demethylpodophyllotoxins.Journal of medicinal chemistry, , Mar-06, Volume: 35, Issue:5, 1992
Antitumor agents. 124. New 4 beta-substituted aniline derivatives of 6,7-O,O-demethylene-4'-O-demethylpodophyllotoxin and related compounds as potent inhibitors of human DNA topoisomerase II.Journal of medicinal chemistry, , Mar-06, Volume: 35, Issue:5, 1992
Antitumor agents, 130, Novel 4 beta-arylamino derivatives of 3',4'-didemethoxy-3',4'-dioxo-4-deoxypodophyllotoxin as potent inhibitors of human DNA topoisomerase II.Journal of natural products, , Volume: 55, Issue:8, 1992
Antitumor agents. 120. New 4-substituted benzylamine and benzyl ether derivatives of 4'-O-demethylepipodophyllotoxin as potent inhibitors of human DNA topoisomerase II.Journal of medicinal chemistry, , Volume: 34, Issue:12, 1991
Antitumor agents. 113. New 4 beta-arylamino derivatives of 4'-O-demethylepipodophyllotoxin and related compounds as potent inhibitors of human DNA topoisomerase II.Journal of medicinal chemistry, , Volume: 33, Issue:9, 1990
Antitumor agents. 111. New 4-hydroxylated and 4-halogenated anilino derivatives of 4'-demethylepipodophyllotoxin as potent inhibitors of human DNA topoisomerase II.Journal of medicinal chemistry, , Volume: 33, Issue:5, 1990
Antitumor agents. 194. Synthesis and biological evaluations of 4-beta-mono-, -di-, and -trisubstituted aniline-4'-O-demethyl-podophyllotoxin and related compounds with improved pharmacological profiles.Journal of medicinal chemistry, , Jul-01, Volume: 42, Issue:13, 1999
Antitumor agents. 123. Synthesis and human DNA topoisomerase II inhibitory activity of 2'-chloro derivatives of etoposide and 4 beta-(arylamino)-4'-O-demethylpodophyllotoxins.Journal of medicinal chemistry, , Mar-06, Volume: 35, Issue:5, 1992
Antitumor agents. 124. New 4 beta-substituted aniline derivatives of 6,7-O,O-demethylene-4'-O-demethylpodophyllotoxin and related compounds as potent inhibitors of human DNA topoisomerase II.Journal of medicinal chemistry, , Mar-06, Volume: 35, Issue:5, 1992
Antitumor agents, 130, Novel 4 beta-arylamino derivatives of 3',4'-didemethoxy-3',4'-dioxo-4-deoxypodophyllotoxin as potent inhibitors of human DNA topoisomerase II.Journal of natural products, , Volume: 55, Issue:8, 1992
Antitumor agents. 120. New 4-substituted benzylamine and benzyl ether derivatives of 4'-O-demethylepipodophyllotoxin as potent inhibitors of human DNA topoisomerase II.Journal of medicinal chemistry, , Volume: 34, Issue:12, 1991
Antitumor agents. 113. New 4 beta-arylamino derivatives of 4'-O-demethylepipodophyllotoxin and related compounds as potent inhibitors of human DNA topoisomerase II.Journal of medicinal chemistry, , Volume: 33, Issue:9, 1990
Design, Synthesis, Dynamic Docking, Biochemical Characterization, and Journal of medicinal chemistry, , 04-09, Volume: 63, Issue:7, 2020
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Enables
This protein enables 13 target(s):
| Target | Category | Definition |
|---|
| magnesium ion binding | molecular function | Binding to a magnesium (Mg) ion. [GOC:ai] |
| DNA binding | molecular function | Any molecular function by which a gene product interacts selectively and non-covalently with DNA (deoxyribonucleic acid). [GOC:dph, GOC:jl, GOC:tb, GOC:vw] |
| chromatin binding | molecular function | Binding to chromatin, the network of fibers of DNA, protein, and sometimes RNA, that make up the chromosomes of the eukaryotic nucleus during interphase. [GOC:jl, ISBN:0198506732, PMID:20404130] |
| RNA binding | molecular function | Binding to an RNA molecule or a portion thereof. [GOC:jl, GOC:mah] |
| DNA topoisomerase type II (double strand cut, ATP-hydrolyzing) activity | molecular function | Catalysis of a DNA topological transformation by transiently cleaving a pair of complementary DNA strands to form a gate through which a second double-stranded DNA segment is passed, after which the severed strands in the first DNA segment are rejoined, driven by ATP hydrolysis. The enzyme changes the linking number in multiples of 2. [PMID:8811192] |
| protein kinase C binding | molecular function | Binding to protein kinase C. [GOC:jl] |
| protein binding | molecular function | Binding to a protein. [GOC:go_curators] |
| ATP binding | molecular function | Binding to ATP, adenosine 5'-triphosphate, a universally important coenzyme and enzyme regulator. [ISBN:0198506732] |
| ATP-dependent activity, acting on DNA | molecular function | Catalytic activity that acts to modify DNA, driven by ATP hydrolysis. [GOC:pdt] |
| DNA binding, bending | molecular function | The activity of binding selectively and non-covalently to and distorting the original structure of DNA, typically a straight helix, into a bend, or increasing the bend if the original structure was intrinsically bent due to its sequence. [GOC:krc, GOC:vw, PMID:10710711, PMID:19037758] |
| protein homodimerization activity | molecular function | Binding to an identical protein to form a homodimer. [GOC:jl] |
| ubiquitin binding | molecular function | Binding to ubiquitin, a protein that when covalently bound to other cellular proteins marks them for proteolytic degradation. [GOC:ecd] |
| protein heterodimerization activity | molecular function | Binding to a nonidentical protein to form a heterodimer. [GOC:ai] |
Located In
This protein is located in 7 target(s):
| Target | Category | Definition |
|---|
| chromosome, centromeric region | cellular component | The region of a chromosome that includes the centromeric DNA and associated proteins. In monocentric chromosomes, this region corresponds to a single area of the chromosome, whereas in holocentric chromosomes, it is evenly distributed along the chromosome. [GOC:cjm, GOC:elh, GOC:kmv, GOC:pr] |
| condensed chromosome | cellular component | A highly compacted molecule of DNA and associated proteins resulting in a cytologically distinct structure. [GOC:elh] |
| male germ cell nucleus | cellular component | The nucleus of a male germ cell, a reproductive cell in males. [CL:0000015, GOC:hjd, GOC:mtg_sensu] |
| nucleus | cellular component | A membrane-bounded organelle of eukaryotic cells in which chromosomes are housed and replicated. In most cells, the nucleus contains all of the cell's chromosomes except the organellar chromosomes, and is the site of RNA synthesis and processing. In some species, or in specialized cell types, RNA metabolism or DNA replication may be absent. [GOC:go_curators] |
| nucleoplasm | cellular component | That part of the nuclear content other than the chromosomes or the nucleolus. [GOC:ma, ISBN:0124325653] |
| nucleolus | cellular component | A small, dense body one or more of which are present in the nucleus of eukaryotic cells. It is rich in RNA and protein, is not bounded by a limiting membrane, and is not seen during mitosis. Its prime function is the transcription of the nucleolar DNA into 45S ribosomal-precursor RNA, the processing of this RNA into 5.8S, 18S, and 28S components of ribosomal RNA, and the association of these components with 5S RNA and proteins synthesized outside the nucleolus. This association results in the formation of ribonucleoprotein precursors; these pass into the cytoplasm and mature into the 40S and 60S subunits of the ribosome. [ISBN:0198506732] |
| cytoplasm | cellular component | The contents of a cell excluding the plasma membrane and nucleus, but including other subcellular structures. [ISBN:0198547684] |
Active In
This protein is active in 1 target(s):
| Target | Category | Definition |
|---|
| nucleus | cellular component | A membrane-bounded organelle of eukaryotic cells in which chromosomes are housed and replicated. In most cells, the nucleus contains all of the cell's chromosomes except the organellar chromosomes, and is the site of RNA synthesis and processing. In some species, or in specialized cell types, RNA metabolism or DNA replication may be absent. [GOC:go_curators] |
Part Of
This protein is part of 3 target(s):
| Target | Category | Definition |
|---|
| DNA topoisomerase type II (double strand cut, ATP-hydrolyzing) complex | cellular component | Complex that possesses DNA topoisomerase II (double strand cut, ATP-hydrolyzing) activity. [GOC:bhm, GOC:krc, GOC:mah, WikiPedia:Type_II_topoisomerase] |
| protein-containing complex | cellular component | A stable assembly of two or more macromolecules, i.e. proteins, nucleic acids, carbohydrates or lipids, in which at least one component is a protein and the constituent parts function together. [GOC:dos, GOC:mah] |
| ribonucleoprotein complex | cellular component | A macromolecular complex that contains both RNA and protein molecules. [GOC:krc, GOC:vesicles] |
Involved In
This protein is involved in 16 target(s):
| Target | Category | Definition |
|---|
| hematopoietic progenitor cell differentiation | biological process | The process in which precursor cell type acquires the specialized features of a hematopoietic progenitor cell, a class of cell types including myeloid progenitor cells and lymphoid progenitor cells. [GOC:add, GOC:rl, ISBN:0781735149, PMID:16551251] |
| DNA topological change | biological process | The process in which a transformation is induced in the topological structure of a double-stranded DNA helix, resulting in a change in linking number. [ISBN:071673706X, ISBN:0935702490] |
| DNA ligation | biological process | The re-formation of a broken phosphodiester bond in the DNA backbone, carried out by DNA ligase. [ISBN:0815316194] |
| DNA damage response | biological process | Any process that results in a change in state or activity of a cell (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a stimulus indicating damage to its DNA from environmental insults or errors during metabolism. [GOC:go_curators] |
| chromosome segregation | biological process | The process in which genetic material, in the form of chromosomes, is organized into specific structures and then physically separated and apportioned to two or more sets. In eukaryotes, chromosome segregation begins with the condensation of chromosomes, includes chromosome separation, and ends when chromosomes have completed movement to the spindle poles. [GOC:jl, GOC:mah, GOC:mtg_cell_cycle, GOC:vw] |
| female meiotic nuclear division | biological process | A cell cycle process by which the cell nucleus divides as part of a meiotic cell cycle in the female germline. [GOC:dph, GOC:ems, GOC:mah, GOC:vw] |
| apoptotic chromosome condensation | biological process | The compaction of chromatin during apoptosis. [GOC:mah] |
| embryonic cleavage | biological process | The first few specialized divisions of an activated animal egg. [GOC:clt, ISBN:0070524300] |
| regulation of circadian rhythm | biological process | Any process that modulates the frequency, rate or extent of a circadian rhythm. A circadian rhythm is a biological process in an organism that recurs with a regularity of approximately 24 hours. [GOC:dph, GOC:jl, GOC:tb] |
| positive regulation of apoptotic process | biological process | Any process that activates or increases the frequency, rate or extent of cell death by apoptotic process. [GOC:jl, GOC:mtg_apoptosis] |
| positive regulation of single stranded viral RNA replication via double stranded DNA intermediate | biological process | Any process that activates or increases the frequency, rate or extent of retroviral genome replication. [GOC:go_curators] |
| positive regulation of transcription by RNA polymerase II | biological process | Any process that activates or increases the frequency, rate or extent of transcription from an RNA polymerase II promoter. [GOC:go_curators, GOC:txnOH] |
| rhythmic process | biological process | Any process pertinent to the generation and maintenance of rhythms in the physiology of an organism. [GOC:jid] |
| negative regulation of DNA duplex unwinding | biological process | Any process that stops, prevents or reduces the frequency, rate or extent of DNA duplex unwinding. [GO_REF:0000058, GOC:TermGenie, PMID:26503245] |
| resolution of meiotic recombination intermediates | biological process | The cleavage and rejoining of intermediates, such as Holliday junctions, formed during meiotic recombination to produce two intact molecules in which genetic material has been exchanged. [GOC:elh, PMID:11733053] |
| sister chromatid segregation | biological process | The cell cycle process in which sister chromatids are organized and then physically separated and apportioned to two or more sets. [GOC:ai, GOC:elh] |