New antibiotic molecules: Bypassing the membrane barrier of gram negative bacteria increases the activity of peptide deformylase inhibitors

PLoS ONE

Volumn 4, Issue 7, 2009, Pages

  Mamelli, Laurent ^a   Petit, Sylvain ^b   Chevalier, Jacqueline ^a   Giglione, Carmela ^b   Lieutaud, Aurélie ^a   Meinnel, Thierry ^b   Artaud, Isabelle ^b   Pagès, Jean Marie ^a  

^a Aix Marseille University   (France)

^b CNRS   (France)

Author keywords

[No Author keywords available]

Indexed keywords

2 (5 BROMO 1H INDOL 3 YL) N HYDROXYACETAMIDE; ACTINONIN; CEFTAZIDIME; CHLORAMPHENICOL; ERYTHROMYCIN; N (8 AMINO 1 CARBOXYOCTYL)ALANYLPROLINE; NORFLOXACIN; PEPTIDE DEFORMYLASE INHIBITOR; SESQUISULFUR MUSTARD; SIGMA; SM 2; TETRACYCLINE; UNCLASSIFIED DRUG; AMIDASE; ANTIINFECTIVE AGENT; ENZYME INHIBITOR; PEPTIDE DEFORMYLASE;

ANTIBACTERIAL ACTIVITY; ANTIBIOTIC SENSITIVITY; ARTICLE; BACTERIAL MEMBRANE; BACTERIAL STRAIN; BACTERIUM ISOLATE; CONTROLLED STUDY; ENTEROBACTER AEROGENES; ESCHERICHIA COLI; GRAM NEGATIVE BACTERIUM; KLEBSIELLA PNEUMONIAE; MEMBRANE PERMEABILITY; MINIMUM INHIBITORY CONCENTRATION; NONHUMAN; PERMEABILITY BARRIER; PSEUDOMONAS AERUGINOSA; STRUCTURE ACTIVITY RELATION; CELL MEMBRANE PERMEABILITY; DRUG ANTAGONISM; DRUG EFFECT;

BACTERIA (MICROORGANISMS); NEGIBACTERIA;

AMIDOHYDROLASES; ANTI-BACTERIAL AGENTS; CELL MEMBRANE PERMEABILITY; ENZYME INHIBITORS; GRAM-NEGATIVE BACTERIA;

EID: 68149091881     PISSN: None     EISSN: 19326203     Source Type: Journal    
DOI: 10.1371/journal.pone.0006443     Document Type: Article

References (45)

1. Chopra I, Schofield C, Everett M, O'Neill A, Miller K, et al. (2008) Treatment of health-care-associated infections caused by Gram-negative bacteria: a consensus statement. Lancet Infect Dis 8: 133-139.
2. Blot S, Depuydt P, Vandewoude K, De Bacquer D (2007) Measuring the impact of multidrug resistance in nosocomial infection. Curr Opin Infect Dis 20: 391-396.
3. Rice LB (2007) Emerging issues in the management of infections caused by multidrug-resistant gram-negative bacteria. Cleve Clin J Med 74 Suppl 4: S12-20.
4. Paterson DL (2008) Impact of antibiotic resistance in gram-negative bacilli on empirical and definitive antibiotic therapy. Clin Infect Dis 47 Suppl 1: S14-20.
5. in enterobacterial pathogens. Curr Drug Targets 9: 750-759.
6. Nikaido H (2003) Molecular basis of bacterial outer membrane permeability revisited. Microbiol Mol Biol Rev 67: 593-656.
7. Pagès JM, James CE, Winterhalter M (2008) The porin and the permeating antibiotic: a selective diffusion barrier in Gram-negative bacteria. Nat Rev Microbiol 6: 893-903.
8. Lomovskaya O, Bostian KA (2006) Pratical applications and feasibility of efflux pump inhibitors in the clinic-a vision for applied use. Biochem Pharmacol 71: 910-918.
9. Mahamoud A, Chevalier J, Alibert-Franco S, Kern WV, Pagès JM (2007) Antibiotic efflux pumps in Gram-negative bacteria: the inhibitor response strategy. J Antimicrob Chemother 59: 1223-1229.
10. Wright GD (2007) The antibiotic resistome: the nexus of chemical and genetic diversity. Nat Rev Microbiol 5: 175-186.
11. Falagas ME, Rafailidis PI (2008) Re-emergence of colistin in today's world of multidrug-resistant organisms: personal perspectives. Expert Opin Investig Drugs 17: 973-981.
12. O'Neill AJ (2008) New antibacterial agents for treating infections caused by multi-drug resistant Gram-negative bacteria. Expert Opin Investig Drugs 17: 297-302.
13. Boularot A, Giglione C, Artaud I, Meinnel T (2004) Structure-activity relationship analysis and therapeutic potential of peptide deformylase inhibitors. Curr Opin Investig Drugs 5: 809-822.
14. Jain R, Chen D, White RJ, Patel DV, Yuan Z (2005) Bacterial Peptide deformylase inhibitors: a new class of antibacterial agents. Curr Med Chem 12: 1607-1621.
15. Johnson KW, Lofland D, Moser HE (2005) PDF inhibitors: an emerging class of antibacterial drugs. Curr Drug Targets Infect Disord 5: 39-52.
16. Yu EW, Aires JR, McDermott G, Nikaido H (2005) A periplasmic drug-binding site of the AcrB multidrug efflux pump: a crystallographic and site-directed mutagenesis study. J Bacteriol 187: 6804-6815.
17. Chen DZ, Patel DV, Hackbarth CJ, Wang W, Dreyer G, et al. (2000) Actinonin, a naturally occurring antibacterial agent, is a potent deformylase inhibitor. Biochemistry 39: 1256-1262.
18. Boularot A, Giglione C, Petit S, Duroc Y, Alves de Sousa R, et al. (2007) Discovery and refinement of a new structural class of potent peptide deformylase inhibitors. J Med Chem 50: 10-20.
19. Petit S, Duroc Y, Larue V, Giglione C, Leon C, et al. (2009) Structure-activity relationship analysis of the peptide deformylase inhibitor 5-Bromo-1H-indole-3-acetohydroxamic Acid. Chem Med Chem 4: 261-275.
20. Dean CR, Narayan S, Richards J, Daigle DM, Esterow S, et al. (2007) Reduced susceptibility of Haemophilus influenzae to the peptide deformylase inhibitor LBM415 can result from target protein overexpression due to amplified chromosomal def gene copy number. Antimicrob Agents Chemother 51: 1004-1010.
21. Margolis PS, Hackbarth CJ, Young DC, Wang W, Chen D, et al. (2000) Peptide deformylase in Staphylococcus aureus: resistance to inhibition is mediated by mutations in the formyltransferase gene. Antimicrob Agents Chemother 44: 1825-1831.
22. Duroc Y, Giglione C, Meinnel T (2009) Mutations in three distinct loci cause resistance to peptide deformylase inhibitors in Bacillus subtilis. Antimicrob Agents Chemother 53: 1673-1678.
23. Dean CR, Narayan S, Daigle DM, Dzink-Fox JL, Puyang X, et al. (2005) Role of the AcrAB-TolC efflux pump in determining susceptibility of Haemophilus influenzae to the novel peptide deformylase inhibitor LBM415. Antimicrob Agents Chemother 49: 3129-3135.
24. Fritsche TR, Sader HS, Cleeland R, Jones RN (2005) Comparative antimicrobial characterization of LBM415 (NVP PDF-713), a new peptide deformylase inhibitor of clinical importance. Antimicrob Agents Chemother 49: 1468-1476.
25. Sahalan AZ, Dixon RA (2008) Role of the cell envelope in the antibacterial activities of polymyxin B and polymyxin B nonapeptide against Escherichia coli. Int J Antimicrob Agents 31: 224-227.
26. Landman D, Georgescu C, Martin DA, Quale J (2008) Polymyxins revisited. Clin Microbiol Rev 21: 449-465.
27. Cholet R, Chevalier J, Bryskier A, Pagès JM (2004) The AcrAB-TolC pump is involved in macrolide resistance but not in telithromycin efflux in Enterobacter aerogenes and Escherichia coli. Antimicrob Agents Chemother 48: 3621-3624.
28. Li XZ, Nikaido H (2004) Efflux-mediated drug resistance in bacteria. Drugs 64: 159-204.
29. Piddock LJ (2006) Multidrug-resistance efflux pumps - not just for resistance. Nat Rev Microbiol 4: 629-636.
30. Poole K (2005) Efflux-mediated antimicrobial resistance. J Antimicrob Chemother 56: 20-51.
31. Plesiat P, Nikaido H (1992) Outer membranes of gram-negative bacteria are permeable to steroid probes. Mol Microbiol 6: 1323-1333.
32. Li XZ, Nikaido H (2004) Efflux-mediated drug resistance in bacteria. Drugs 64: 159-204.
33. Fieulaine S, Juillan-Binard C, Serero A, Dardel F, Giglione C, et al. (2005) The crystal structure of mitochondrial (Type 1A) peptide deformylase provides clear guidelines for the design of inhibitors specific for the bacterial forms. J Biol Chem 280: 42315-4224.
34. Viveiros M, Jesus A, Brito M, Leandro C, Martins M, et al. (2005) Inducement and reversal of tetracycline resistance in Escherichia coli K-12 and expression of proton gradient-dependent multidrug efflux pump genes. Antimicrob Agents Chemother 49: 3578-3582.
35. Elkins CA, Mullis LB (2007) Substrate competition studies using whole-cell accumulation assays with the major tripartite multidrug efflux pumps of Escherichia coli. Antimicrob Agents Chemother 51: 923-929.
36. Su CC, Yu EW (2007) Ligand-transporter interaction in the AcrB multidrug efflux pump determined by fluorescence polarization assay. FEBS Lett 581: 4972-4976.
37. Yuan Z, White RJ (2006) The evolution of peptide deformylase as a target: contribution of biochemistry, genetics and genomics. Biochem Pharmacol 71: 1042-1047.
38. Murata T, Tseng W, Guina T, Miller SI, Nikaido H (2007) PhoPQ-mediated regulation produces a more robust permeability barrier in the outer membrane of Salmonella enterica serovar typhimurium. J Bacteriol 189: 7213-7222.
39. Pankuch GA, Lin G, Seifert H, Appelbaum PC (2008) Activity of meropenem with and without ciprofloxacin and colistin against Pseudomonas aeruginosa and Acinetobacter baumannii. Antimicrob Agents Chemother 52: 333-336.
40. Malléa M, Chevalier J, Bornet C, Eyraud A, Davin-Régli A, et al. (1998) Porin alteration and active efflux: two in vivo drug resistance strategies used by Enterobacter aerogenes. Microbiology 144: 3003-3009.
41. Pradel E, Pagès JM (2002) The AcrAB-TolC efflux pump contributes to multidrug resistance in the nosocomial pathogen Enterobacter aerogenes. Antimicrob Agents Chemother 46: 2640-2643.
42. Chevalier J, Pagès JM, Eyraud A, Malléa M (2000) Membrane permeability modifications are involved in antibiotic resistance in Klebsiella pneumoniae. Biochem Biophys Res Commun 274: 496-499.
43. Salmi C, Loncle C, Vidal N, Letourneux Y, Fantini J, et al. (2008) Squalamine: an appropriate strategy against the emergence of multidrug resistant gramnegative bacteria? PLoS ONE 3: e2765.
44. Chevalier J, Mulfinger C, Garnotel E, Nicolas P, Davin-Régli A, et al. (2008) Identification and evolution of drug efflux pump in clinical Enterobacter aerogenes strains isolated in 1995 and 2003. PLoS ONE 3: e3203.
45. Cavallo JD, Chardon H, Chidiac C, Courvalin P, Dabernat H, et al. (2008) Comité de l'Antibiogramme de la Société Francaise de Microbiologie [http://www.sfm.asso.fr/publi/general.php?pa=1].