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Items: 1 to 50 of 52

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.

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
4.

Effect of a mitochondrial-targeted coenzyme Q analog on pancreatic β-cell function and energetics in high fat fed obese mice.

Imai Y, Fink BD, Promes JA, Kulkarni CA, Kerns RJ, Sivitz WI.

Pharmacol Res Perspect. 2018 Jun;6(3):e00393. doi: 10.1002/prp2.393. Epub 2018 May 18.

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.

Interactions between Quinolones and Bacillus anthracis Gyrase and the Basis of Drug Resistance.

Ashley RE, Lindsey RH Jr, McPherson SA, Turnbough CL Jr, Kerns RJ, Osheroff N.

Biochemistry. 2017 Aug 15;56(32):4191-4200. doi: 10.1021/acs.biochem.7b00203. Epub 2017 Aug 1.

7.

Metabolic effects of a mitochondrial-targeted coenzyme Q analog in high fat fed obese mice.

Fink BD, Guo DF, Kulkarni CA, Rahmouni K, Kerns RJ, Sivitz WI.

Pharmacol Res Perspect. 2017 Mar 10;5(2):e00301. doi: 10.1002/prp2.301. eCollection 2017 Apr.

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.

N-Arylacyl O-sulfonated aminoglycosides as novel inhibitors of human neutrophil elastase, cathepsin G and proteinase 3.

Craciun I, Fenner AM, Kerns RJ.

Glycobiology. 2016 Jul;26(7):701-709. doi: 10.1093/glycob/cww011. Epub 2016 Feb 5.

10.

Crystal structure and stability of gyrase-fluoroquinolone cleaved complexes from Mycobacterium tuberculosis.

Blower TR, Williamson BH, Kerns RJ, Berger JM.

Proc Natl Acad Sci U S A. 2016 Feb 16;113(7):1706-13. doi: 10.1073/pnas.1525047113. Epub 2016 Jan 20.

11.

Fluoroquinolone interactions with Mycobacterium tuberculosis gyrase: Enhancing drug activity against wild-type and resistant gyrase.

Aldred KJ, Blower TR, Kerns RJ, Berger JM, Osheroff N.

Proc Natl Acad Sci U S A. 2016 Feb 16;113(7):E839-46. doi: 10.1073/pnas.1525055113. Epub 2016 Jan 20.

12.

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.

13.

Activity of quinolone CP-115,955 against bacterial and human type II topoisomerases is mediated by different interactions.

Aldred KJ, Schwanz HA, Li G, Williamson BH, McPherson SA, Turnbough CL Jr, Kerns RJ, Osheroff N.

Biochemistry. 2015 Feb 10;54(5):1278-86. doi: 10.1021/bi501073v. Epub 2015 Jan 23.

14.

Bypassing fluoroquinolone resistance with quinazolinediones: studies of drug-gyrase-DNA complexes having implications for drug design.

Drlica K, Mustaev A, Towle TR, Luan G, Kerns RJ, Berger JM.

ACS Chem Biol. 2014 Dec 19;9(12):2895-904. doi: 10.1021/cb500629k. Epub 2014 Nov 4.

15.

A mitochondrial-targeted coenzyme q analog prevents weight gain and ameliorates hepatic dysfunction in high-fat-fed mice.

Fink BD, Herlein JA, Guo DF, Kulkarni C, Weidemann BJ, Yu L, Grobe JL, Rahmouni K, Kerns RJ, Sivitz WI.

J Pharmacol Exp Ther. 2014 Dec;351(3):699-708. doi: 10.1124/jpet.114.219329. Epub 2014 Oct 9.

16.

Bacillus anthracis GrlAV96A topoisomerase IV, a quinolone resistance mutation that does not affect the water-metal ion bridge.

Aldred KJ, Breland EJ, McPherson SA, Turnbough CL Jr, Kerns RJ, Osheroff N.

Antimicrob Agents Chemother. 2014 Dec;58(12):7182-7. doi: 10.1128/AAC.03734-14. Epub 2014 Sep 22.

17.

Role of the water-metal ion bridge in mediating interactions between quinolones and Escherichia coli topoisomerase IV.

Aldred KJ, Breland EJ, Vlčková V, Strub MP, Neuman KC, Kerns RJ, Osheroff N.

Biochemistry. 2014 Sep 2;53(34):5558-67. doi: 10.1021/bi500682e. Epub 2014 Aug 21.

18.

Lethal synergy involving bicyclomycin: an approach for reviving old antibiotics.

Malik M, Li L, Zhao X, Kerns RJ, Berger JM, Drlica K.

J Antimicrob Chemother. 2014 Dec;69(12):3227-35. doi: 10.1093/jac/dku285. Epub 2014 Jul 31.

19.

Mechanism of quinolone action and resistance.

Aldred KJ, Kerns RJ, Osheroff N.

Biochemistry. 2014 Mar 18;53(10):1565-74. doi: 10.1021/bi5000564. Epub 2014 Mar 7. Review.

20.

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.

21.

Overcoming target-mediated quinolone resistance in topoisomerase IV by introducing metal-ion-independent drug-enzyme interactions.

Aldred KJ, Schwanz HA, Li G, McPherson SA, Turnbough CL Jr, Kerns RJ, Osheroff N.

ACS Chem Biol. 2013 Dec 20;8(12):2660-8. doi: 10.1021/cb400592n. Epub 2013 Sep 30.

22.

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.

23.

Topoisomerase IV-quinolone interactions are mediated through a water-metal ion bridge: mechanistic basis of quinolone resistance.

Aldred KJ, McPherson SA, Turnbough CL Jr, Kerns RJ, Osheroff N.

Nucleic Acids Res. 2013 Apr;41(8):4628-39. doi: 10.1093/nar/gkt124. Epub 2013 Mar 4.

24.

Chemical probes of a trisubstituted pyrrole to identify its protein target(s) in Plasmodium sporozoites.

Towle T, Chang I, Kerns RJ, Bhanot P.

Bioorg Med Chem Lett. 2013 Mar 15;23(6):1874-7. doi: 10.1016/j.bmcl.2013.01.010. Epub 2013 Jan 11. Erratum in: Bioorg Med Chem Lett. 2013 May 1;23(9):2812. Chang, Isabel [corrected to Chang, Isabell].

25.

Bioenergetic effects of mitochondrial-targeted coenzyme Q analogs in endothelial cells.

Fink BD, Herlein JA, Yorek MA, Fenner AM, Kerns RJ, Sivitz WI.

J Pharmacol Exp Ther. 2012 Sep;342(3):709-19. doi: 10.1124/jpet.112.195586. Epub 2012 Jun 1.

26.

Induction of mycobacterial resistance to quinolone class antimicrobials.

Malik M, Chavda K, Zhao X, Shah N, Hussain S, Kurepina N, Kreiswirth BN, Kerns RJ, Drlica K.

Antimicrob Agents Chemother. 2012 Jul;56(7):3879-87. doi: 10.1128/AAC.00474-12. Epub 2012 May 7.

27.

Drug interactions with Bacillus anthracis topoisomerase IV: biochemical basis for quinolone action and resistance.

Aldred KJ, McPherson SA, Wang P, Kerns RJ, Graves DE, Turnbough CL Jr, Osheroff N.

Biochemistry. 2012 Jan 10;51(1):370-81. doi: 10.1021/bi2013905. Epub 2011 Dec 16.

28.

Synthesis, separation, and characterization of amphiphilic sulfated oligosaccharides enabled by reversed-phase ion pairing LC and LC-MS methods.

Fenner AM, Kerns RJ.

Carbohydr Res. 2011 Dec 13;346(17):2792-800. doi: 10.1016/j.carres.2011.09.020. Epub 2011 Sep 24.

29.

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.

30.

Fluoroquinolone and quinazolinedione activities against wild-type and gyrase mutant strains of Mycobacterium smegmatis.

Malik M, Marks KR, Mustaev A, Zhao X, Chavda K, Kerns RJ, Drlica K.

Antimicrob Agents Chemother. 2011 May;55(5):2335-43. doi: 10.1128/AAC.00033-11. Epub 2011 Mar 7.

31.

Effect of N-1/c-8 ring fusion and C-7 ring structure on fluoroquinolone lethality.

Malik M, Marks KR, Schwanz HA, German N, Drlica K, Kerns RJ.

Antimicrob Agents Chemother. 2010 Dec;54(12):5214-21. doi: 10.1128/AAC.01054-10. Epub 2010 Sep 20.

32.

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.

33.
34.

Novel approach for comparing the abilities of quinolones to restrict the emergence of resistant mutants during quinolone exposure.

Malik M, Hoatam G, Chavda K, Kerns RJ, Drlica K.

Antimicrob Agents Chemother. 2010 Jan;54(1):149-56. doi: 10.1128/AAC.01035-09. Epub 2009 Oct 5.

35.

Use of gyrase resistance mutants to guide selection of 8-methoxy-quinazoline-2,4-diones.

German N, Malik M, Rosen JD, Drlica K, Kerns RJ.

Antimicrob Agents Chemother. 2008 Nov;52(11):3915-21. doi: 10.1128/AAC.00330-08. Epub 2008 Sep 2.

36.

Synthesis and evaluation of fluoroquinolone derivatives as substrate-based inhibitors of bacterial efflux pumps.

German N, Wei P, Kaatz GW, Kerns RJ.

Eur J Med Chem. 2008 Nov;43(11):2453-63. doi: 10.1016/j.ejmech.2008.01.042. Epub 2008 Feb 8.

PMID:
18358571
37.

Synthesis and evaluation of PSSRI-based inhibitors of Staphylococcus aureus multidrug efflux pumps.

German N, Kaatz GW, Kerns RJ.

Bioorg Med Chem Lett. 2008 Feb 15;18(4):1368-73. doi: 10.1016/j.bmcl.2008.01.014. Epub 2008 Jan 9.

PMID:
18242086
38.

Variability in the carbazole assay for N-desulfonated/N-acylated heparin derivatives.

Hattan CM, Kerns RJ.

Carbohydr Res. 2007 Dec 10;342(17):2664-9. Epub 2007 Aug 23.

PMID:
17850773
39.

Quinolone-mediated bacterial death.

Drlica K, Malik M, Kerns RJ, Zhao X.

Antimicrob Agents Chemother. 2008 Feb;52(2):385-92. Epub 2007 Aug 27. Review. No abstract available.

40.
41.

Semi-synthetic heparin derivatives: chemical modifications of heparin beyond chain length, sulfate substitution pattern and N-sulfo/N-acetyl groups.

Fernández C, Hattan CM, Kerns RJ.

Carbohydr Res. 2006 Jul 24;341(10):1253-65. Epub 2006 May 18. Review.

PMID:
16712822
42.

Susceptibility studies of piperazinyl-cross-linked fluoroquinolone dimers against test strains of Gram-positive and Gram-negative bacteria.

Kerns RJ, Rybak MJ, Cheung CM.

Diagn Microbiol Infect Dis. 2006 Apr;54(4):305-10. Epub 2006 Feb 8.

PMID:
16466892
44.
45.

Ciprofloxacin dimers target gyrase in Streptococcus pneumoniae.

Gould KA, Pan XS, Kerns RJ, Fisher LM.

Antimicrob Agents Chemother. 2004 Jun;48(6):2108-15.

46.
47.

Structural features of piperazinyl-linked ciprofloxacin dimers required for activity against drug-resistant strains of Staphylococcus aureus.

Kerns RJ, Rybak MJ, Kaatz GW, Vaka F, Cha R, Grucz RG, Diwadkar VU.

Bioorg Med Chem Lett. 2003 Jul 7;13(13):2109-12.

PMID:
12798315
48.

Piperazinyl-linked fluoroquinolone dimers possessing potent antibacterial activity against drug-resistant strains of Staphylococcus aureus.

Kerns RJ, Rybak MJ, Kaatz GW, Vaka F, Cha R, Grucz RG, Diwadkar VU, Ward TD.

Bioorg Med Chem Lett. 2003 May 19;13(10):1745-9.

PMID:
12729656
49.

Oxazolidinone protected 2-amino-2-deoxy-D-glucose derivatives as versatile intermediates in stereoselective oligosaccharide synthesis and the formation of alpha-linked glycosides.

Benakli K, Zha C, Kerns RJ.

J Am Chem Soc. 2001 Sep 26;123(38):9461-2. No abstract available. Erratum in: J Am Chem Soc 2001 Dec 26;123(51):12933.

PMID:
11562237
50.

Enzymatic preparation of heparin disaccharides as building blocks in glycosaminoglycan synthesis.

Kim YS, Thanawiroon C, Bazin HG, Kerns RJ, Linhard RJ.

Prep Biochem Biotechnol. 2001 May;31(2):113-24.

PMID:
11426699

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