Olga Lomovskaya

Summary

Publications

  1. ncbi request reprint Peptidomimetics of efflux pump inhibitors potentiate the activity of levofloxacin in Pseudomonas aeruginosa
    Thomas E Renau
    Essential Therapeutics, Inc, 850Maude Avenue, Mountain View, CA 94043, USA
    Bioorg Med Chem Lett 12:763-6. 2002
  2. ncbi request reprint It takes three to tango
    Olga Lomovskaya
    Nat Biotechnol 20:1210-2. 2002
  3. pmc Use of an efflux pump inhibitor to determine the prevalence of efflux pump-mediated fluoroquinolone resistance and multidrug resistance in Pseudomonas aeruginosa
    Jane Kriengkauykiat
    University of Southern California, School of Pharmacy, 1985 Zonal Ave, Los Angeles, CA 90089, USA
    Antimicrob Agents Chemother 49:565-70. 2005
  4. pmc Pharmacodynamics of levofloxacin against Pseudomonas aeruginosa with reduced susceptibility due to different efflux pumps: do elevated MICs always predict reduced in vivo efficacy?
    David C Griffith
    Mpex Pharmaceuticals, Inc 3030 Bunker Hill St, Suite 200, San Diego, CA 92109, USA
    Antimicrob Agents Chemother 50:1628-32. 2006
  5. pmc Vacuuming the periplasm
    Olga Lomovskaya
    Mpex Pharmaceuticals, Inc, 5500 Campanile Dr, San Diego, CA 92182, USA
    J Bacteriol 187:1879-83. 2005
  6. ncbi request reprint Waltzing transporters and 'the dance macabre' between humans and bacteria
    Olga Lomovskaya
    Mpex Pharmaceuticals, Inc 3030 Bunker Hill Street, Suite 200 San Diego, California 92109, USA
    Nat Rev Drug Discov 6:56-65. 2007
  7. ncbi request reprint Quinazolinone fungal efflux pump inhibitors. Part 2: In vitro structure-activity relationships of (N-methyl-piperazinyl)-containing derivatives
    William J Watkins
    Essential Therapeutics, Inc, 850 Maude Ave, Mountain View, CA 94043, USA
    Bioorg Med Chem Lett 14:5133-7. 2004
  8. ncbi request reprint Quinazolinone fungal efflux pump inhibitors. Part 3: (N-methyl)piperazine variants and pharmacokinetic optimization
    William J Watkins
    Essential Therapeutics, Inc, 850 Maude Ave, Mountain View, CA 94043, USA
    Bioorg Med Chem Lett 17:2802-6. 2007
  9. doi request reprint Effect of oxygen limitation on the in vitro activity of levofloxacin and other antibiotics administered by the aerosol route against Pseudomonas aeruginosa from cystic fibrosis patients
    Paula King
    Mpex Pharmaceuticals, Inc, San Diego, CA 92121 1309, USA
    Diagn Microbiol Infect Dis 66:181-6. 2010
  10. pmc In vitro pharmacodynamics of levofloxacin and other aerosolized antibiotics under multiple conditions relevant to chronic pulmonary infection in cystic fibrosis
    Paula King
    Mpex Pharmaceuticals, Inc, 11535 Sorrento Valley Road, San Diego, CA 92121 1309, USA
    Antimicrob Agents Chemother 54:143-8. 2010

Research Grants

  1. Rational Discovery of Efflux Pump Inhibitors
    Olga Lomovskaya; Fiscal Year: 2005

Detail Information

Publications18

  1. ncbi request reprint Peptidomimetics of efflux pump inhibitors potentiate the activity of levofloxacin in Pseudomonas aeruginosa
    Thomas E Renau
    Essential Therapeutics, Inc, 850Maude Avenue, Mountain View, CA 94043, USA
    Bioorg Med Chem Lett 12:763-6. 2002
    ..A number of the new analogues were as active or more active than the lead, demonstrating that a peptide backbone is not essential for activity...
  2. ncbi request reprint It takes three to tango
    Olga Lomovskaya
    Nat Biotechnol 20:1210-2. 2002
  3. pmc Use of an efflux pump inhibitor to determine the prevalence of efflux pump-mediated fluoroquinolone resistance and multidrug resistance in Pseudomonas aeruginosa
    Jane Kriengkauykiat
    University of Southern California, School of Pharmacy, 1985 Zonal Ave, Los Angeles, CA 90089, USA
    Antimicrob Agents Chemother 49:565-70. 2005
    ..aeruginosa. Our data support the fact that increased fluoroquinolone usage can negatively impact susceptibility of P. aeruginosa to multiple classes of antipseudomonal agents...
  4. pmc Pharmacodynamics of levofloxacin against Pseudomonas aeruginosa with reduced susceptibility due to different efflux pumps: do elevated MICs always predict reduced in vivo efficacy?
    David C Griffith
    Mpex Pharmaceuticals, Inc 3030 Bunker Hill St, Suite 200, San Diego, CA 92109, USA
    Antimicrob Agents Chemother 50:1628-32. 2006
    ..These data show that while the MexEF-OprN efflux pump can provide P. aeruginosa resistance to levofloxacin in vitro, it appears to be less efficient in providing resistance to levofloxacin in animal models of infection...
  5. pmc Vacuuming the periplasm
    Olga Lomovskaya
    Mpex Pharmaceuticals, Inc, 5500 Campanile Dr, San Diego, CA 92182, USA
    J Bacteriol 187:1879-83. 2005
  6. ncbi request reprint Waltzing transporters and 'the dance macabre' between humans and bacteria
    Olga Lomovskaya
    Mpex Pharmaceuticals, Inc 3030 Bunker Hill Street, Suite 200 San Diego, California 92109, USA
    Nat Rev Drug Discov 6:56-65. 2007
    ..Here, we review recent advances in the field and describe various approaches used in combating efflux-mediated resistance...
  7. ncbi request reprint Quinazolinone fungal efflux pump inhibitors. Part 2: In vitro structure-activity relationships of (N-methyl-piperazinyl)-containing derivatives
    William J Watkins
    Essential Therapeutics, Inc, 850 Maude Ave, Mountain View, CA 94043, USA
    Bioorg Med Chem Lett 14:5133-7. 2004
    ....
  8. ncbi request reprint Quinazolinone fungal efflux pump inhibitors. Part 3: (N-methyl)piperazine variants and pharmacokinetic optimization
    William J Watkins
    Essential Therapeutics, Inc, 850 Maude Ave, Mountain View, CA 94043, USA
    Bioorg Med Chem Lett 17:2802-6. 2007
    ..albicans and C. glabrata over-expressing ABC-type efflux pumps are systematically explored. Rat protein binding and pharmacokinetics of selected analogues are reported...
  9. doi request reprint Effect of oxygen limitation on the in vitro activity of levofloxacin and other antibiotics administered by the aerosol route against Pseudomonas aeruginosa from cystic fibrosis patients
    Paula King
    Mpex Pharmaceuticals, Inc, San Diego, CA 92121 1309, USA
    Diagn Microbiol Infect Dis 66:181-6. 2010
    ..In contrast, levofloxacin maintains activity against P. aeruginosa under anaerobic or hypoxic conditions similar to those found in CF microaerophilic environments...
  10. pmc In vitro pharmacodynamics of levofloxacin and other aerosolized antibiotics under multiple conditions relevant to chronic pulmonary infection in cystic fibrosis
    Paula King
    Mpex Pharmaceuticals, Inc, 11535 Sorrento Valley Road, San Diego, CA 92121 1309, USA
    Antimicrob Agents Chemother 54:143-8. 2010
    ..The results of the study show that the high concentrations of levofloxacin readily achievable in the lung following aerosol delivery may be useful for the management of pulmonary infections in patients with cystic fibrosis...
  11. doi request reprint Levofloxacin reduces inflammatory cytokine levels in human bronchial epithelia cells: implications for aerosol MP-376 (levofloxacin solution for inhalation) treatment of chronic pulmonary infections
    Ruslan Tsivkovskii
    Mpex Pharmaceuticals, San Diego, CA, USA
    FEMS Immunol Med Microbiol 61:141-6. 2011
    ....
  12. ncbi request reprint Conformationally-restricted analogues of efflux pump inhibitors that potentiate the activity of levofloxacin in Pseudomonas aeruginosa
    Thomas E Renau
    Essential Therapeutics, Inc, 850Maude Avenue, Mountain View, CA 94043, USA
    Bioorg Med Chem Lett 13:2755-8. 2003
    ....
  13. ncbi request reprint Practical applications and feasibility of efflux pump inhibitors in the clinic--a vision for applied use
    Olga Lomovskaya
    Mpex Pharmaceuticals Inc, 3030 Bunker Hill Street, San Diego, CA 92109, USA
    Biochem Pharmacol 71:910-8. 2006
    ..It is also apparent that some changes in regulatory decision-making regarding resistance would be very helpful in order to facilitate approval of agents aiming to reverse resistance and prevent its further development...
  14. ncbi request reprint Quinazolinone-based fungal efflux pump inhibitors. Part 1: Discovery of an (N-methylpiperazine)-containing derivative with activity in clinically relevant Candida spp
    Rémy C Lemoine
    Essential Therapeutics, Inc, 850 Maude Ave, Mountain View, CA 94043, USA
    Bioorg Med Chem Lett 14:5127-31. 2004
    ..albicans is described. Attempts to improve the aqueous solubility of screening hits led to the discovery of an analog with greatly improved physical properties and activity against clinically-relevant Candida spp...
  15. ncbi request reprint On the mechanism of substrate specificity by resistance nodulation division (RND)-type multidrug resistance pumps: the large periplasmic loops of MexD from Pseudomonas aeruginosa are involved in substrate recognition
    Weimin Mao
    Essential Therapeutics Inc, 850 Maude Ave, Mountain View, CA 94043, USA
    Mol Microbiol 46:889-901. 2002
    ..These results are consistent with the hypothesis that, in the case of RND transporters, the LPLs are directly implicated in substrate recognition and contain multiple sites of interaction for various structurally diverse compounds...
  16. pmc MexXY-OprM efflux pump is necessary for a adaptive resistance of Pseudomonas aeruginosa to aminoglycosides
    Didier Hocquet
    Laboratoire de Bacteriologie, Hopital Jean Minjoz, Besancon, France
    Antimicrob Agents Chemother 47:1371-5. 2003
    ..Altogether, these results indicate that the resistance process requires the rapid production of MexXY and the interaction of these proteins with the constitutively produced component OprM...
  17. pmc Drug-induced conformational changes in multidrug efflux transporter AcrB from Haemophilus influenzae
    Vishakha Dastidar
    Department of Chemistry and Biochemistry, 620 Parrington Oval, Norman, OK 73019, USA
    J Bacteriol 189:5550-8. 2007
    ..We report that the reactivity of specific cysteines with FM is affected by the presence of some but not all substrates. Our results suggest that substrates induce conformational changes in AcrB(HI)...
  18. pmc Multidrug pump inhibitors uncover remarkable activity of plant antimicrobials
    George Tegos
    Department of Biology, Northeastern University, Boston, Massachusetts 02115, USA
    Antimicrob Agents Chemother 46:3133-41. 2002
    ..These findings also suggest that plant antimicrobials might be developed into effective, broad-spectrum antibiotics in combination with inhibitors of MDRs...

Research Grants1

  1. Rational Discovery of Efflux Pump Inhibitors
    Olga Lomovskaya; Fiscal Year: 2005
    ..By the end of Phase I, several distinct chemotypes will have been identified. Phase II studies will further optimize these compounds to develop a drug that will improve, preserve and expand the clinical effectiveness of AG antibiotics. ..