Mode of action of the microbial metabolite GE23077, a novel potent and selective inhibitor of bacterial RNA polymerase

European Journal of Biochemistry

Volumn 271, Issue 15, 2004, Pages 3146-3154

  Sarubbi, Edoardo ^a,b   Monti, Federica ^a,c   Corti, Emiliana ^a   Miele, Anna ^a,d   Selva, Enrico ^a  

^a Vicuron Pharmaceuticals   (Italy)

^b SANOFI   (France)

^c Arpida Ltd   (Switzerland)

^d Aventis Pharma   (Italy)

Author keywords

Antibiotic; Cell permeabilization; Natural product; Rifampicin; Transcription initiation

Indexed keywords

ANTIBIOTIC AGENT; BACTERIAL RNA; ENZYME INHIBITOR; GE 23077; LIPIARMYCIN; RIFAMPICIN; RNA POLYMERASE; STREPTOLYDIGIN; UNCLASSIFIED DRUG;

ANTIBIOTIC RESISTANCE; ANTIMICROBIAL ACTIVITY; ARTICLE; BACILLUS SUBTILIS; BACTERIAL CELL; CELL PERMEABILIZATION; COMPLEX FORMATION; CONTROLLED STUDY; DRUG MECHANISM; DRUG STRUCTURE; ENZYME INHIBITION; ESCHERICHIA COLI; MACROMOLECULE; MICROBIAL METABOLISM; NONHUMAN; PRIORITY JOURNAL; RNA SYNTHESIS; RNA TRANSLATION; TRANSCRIPTION INITIATION;

ACTINOMYCETALES; AMINOGLYCOSIDES; DNA, BACTERIAL; DNA-DIRECTED RNA POLYMERASES; DRUG RESISTANCE; ESCHERICHIA COLI; INHIBITORY CONCENTRATION 50; MOLECULAR STRUCTURE; PEPTIDES, CYCLIC; RIFAMYCINS; SUBSTRATE SPECIFICITY; TRANSCRIPTION, GENETIC;

ACTINOMADURA; ACTINOMADURA SP.; BACILLUS SUBTILIS; BACTERIA (MICROORGANISMS); ESCHERICHIA COLI; EUKARYOTA; NEGIBACTERIA; POSIBACTERIA; TRITICUM AESTIVUM;

EID: 3242881098     PISSN: 00142956     EISSN: None     Source Type: Journal    
DOI: 10.1111/j.1432-1033.2004.04244.x     Document Type: Article

References (35)

1. Borukhov, S. & Nudler, E. (2003) RNA polymerase holoenzyme: structure, function and biological implications. Curr. Opin. Microbiol. 6, 93-100.
2. Burgess, R.R. & Anthony, L. (2001) How sigma docks to RNA polymerase and what sigma does. Curr. Opin. Microbiol. 4, 126-131.
3. Borukhov, S. & Severinov, K. (2002) Role of the RNA polymerase sigma subunit in transcription initiation. Res. Microbiol. 153, 557-562.
4. Zhang, G., Campbell, E.A., Minakhin, L., Richter, C., Severinov, K. & Darst, S.A. (1999) Crystal structure of Thermus aquaticus core RNA polymerase at 3.3 Å resolution. Cell 98, 811-824.
5. Murakami, K.S., Masuda, S. & Darst, S.A. (2002) Structural basis of transcription initiation: RNA polymerase holoenzyme at 4 Å resolution. Science 296, 1280-1284.
6. Vassylyev, D.G., Sekine, S., Laptenko, O., Lee, J., Vassylyeva, M.N., Borukhov, S. & Yokoyama, S. (2002) Crystal structure of a bacterial RNA polymerase holoenzyme at 2.6 Å resolution. Nature 417, 712-719.
7. Murakami, K.S., Masuda, S., Campbell, E.A., Muzzin, O. & Darst, S.A. (2002) Structural basis of transcription initiation: an RNA polymerase holoenzyme-DNA complex. Science 296, 1285-1290.
8. 70), promoters and the kinetics of the steps of transcription initiation. In: Escherichia coli and Salmonella typhimurium: Cellular and Molecular Biology. (Neidhart, F.C., ed.), pp. 792-820. ASM Press, Washington, DC.
9. Sensi, P. (1983) History of the development of rifampin. Rev. Infect. Dis. 3, 402-406.
10. Parenti, F. & Lancini, G. (1997) Rifamycins. In Antibiotics and Chemotherapy (O'Grady, F., Lambert, H.P., Finch, R.G. & Greenwood, D., eds), 7th edn, pp. 453-459. Churchill Livingstone, New York, NY.
11. Sonenshein, A.L. & Alexander, H.B. (1979) Initiation of transcription in vitro inhibited by lipiarmycin. J. Mol. Biol. 127, 55-72.
12. McClure, W.R. (1980) On the mechanism of streptolydigin inhibition of Escherichia coli RNA polymerase. J. Biol. Chem. 255, 1610-1616.
13. Reichenbach, H. & Hofle, G. (1999) Myxobacteria as producers of secondary metabolites. In Drug Discovery from Nature (Grabley, S. & Thiericke, R., eds), pp. 149-178. Springer-Verlag, Berlin, Germany.
14. O'Neill, A., Oliva, B., Storey, C., Hoyle, A., Fishwick. C. & Chopra, I. (2000) RNA polymerase inhibitors with activity against rifampicin-resistant mutants of Staphylococcus aureus. Antimicrob. Agents Chemother. 44, 3163-3166.
15. Artsimovitch, I., Chu, C., Lynch, A.S. & Landick, R. (2003) A new class of bacterial RNA polymerase inhibitors affects nucleotide addition. Science 302, 650-654.
16. McClure, W.R. & Cech, C.L. (1978) On the mechanism of rifampicin inhibition of RNA synthesis. J. Biol. Chem. 253, 8949-8956.
17. Campbell, E.A., Korzheva, N., Mustaev, A., Murakami, K., Nair, S., Goldfarb, A. & Darst, S.A. (2001) Structural mechanism for rifampicin inhibition of bacterial RNA polymerase. Cell 104, 901-912.
18. Yang, X. & Price, C.W. (1995) Streptolydigin resistance can be conferred by alterations to either the beta or beta′ subunits of Bacillus subtilis RNA polymerase. J. Biol. Chem. 270, 23930-23933.
19. Ciciliato, I., Corti, E., Sarubbi, E., Stefanelli, S., Gastaldo, L., Montanini, N., Kurz, M., Losi, D., Marinelli, F. & Selva, E. (2004) Antibiotic GE23077, a new inhibitor of bacterial RNA polymerase. I. Taxonomy, isolation and characterization. J. Antibiot. 57, 210-217.
20. Plevani, P., Albertini, A.M., Galizzi, A., Adamoli, A., Mastromei, G., Riva, S. & Cassani, G. (1977) RNA polymerase from Bacillus subtilis: isolation of core and holo enzyme by DNA-cellulose chromatography. Nucleic Acids Res. 4, 603-623.
21. Jin, D.J. & Gross, C.A. (1988) Mapping and sequencing of mutations in the Escherichia coli rpoB gene that lead to rifampicin resistance. J. Mol. Biol. 202, 45-58.
22. Hager, D.A., Jin, D.J. & Burgess, R.R. (1990) Use of mono Q high resolution ion exchange chromatography to obtain highly pure and active Escherichia coli RNA polymerase. Biochemistry 29, 7890-7894.
23. Somma, S., Pirali, G., White, R. & Parenti, F. (1975) Lipiarmycin, a new antibiotic from Actinoplanes. III. Mechanism of action. J. Antibiot. 28, 543-549.
24. Nikaido, H. & Vaara, M. (1987) Outer membrane. In Escherichia coli and Salmonella typhimurium: Cellular and Molecular Biology (Neidhart, F.C., ed.), pp. 7-22. ASM Press, Washington, DC.
25. Leive, L. (1965) Actinomycin sensitivity in Escherichia coli produced by EDTA. Biochem. Biophys. Res. Commun. 18, 13-17.
26. van de Klundert, J.A.M., van der Meide, P.H., van de Putte, P. & Bosch, L. (1978) Mutants of Escherichia coli altered in both genes coding for the elongation factor Tu. Proc. Natl Acad. Sci. USA 75, 4470-4473.
27. Zeef, L.A.H., Bosch, L., Anborgh, P.H., Catin, R., Parmeggiani, A. & Hilgenfeld, R. (1994) Pulvomycin-resistant mutants of E. coli elongation factor Tu. EMBO J. 13, 5113-5120.
28. Gros, F., Gallant, J., Weisberg, R. & Cashel, M. (1967) Decryptification of RNA polymerase in whole cells of Escherichia coli. J. Mol. Biol. 25, 555.
29. Staudenbauer, W.L. (1975) Novobiocin - a specific inhibitor of semiconservative DNA replication in permeabilized Escherichia coli cells. J. Mol. Biol. 96, 201-205.
30. Hall, C.C., Bertasso, A., Watkins, J.D. & Georgopapadakou, N.H. (1992) Screening assays for protein synthesis inhibitors. J. Antibiot. 45, 1697-1699.
31. Ovchinnikov, Y.A., Monastyrskaya, G.S., Guriev, S.O., Kalinina, N.F., Sverdlov, E.D., Gragerov, A.I., Bass, I.A., Kiver, I.F., Moiseyeva, E.P., Igumnov, V.N., Mindlin, S.Z., Nikiforov, V.G. & Khesin, R.B. (1983) RNA polymerase rifampicin resistance mutations in Escherichia coli: sequence changes and dominance. Mol. Gen. Genet. 190, 344-348.
32. Mekler, V., Kortkhonjia, E., Mukhopadhyay, J., Knight, J., Revyakin, A., Kapanidis, A.N., Niu, W., Ebright, Y.W., Levy, R. & Ebright, R.H. (2002) Structural organization of bacterial RNA polymerase holoenzyme and the RNA polymerase-promoter open complex. Cell 108, 599-614.
33. Barrett, C.T. & Barrett, J.F. (2003) Antibacterials: are the new entries enough to deal with the emerging resistance problems? Curr. Opin. Biotechnol. 14, 621-626.
34. Enright, M.C. & McKenzy, H. (1997) Moraxella (Branhamella) catarrhalis: clinical and molecular aspects of a rediscovered pathogen. J. Med. Microbiol. 46, 360-371.
35. McGregor, K., Chang, B.J., Mee, B.J. & Riley, T.V. (1998) Moraxella catarrhalis: clinical significance, antimicrobial susceptibility and BRO β-lactamases. Eur. J. Microbiol. Infect. Dis. 17, 219-234.