MmpL3 is the cellular target of the antitubercular pyrrole derivative BM212

Antimicrobial Agents and Chemotherapy

Volumn 56, Issue 1, 2012, Pages 324-331

  La Rosa, Valentina ^a   Poce, Giovanna ^b,c   Canseco, Julio Ortiz ^a   Buroni, Silvia ^a   Pasca, Maria Rosalia ^a   Biava, Mariangela ^c   Raju, Ravikiran M ^b   Porretta, Giulio Cesare ^c   Alfonso, Salvatore ^c   Battilocchio, Claudio ^c   Javid, Babak ^b   Sorrentino, Flavia ^b   Ioerger, Thomas R ^e   Sacchettini, James C ^e   Manetti, Fabrizio ^d   Botta, Maurizio ^d   De Logu, Alessandro ^f   Rubin, Eric J ^b   De Rossi, Edda ^a  

^a UNIVERSITY OF PAVIA   (Italy)

^b HARVARD SCHOOL OF PUBLIC HEALTH   (United States)

^c SAPIENZA UNIVERSITY OF ROME   (Italy)

^d UNIVERSITY OF SIENA   (Italy)

^e TEXAS A AND M UNIVERSITY   (United States)

^f UNIVERSITY OF CAGLIARI   (Italy)

Author keywords

[No Author keywords available]

Indexed keywords

1,5 BIS(4 CHLOROPHENYL) 2 METHYL 3 (4 METHYL 1 PIPERAZINYLMETHYL)PYRROLE; BCG VACCINE; CARBONYL CYANIDE CHLOROPHENYLHYDRAZONE; PYRROLE DERIVATIVE; RESERPINE; UNCLASSIFIED DRUG; VERAPAMIL;

ANTIBIOTIC RESISTANCE; ARTICLE; BACTERIAL GENE; BACTERIAL STRAIN; BACTERIUM ISOLATE; DRUG STRUCTURE; DRUG SYNTHESIS; GENE MUTATION; GENE SEQUENCE; MMPL3 GENE; MYCOBACTERIUM BOVIS; MYCOBACTERIUM SMEGMATIS; MYCOBACTERIUM TUBERCULOSIS; NONHUMAN; PRIORITY JOURNAL;

ANIMALS; ANTITUBERCULAR AGENTS; CARBON RADIOISOTOPES; CARBONYL CYANIDE M-CHLOROPHENYL HYDRAZONE; CATTLE; DNA MUTATIONAL ANALYSIS; DRUG RESISTANCE, MULTIPLE, BACTERIAL; GENOME, BACTERIAL; GENOMIC LIBRARY; HUMANS; MEMBRANE TRANSPORT PROTEINS; MICROBIAL SENSITIVITY TESTS; MUTATION; MYCOBACTERIUM BOVIS; MYCOBACTERIUM INFECTIONS, NONTUBERCULOUS; MYCOBACTERIUM SMEGMATIS; MYCOBACTERIUM TUBERCULOSIS; PIPERAZINES; PYRROLES; RESERPINE; VERAPAMIL;

EID: 84455173193     PISSN: 00664804     EISSN: 10986596     Source Type: Journal    
DOI: 10.1128/AAC.05270-11     Document Type: Article

References (23)

1. Ainsa JA, Martin C, Cabeza M, De la Cruz F, Mendiola MV. 1996. Construction of a family of Mycobacterium/Escherichia coli shuttle vectors derived from pAL5000 and pACYC184: their use for cloning an antibiotic- resistance gene from Mycobacterium fortuitum. Gene 176:23-26. (Pubitemid 26375747)
2. Banerjee A, et al. 1994. inhA, a gene encoding a target for isoniazid and ethionamide in Mycobacterium tuberculosis. Science 263:227-230. (Pubitemid 24067929)
3. Biava M. 2002. BM212 and its derivatives as a new class of antimycobacterial active agents. Curr. Med. Chem. 9:1859-1869. (Pubitemid 35230255)
4. Biava M, et al. 2011. Developing pyrrole-derived antimycobacterial agents: a rational lead optimization approach. ChemMedChem 6:593-598.
5. Chan ED, Iseman MD. 2008. Multidrug-resistant and extensively drug-resistant tuberculosis: a review. Curr. Opin. Infect. Dis. 21:587-595.
6. Cole ST, et al. 1998. Deciphering the biology of Mycobacterium tuberculosis from the complete genome sequence. Nature 393:537-544. (Pubitemid 28319235)
7. Deidda D, et al. 1998. Bactericidal activities of the pyrrole derivative BM 212 against multidrug-resistant and intramacrophagic Mycobacterium tuberculosis strains. Antimicrob. Agents Chemother. 42:3035-3037. (Pubitemid 28501251)
8. Domenech P, Reed MB, Barry CE III. 2005. Contribution of the Mycobacterium tuberculosis MmpL protein family to virulence and drug resistance. Infect. Immun. 73:3492-3501. (Pubitemid 40745893)
9. Donnelly-Wu MK, Jacobs WR, Jr, Hatfull GF. 1993. Superinfection immunity of mycobacteriophage L5: applications for genetic transformation of mycobacteria. Mol. Microbiol. 7:407-417. (Pubitemid 23051205)
10. Jacobs WR, Jr, et al. 1991. Genetic systems for mycobacteria. Methods Enzymol. 204:537-555.
11. Jones DT, Taylor WR, Thornton JM. 1994. A model recognition approach to the prediction of all-helical membrane protein structure and topology. Biochemistry 33:3038-3049. (Pubitemid 24103366)
12. Lenaerts AJ, Degroote MA, Orme IM. 2008. Preclinical testing of new drugs for tuberculosis: current challenges. Trends Microbiol. 16:48-54.
13. Lienhardt C, Vernon A, Raviglione MC. 2010. New drugs and new regimens for the treatment of tuberculosis: review of the drug development pipeline and implications for national programmes. Curr. Opin. Pulm. Med. 16:186-193.
14. Mdluli K, et al. 1998. Inhibition of a Mycobacterium tuberculosis β-ketoacyl ACP synthase by isoniazid. Science 280:1607-1610. (Pubitemid 28277706)
15. Payne DJ, Gwynn MN, Holmes DJ, Pompliano DL. 2007. Drugs for bad bugs: confronting the challenges of antibacterial discovery. Nat. Rev. Drug Discov. 6:29-40. (Pubitemid 46020284)
16. Poole K. 2007. Efflux pumps as antimicrobial resistance mechanisms. Ann. Med. 39:162-176. (Pubitemid 46676478)
17. Ramaswamy S, Musser JM. 1998. Molecular genetic basis of antimicrobial agent resistance in Mycobacterium tuberculosis: 1998 update. Tuber. Lung Dis. 79:3-29. (Pubitemid 29050434)
18. Riccardi G, Pasca MR, Buroni S. 2009. Mycobacterium tuberculosis: drug resistance and future perspectives. Future Microbiol. 4:597-614.
19. Rozwarski D, Grant G, Barton D, Jacobs WR, Jr, Sacchettini JC. 1998. Modification of the NADH of the isoniazid target (InhA) from Mycobacterium tuberculosis. Science 279:98-102. (Pubitemid 28079164)
20. Sambrook J, Russell DW. 2001. Molecular cloning: a laboratory manual, 3rd ed. Cold Spring Harbor Laboratory Press, Cold Spring Harbor, NY.
21. Szybalski W, Bryson V. 1952. Genetic studies on microbial cross resistance to toxic agents. 1. Cross resistance of Escherichia coli to 15 antibiotics. J. Bacteriol. 64:489-499.
22. Tullius MV, et al. 2011. Discovery and characterization of a unique mycobacterial heme acquisition system. Proc. Natl. Acad. Sci. U. S. A. 12:5051-5056.
23. Wyatt PG, Gilbert IH, Read KD, Fairlamb AH. 2011. Target validation: linking target and chemical properties to desired product profile. Curr. Top. Med. Chem. 11:1275-1283.