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Review

Patent developments in antimycobacterial small-molecule therapeutics

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Pages 131-140 | Published online: 22 Apr 2005

Bibliography

  • CORBETT EL, WATT CJ, WALKER N et al.: The growing burden of tuberculosis: global trends and interactions with the HIV epidemic. Arch. Intern. Med. (2003) 163:1009–1021.
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  • HICKEY MJ, ARAIN TM, SHAWAR RM et al.: Luciferase in vivo expression technology: use of recombinant mycobacterial reporter strains to evaluate antimycobacterial activity in mice. Antimicrob. Agents Chemother. (1996) 32:400–407.
  • •First publication on Luciferase in vivo expression (LIVE) using an enhanced luciferase-expressing mycobacterial strain. This report also contains references on the use of recombinant mycobacteria and reporter mycobacteriophages expressing firefly or bacterial luciferase to measure drug susceptibility in vitro.
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  • LOUNIS N, ROSCIGNO G: In vitro and in vivo activities of rifamycin derivatives against mycobacterial Infections. Curr. Pharm. Design (2004) 10:3229–3238.
  • •Summary of the in vitro and in vivo activities of new rifamycin derivatives.
  • ANDRIES K, VERHASSELT P, GUILLEMONT J et al.: Science (2004), doi:10.1126/science.1106753 (2004).
  • ••Comprehensive multi-disciplinary study ofR- 19207910, a diarylquinoline that shows promise as new TB drug candidate.
  • HUTCHINSON DK: Recent advances in oxazolidinone antibacterial agent research. Expert Opin. Ther. Patents (2004) 14:1309–1328.
  • •Comprehensive review on the oxazolidinone patent literature from 2000 to 2003, covering issues such as toxicity, spectrum of antimicrobial activity and resistance.
  • HARTH G, HORWITZ Mk An inhibitor of exported Mycobacterium tuberculosis glutamine synthetase selectively blocks the growth of pathogenic mycobacteria in axenic culture and in human monocytes: extracellular proteins as potential novel drug targets. J. Exp. Med. (1999) 189:1425–1435.
  • ••First publication to suggest the therapeuticpotential of targeting extracellular enzymes exported by pathogenic (myco)bacteria and to link the extracellular presence of Glutamine synthase to the virulence-associated cell wall component poly-L-glutamate/glutamine.
  • HARTH G, ZAMECNIK PC, TANG J-Y, TABATADZA D, HORWITZ MA: Treatment of Mycobacterium tuberculosis with antisense oligonucleotides to glutamine synthetase mRNA inhibits glutamine synthetase activity, formation of the poly-I-glutamate/glutamine cell wall structure, and bacterial replication. Proc. Natl Acad. Sci. USA (2000) 97:418–423.
  • ••The first report to demonstrate thefeasibility of using antisense technology to combat M tuberculosis. The fact the phosphorothioate oligodeoxynudeotides can penetrate the cell wall barrier looks promising with regard to their use for target validation.
  • GILL HS, PFLUEGL GM, EISENBERG D: Multicopy crystallographic refinement of a relaxed glutamine synthetase from Mycobacterium tuberculosis highlights flexible loops in the enzymatic mechanism and its regulation. Biochemistry (2002) 41:9863–9872.
  • GILL HS, EISENBERG D: The crystal structure of phosphinothrecin in the active site of glutamine synthetase illuminates the mechanism of enzyme inhibition. Biochemistry (2001) 40:1903–1912.
  • ROOSENBERG JM, LIN Y-M, MILLER MJ: Studies and syntheses of siderophores, microbial iron chelators, and analogs as potential drug delivery agents. Curr. Med. Chem. (2000) 7:159–197.
  • •Review of the most representative siderophores as well as of the application of synthetic variants as species-selective active drug transport (the 'Trojan Horse' approach).
  • DEIDDA D, LAMPIS G, FIORAVANTI R et al.: Bactericidal activities of the pyrrole derivative BM212 against multidrug-resistant and intramacrophagic Mycobacterium tuberculosis strains. Antimicrob. Agents Chemother. (1998) 42:3035–3037.
  • •First report on the antimycobacterial activity of pyrroles.
  • COLE ST, BROSCH R, PARKHILL J et al. Deciphering the biology of Mycobacterium tuberculosis from the complete genome sequence. Nature (1998) 293:537–544.
  • ••Landmark publication on the cloning ofthe complete genome of M. tuberculosis: a potentially invaluable source of information that might permit both the identification of new drug targets and novel methods to shorten treatment.
  • DUNCAN K: Identification and validation of novel drug targets in tuberculosis. Curr. Pharm . Design (2004) 10:3185–3194.
  • ••Excellent review on M tuberculosis targets,grouped according to the pathways or functions.
  • BARRY CE: Preclinical candidates and targets for tuberculosis therapy. Curr. Opin. Invest. Drugs (2001) 2:198–201.
  • CLEMENS DL, HORWITZ MA: Characterization of the Mycobacterium tuberculosis phagosome and evidence that phagosomal maturation is inhibited. J. Exp. Med. (1995) 181:257–270.
  • MITCHINSON DA, COATES, ARM: Predictive in vitro models of the sterilizing activity of anti-tuberculosis drugs. Curr. Pharm. Design (2004) 10:3285–3295.
  • •Review on the problems of in vitro assays to measure the potential activity against persisters, i.e., slow-growing cavitary bacilli.
  • BARRY CE, BOSHOFF HIM, DOWD CS: Prospects for clinical introduction of nitroimidazole antibiotics for the treatment of tuberculosis. Curr. Pharm. Design (2004) 10:3239–3262.
  • •Comprehensive review on the controversial nitroimidazoles as potential antimycobacterial agents.

Websites

  • http://www.who.int/topics/tuberculosis/en/ WHO Tuberculosis.
  • •Contains links to interesting WHO information resources concerning TB.
  • http://www.who.int/gtb/publicationsktgnp/P DF /2003.313. pdf Treatment of tuberculosis: guidelines for national programmes, 3rd ed.

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