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Items: 1 to 50 of 71

1.

Probing structural requirements for human topoisomerase I inhibition by a novel N1-Biphenyl fluoroquinolone.

Delgado JL, Lentz SRC, Kulkarni CA, Chheda PR, Held HA, Hiasa H, Kerns RJ.

Eur J Med Chem. 2019 Jun 15;172:109-130. doi: 10.1016/j.ejmech.2019.03.040. Epub 2019 Mar 20.

PMID:
30959322
2.

The C7-aminomethylpyrrolidine group rescues the activity of a thio-fluoroquinolone.

Lentz SRC, Chheda PR, Oppegard LM, Towle TR, Kerns RJ, Hiasa H.

Biochimie. 2019 May;160:24-27. doi: 10.1016/j.biochi.2019.02.002. Epub 2019 Feb 11.

PMID:
30763638
3.

Analysis of mutational patterns in quinolone resistance-determining regions of GyrA and ParC of clinical isolates.

Ostrer L, Khodursky RF, Johnson JR, Hiasa H, Khodursky A.

Int J Antimicrob Agents. 2019 Mar;53(3):318-324. doi: 10.1016/j.ijantimicag.2018.12.004. Epub 2018 Dec 21.

PMID:
30582984
4.

Novel N-1 substituted fluoroquinolones inhibit human topoisomerase I activity and exhibit anti-proliferative activity.

Oppegard LM, Delgado JL, Kulkarni CA, Towle TR, Hart DE, Williams BP, Lentz SRC, Norris BJ, Flory CM, Schumacher RJ, Murry DJ, Kerns RJ, Hiasa H.

Invest New Drugs. 2019 Apr;37(2):378-383. doi: 10.1007/s10637-018-0666-x. Epub 2018 Sep 10.

PMID:
30198058
5.

Design, synthesis, and evaluation of novel N-1 fluoroquinolone derivatives: Probing for binding contact with the active site tyrosine of gyrase.

Towle TR, Kulkarni CA, Oppegard LM, Williams BP, Picha TA, Hiasa H, Kerns RJ.

Bioorg Med Chem Lett. 2018 Jun 1;28(10):1903-1910. doi: 10.1016/j.bmcl.2018.03.085. Epub 2018 Mar 30.

6.

Topoisomerases as anticancer targets.

Delgado JL, Hsieh CM, Chan NL, Hiasa H.

Biochem J. 2018 Jan 23;475(2):373-398. doi: 10.1042/BCJ20160583. Review.

7.

DNA Topoisomerases as Targets for Antibacterial Agents.

Hiasa H.

Methods Mol Biol. 2018;1703:47-62. doi: 10.1007/978-1-4939-7459-7_3.

PMID:
29177732
8.

Suppression of gyrase-mediated resistance by C7 aryl fluoroquinolones.

Malik M, Mustaev A, Schwanz HA, Luan G, Shah N, Oppegard LM, de Souza EC, Hiasa H, Zhao X, Kerns RJ, Drlica K.

Nucleic Acids Res. 2016 Apr 20;44(7):3304-16. doi: 10.1093/nar/gkw161. Epub 2016 Mar 16.

9.

Fluoroquinolones stimulate the DNA cleavage activity of topoisomerase IV by promoting the binding of Mg(2+) to the second metal binding site.

Oppegard LM, Schwanz HA, Towle TR, Kerns RJ, Hiasa H.

Biochim Biophys Acta. 2016 Mar;1860(3):569-75. doi: 10.1016/j.bbagen.2015.12.019. Epub 2015 Dec 23.

10.

Synthesis and evaluation of N-alkyl-9-aminoacridines with antibacterial activity.

Benoit AR, Schiaffo C, Salomon CE, Goodell JR, Hiasa H, Ferguson DM.

Bioorg Med Chem Lett. 2014 Jul 15;24(14):3014-7. doi: 10.1016/j.bmcl.2014.05.037. Epub 2014 May 22.

PMID:
24908610
11.

Fluoroquinolone-gyrase-DNA complexes: two modes of drug binding.

Mustaev A, Malik M, Zhao X, Kurepina N, Luan G, Oppegard LM, Hiasa H, Marks KR, Kerns RJ, Berger JM, Drlica K.

J Biol Chem. 2014 May 2;289(18):12300-12. doi: 10.1074/jbc.M113.529164. Epub 2014 Feb 4.

12.

Flavone-based analogues inspired by the natural product simocyclinone D8 as DNA gyrase inhibitors.

Verghese J, Nguyen T, Oppegard LM, Seivert LM, Hiasa H, Ellis KC.

Bioorg Med Chem Lett. 2013 Nov 1;23(21):5874-7. doi: 10.1016/j.bmcl.2013.08.094. Epub 2013 Sep 5.

PMID:
24060488
13.

The antimicrobial lysine-peptoid hybrid LP5 inhibits DNA replication and induces the SOS response in Staphylococcus aureus.

Gottschalk S, Ifrah D, Lerche S, Gottlieb CT, Cohn MT, Hiasa H, Hansen PR, Gram L, Ingmer H, Thomsen LE.

BMC Microbiol. 2013 Aug 14;13:192. doi: 10.1186/1471-2180-13-192.

14.

Selective inhibition of bacterial and human topoisomerases by N-arylacyl O-sulfonated aminoglycoside derivatives.

Fenner AM, Oppegard LM, Hiasa H, Kerns RJ.

ACS Med Chem Lett. 2013 May 9;4(5):470-474.

15.

Solphenazines A-F, glycosylated phenazines from Streptomyces sp. strain DL-93.

Rusman Y, Oppegard LM, Hiasa H, Gelbmann C, Salomon CE.

J Nat Prod. 2013 Jan 25;76(1):91-6. doi: 10.1021/np3007606. Epub 2013 Jan 14.

PMID:
23317013
16.

Inhibition of human topoisomerases I and II by simocyclinone D8.

Oppegard LM, Nguyen T, Ellis KC, Hiasa H.

J Nat Prod. 2012 Aug 24;75(8):1485-9. doi: 10.1021/np300299y. Epub 2012 Aug 6.

PMID:
22867097
17.

Novel acridine-based agents with topoisomerase II inhibitor activity suppress mesothelioma cell proliferation and induce apoptosis.

Raza A, Jacobson BA, Benoit A, Patel MR, Jay-Dixon J, Hiasa H, Ferguson DM, Kratzke RA.

Invest New Drugs. 2012 Aug;30(4):1443-8. doi: 10.1007/s10637-011-9720-7. Epub 2011 Jul 26.

PMID:
21789510
18.

Synthesis and evaluation of 1-cyclopropyl-2-thioalkyl-8-methoxy fluoroquinolones.

Marks KR, Malik M, Mustaev A, Hiasa H, Drlica K, Kerns RJ.

Bioorg Med Chem Lett. 2011 Aug 1;21(15):4585-8. doi: 10.1016/j.bmcl.2011.05.112. Epub 2011 Jun 6.

19.

Comparison of in vitro activities of fluoroquinolone-like 2,4- and 1,3-diones.

Oppegard LM, Streck KR, Rosen JD, Schwanz HA, Drlica K, Kerns RJ, Hiasa H.

Antimicrob Agents Chemother. 2010 Jul;54(7):3011-4. doi: 10.1128/AAC.00190-10. Epub 2010 Apr 19.

20.

Synthesis and cancer cell cytotoxicity of substituted xanthenes.

Giri R, Goodell JR, Xing C, Benoit A, Kaur H, Hiasa H, Ferguson DM.

Bioorg Med Chem. 2010 Feb 15;18(4):1456-63. doi: 10.1016/j.bmc.2010.01.018. Epub 2010 Jan 11.

PMID:
20129790
21.

Quinolones: action and resistance updated.

Drlica K, Hiasa H, Kerns R, Malik M, Mustaev A, Zhao X.

Curr Top Med Chem. 2009;9(11):981-98. Review.

22.

On the role of topoisomerase I in mediating the cytotoxicity of 9-aminoacridine-based anticancer agents.

Gálvez-Peralta M, Hackbarth JS, Flatten KS, Kaufmann SH, Hiasa H, Xing C, Ferguson DM.

Bioorg Med Chem Lett. 2009 Aug 1;19(15):4459-62. doi: 10.1016/j.bmcl.2009.05.037. Epub 2009 May 18.

23.

In vivo and in vitro patterns of the activity of simocyclinone D8, an angucyclinone antibiotic from Streptomyces antibioticus.

Oppegard LM, Hamann BL, Streck KR, Ellis KC, Fiedler HP, Khodursky AB, Hiasa H.

Antimicrob Agents Chemother. 2009 May;53(5):2110-9. doi: 10.1128/AAC.01440-08. Epub 2009 Mar 9.

24.

Anti-proliferative effects of simocyclinone D8 (SD8), a novel catalytic inhibitor of topoisomerase II.

Sadiq AA, Patel MR, Jacobson BA, Escobedo M, Ellis K, Oppegard LM, Hiasa H, Kratzke RA.

Invest New Drugs. 2010 Feb;28(1):20-5. doi: 10.1007/s10637-008-9209-1. Epub 2009 Jan 10.

25.

Novel acridine-based compounds that exhibit an anti-pancreatic cancer activity are catalytic inhibitors of human topoisomerase II.

Oppegard LM, Ougolkov AV, Luchini DN, Schoon RA, Goodell JR, Kaur H, Billadeau DD, Ferguson DM, Hiasa H.

Eur J Pharmacol. 2009 Jan 14;602(2-3):223-9. doi: 10.1016/j.ejphar.2008.11.044. Epub 2008 Dec 3.

26.

Acridine-based agents with topoisomerase II activity inhibit pancreatic cancer cell proliferation and induce apoptosis.

Goodell JR, Ougolkov AV, Hiasa H, Kaur H, Remmel R, Billadeau DD, Ferguson DM.

J Med Chem. 2008 Jan 24;51(2):179-82. doi: 10.1021/jm701228e. Epub 2007 Dec 29.

PMID:
18163538
27.

Assessing sensitivity to antibacterial topoisomerase II inhibitors.

Morgan-Linnell SK, Hiasa H, Zechiedrich L, Nitiss JL.

Curr Protoc Pharmacol. 2007 Dec;Chapter 3:Unit3.13. doi: 10.1002/0471141755.ph0313s39.

29.
30.

Analysis of pleiotropic transcriptional profiles: a case study of DNA gyrase inhibition.

Jeong KS, Xie Y, Hiasa H, Khodursky AB.

PLoS Genet. 2006 Sep 29;2(9):e152. Epub 2006 Aug 2.

31.

Synthesis and evaluation of acridine- and acridone-based anti-herpes agents with topoisomerase activity.

Goodell JR, Madhok AA, Hiasa H, Ferguson DM.

Bioorg Med Chem. 2006 Aug 15;14(16):5467-80. Epub 2006 May 19.

PMID:
16713270
32.

Characterization of a unique type IA topoisomerase in Bacillus cereus.

Li Z, Hiasa H, DiGate R.

Mol Microbiol. 2006 Apr;60(1):140-51.

33.

The "GyrA-box" is required for the ability of DNA gyrase to wrap DNA and catalyze the supercoiling reaction.

Kramlinger VM, Hiasa H.

J Biol Chem. 2006 Feb 10;281(6):3738-42. Epub 2005 Dec 5.

34.
36.

The RuvAB branch migration complex can displace topoisomerase IV.quinolone.DNA ternary complexes.

Shea ME, Hiasa H.

J Biol Chem. 2003 Nov 28;278(48):48485-90. Epub 2003 Sep 17.

39.

A ParE-ParC fusion protein is a functional topoisomerase.

Lavasani LS, Hiasa H.

Biochemistry. 2001 Jul 24;40(29):8438-43.

PMID:
11456480
40.

Stenosis of the trachea caused by retrosternal ossification.

Mori M, Ikemune K, Hiasa H.

Ann Thorac Surg. 2001 Mar;71(3):1035-7.

PMID:
11269427
41.
43.
44.
46.
47.

The structure of supercoiled intermediates in DNA replication.

Peter BJ, Ullsperger C, Hiasa H, Marians KJ, Cozzarelli NR.

Cell. 1998 Sep 18;94(6):819-27.

48.

DNA gyrase and topoisomerase IV: biochemical activities, physiological roles during chromosome replication, and drug sensitivities.

Levine C, Hiasa H, Marians KJ.

Biochim Biophys Acta. 1998 Oct 1;1400(1-3):29-43. Review.

PMID:
9748489
49.
50.

The traE gene of plasmid RP4 encodes a homologue of Escherichia coli DNA topoisomerase III.

Li Z, Hiasa H, Kumar U, DiGate RJ.

J Biol Chem. 1997 Aug 1;272(31):19582-7.

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