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Toward discovering new anti-cancer agents targeting topoisomerase IIα: a facile screening strategy adaptable to high throughput platform.

Lin YS, Huang WC, Chen MS, Hsieh TS.

PLoS One. 2014 May 8;9(5):e97008. doi: 10.1371/journal.pone.0097008. eCollection 2014.


Novel DNA topoisomerase IIα inhibitors from combined ligand- and structure-based virtual screening.

Drwal MN, Marinello J, Manzo SG, Wakelin LP, Capranico G, Griffith R.

PLoS One. 2014 Dec 9;9(12):e114904. doi: 10.1371/journal.pone.0114904. eCollection 2014.


Topoisomerase IIα, rather than IIβ, is a promising target in development of anti-cancer drugs.

Chen W, Qiu J, Shen YM.

Drug Discov Ther. 2012 Oct;6(5):230-7. Review.


NK314, a topoisomerase II inhibitor that specifically targets the alpha isoform.

Toyoda E, Kagaya S, Cowell IG, Kurosawa A, Kamoshita K, Nishikawa K, Iiizumi S, Koyama H, Austin CA, Adachi N.

J Biol Chem. 2008 Aug 29;283(35):23711-20. doi: 10.1074/jbc.M803936200. Epub 2008 Jul 2.


A high-throughput fluorescence anisotropy-based assay for human topoisomerase II β-catalyzed ATP-dependent supercoiled DNA relaxation.

Shapiro AB, Austin CA.

Anal Biochem. 2014 Mar 1;448:23-9. doi: 10.1016/j.ab.2013.11.029. Epub 2013 Dec 3.


The E3 ubiquitin-ligase Bmi1/Ring1A controls the proteasomal degradation of Top2alpha cleavage complex - a potentially new drug target.

Alchanati I, Teicher C, Cohen G, Shemesh V, Barr HM, Nakache P, Ben-Avraham D, Idelevich A, Angel I, Livnah N, Tuvia S, Reiss Y, Taglicht D, Erez O.

PLoS One. 2009 Dec 1;4(12):e8104. doi: 10.1371/journal.pone.0008104.


Contributions of the D-Ring to the activity of etoposide against human topoisomerase IIα: potential interactions with DNA in the ternary enzyme--drug--DNA complex.

Pitts SL, Jablonksy MJ, Duca M, Dauzonne D, Monneret C, Arimondo PB, Anklin C, Graves DE, Osheroff N.

Biochemistry. 2011 Jun 7;50(22):5058-66. doi: 10.1021/bi200531q. Epub 2011 May 13.


Synthesis, biological evaluation and modeling studies of terphenyl topoisomerase IIα inhibitors as anticancer agents.

Qiu J, Zhao B, Zhong W, Shen Y, Lin H.

Eur J Med Chem. 2015 Apr 13;94:427-35. doi: 10.1016/j.ejmech.2015.03.010. Epub 2015 Mar 6.


CS1 is a novel topoisomerase IIα inhibitor with favorable drug resistance profiles.

Shen Y, Chen W, Zhao B, Hao H, Li Z, Lu C, Shen Y.

Biochem Biophys Res Commun. 2014 Oct 24;453(3):302-8. doi: 10.1016/j.bbrc.2014.09.042. Epub 2014 Sep 19.


Synthesis and biological evaluation of C1-O-substituted-3-(3-butylamino-2-hydroxy-propoxy)-xanthen-9-one as topoisomerase IIα catalytic inhibitors.

Park S, Hong E, Kwak SY, Jun KY, Lee ES, Kwon Y, Na Y.

Eur J Med Chem. 2016 Nov 10;123:211-25. doi: 10.1016/j.ejmech.2016.07.046. Epub 2016 Jul 22.


Examination of the Impact of Copper(II) α-(N)-Heterocyclic Thiosemicarbazone Complexes on DNA Topoisomerase IIα.

Wilson JT, Jiang X, McGill BC, Lisic EC, Deweese JE.

Chem Res Toxicol. 2016 Apr 18;29(4):649-58. doi: 10.1021/acs.chemrestox.5b00471. Epub 2016 Mar 23.


Inhibition of human DNA topoisomerase IIα by two novel ellipticine derivatives.

Vann KR, Ergün Y, Zencir S, Oncuoglu S, Osheroff N, Topcu Z.

Bioorg Med Chem Lett. 2016 Apr 1;26(7):1809-12. doi: 10.1016/j.bmcl.2016.02.034. Epub 2016 Feb 15.


Synergistic interaction between histone deacetylase and topoisomerase II inhibitors is mediated through topoisomerase IIbeta.

Marchion DC, Bicaku E, Turner JG, Daud AI, Sullivan DM, Munster PN.

Clin Cancer Res. 2005 Dec 1;11(23):8467-75.


Interactions between the etoposide derivative F14512 and human type II topoisomerases: implications for the C4 spermine moiety in promoting enzyme-mediated DNA cleavage.

Gentry AC, Pitts SL, Jablonsky MJ, Bailly C, Graves DE, Osheroff N.

Biochemistry. 2011 Apr 19;50(15):3240-9. doi: 10.1021/bi200094z. Epub 2011 Mar 28.


3-(3-Butylamino-2-hydroxy-propoxy)-1-hydroxy-xanthen-9-one acts as a topoisomerase IIα catalytic inhibitor with low DNA damage.

Park SE, Chang IH, Jun KY, Lee E, Lee ES, Na Y, Kwon Y.

Eur J Med Chem. 2013 Nov;69:139-45. doi: 10.1016/j.ejmech.2013.07.048. Epub 2013 Aug 11.


HU-331 is a catalytic inhibitor of topoisomerase IIα.

Regal KM, Mercer SL, Deweese JE.

Chem Res Toxicol. 2014 Dec 15;27(12):2044-51. doi: 10.1021/tx500245m. Epub 2014 Dec 3.


Catalytic core of human topoisomerase IIα: insights into enzyme-DNA interactions and drug mechanism.

Lindsey RH Jr, Pendleton M, Ashley RE, Mercer SL, Deweese JE, Osheroff N.

Biochemistry. 2014 Oct 21;53(41):6595-602. doi: 10.1021/bi5010816. Epub 2014 Oct 10.


Synthesis, crystal structure and antiproliferative activity of Cu(II) nalidixic acid-DACH conjugate: comparative in vitro DNA/RNA binding profile, cleavage activity and molecular docking studies.

Arjmand F, Yousuf I, Hadda Tb, Toupet L.

Eur J Med Chem. 2014 Jun 23;81:76-88. doi: 10.1016/j.ejmech.2014.04.080. Epub 2014 May 2.


Chinese hamster ovary cells resistant to the topoisomerase II catalytic inhibitor ICRF-159: a Tyr49Phe mutation confers high-level resistance to bisdioxopiperazines.

Sehested M, Wessel I, Jensen LH, Holm B, Oliveri RS, Kenwrick S, Creighton AM, Nitiss JL, Jensen PB.

Cancer Res. 1998 Apr 1;58(7):1460-8.


Hydroxylated 2,4-diphenyl indenopyridine derivatives as a selective non-intercalative topoisomerase IIα catalytic inhibitor.

Kadayat TM, Park C, Jun KY, Thapa Magar TB, Bist G, Yoo HY, Kwon Y, Lee ES.

Eur J Med Chem. 2015 Jan 27;90:302-14. doi: 10.1016/j.ejmech.2014.11.046. Epub 2014 Nov 24.


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