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Items: 19


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.


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.


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.


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.


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.


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.


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.


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.


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.


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.


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.


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.


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.


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.


Cis-acting elements stimulating kinetoplastid guide RNA-directed editing.

Oppegard LM, Hillestad M, McCarthy RT, Pai RD, Connell GJ.

J Biol Chem. 2003 Dec 19;278(51):51167-75. Epub 2003 Oct 6.


Direct visualisation of RNA editing within a Leishmania tarentolae mitochondrial extract.

Oppegard LM, Connell GJ.

Int J Parasitol. 2002 Jun 15;32(7):859-66.


A mRNA determinant of gRNA-directed kinetoplastid editing.

Kabb AL, Oppegard LM, McKenzie BA, Connell GJ.

Nucleic Acids Res. 2001 Jun 15;29(12):2575-80.


Activation of guide RNA-directed editing of a cytochrome b mRNA.

Oppegard LM, Kabb AL, Connell GJ.

J Biol Chem. 2000 Oct 27;275(43):33911-9.

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