Discovery of Potent Inhibitors of Dihydroneopterin Aldolase Using CrystaLEAD High-Throughput X-ray Crystallographic Screening and Structure-Directed Lead Optimization

Journal of Medicinal Chemistry

Volumn 47, Issue 7, 2004, Pages 1709-1718

  Sanders, William J ^a   Nienaber, Vicki L ^a   Lerner, Claude G ^a   McCall, J Owen ^a   Merrick, Sean M ^a   Swanson, Susan J ^a   Harlan, John E ^a   Stoll, Vincent S ^a   Stamper, Geoffrey F ^a   Betz, Stephen F ^a   Condroski, Kevin R ^a   Meadows, Robert P ^a   Severin, Jean M ^a   Walter, Karl A ^a   Magdalinos, Peter ^a   Jakob, Clarissa G ^a   Wagner, Rolf ^a   Beutel, Bruce A ^a  

^a ABBOTT LABORATORIES   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

7,8 DIHYDRONEOPTERIN ALDOLASE; NEOPTERIN; SULFAMETHOXAZOLE; TETRAHYDROFOLIC ACID; TRIMETHOPRIM; UNCLASSIFIED DRUG;

ARTICLE; CRYSTAL STRUCTURE; DRUG INHIBITION; DRUG TARGETING; ENZYME ACTIVE SITE; ENZYME ASSAY; ENZYME BINDING; ENZYME INHIBITION; HIGH THROUGHPUT SCREENING; IC 50; X RAY CRYSTALLOGRAPHY;

ALDEHYDE-LYASES; BENZOIC ACIDS; BINDING SITES; CRYSTALLOGRAPHY, X-RAY; DATABASES, FACTUAL; ENZYME INHIBITORS; GUANINE; MODELS, MOLECULAR; MOLECULAR STRUCTURE; NEOPTERIN; PURINES; PYRIMIDINES; STRUCTURE-ACTIVITY RELATIONSHIP; TRIAZOLES;

EID: 12144288664     PISSN: 00222623     EISSN: None     Source Type: Journal    
DOI: 10.1021/jm030497y     Document Type: Article

References (43)

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3. Chopra, I.; Hesse, L.; O'Neill, A. J. Exploiting current understanding of antibiotic action for discovery of new drugs. Soc. Appl. Microbiol. Symp. Ser. 2002, 31, 4S-15S. Daw, M. A.; Drah, A. M. Antibiotic resistance: Prospects for the new millennium. J. Chemother. 2001, 13, 587-594. Bax, R.; Mullan, N.; Verhoef, J. The millennium bugs-the need for and development of new antibacterials. Int. J. Antimicrob. Agents 2000, 16, 51-59. Domagala, J. M.; Sanchez, J. P. New approaches and agents to overcome bacterial resistance. Annu. Rep. Med. Chem. 1997, 32, 111-120.
4. Chopra, I.; Hesse, L.; O'Neill, A. J. Exploiting current understanding of antibiotic action for discovery of new drugs. Soc. Appl. Microbiol. Symp. Ser. 2002, 31, 4S-15S. Daw, M. A.; Drah, A. M. Antibiotic resistance: Prospects for the new millennium. J. Chemother. 2001, 13, 587-594. Bax, R.; Mullan, N.; Verhoef, J. The millennium bugs-the need for and development of new antibacterials. Int. J. Antimicrob. Agents 2000, 16, 51-59. Domagala, J. M.; Sanchez, J. P. New approaches and agents to overcome bacterial resistance. Annu. Rep. Med. Chem. 1997, 32, 111-120.
5. Lerner, C. G.; Beutel, B. A. Antibacterial drug discovery in the post-genomics era. Curr. Drug Targets: Infect. Disord. 2002, 2, 109-119. Chan, P. F.; Macarron, R.; Payne, D. J.; Zalacain, M.; Holmes, D. J. Novel antibacterials: a genomics approach to drug discovery. Curr. Drug Targets: Infect. Disord. 2002, 2, 291-308. Volker, C.; Brown, J. R. Bioinformatics and the discovery of novel anti-microbial targets. Curr. Drug Targets: Infect. Disord. 2002, 2, 279-290. Chalker, A. F.; Lunsford, R. D. Rational identification of new antibacterial drug targets that are essential for viability using a genomics-based approach. Pharmacol. Ther. 2002, 95, 1-20. Isaacson, R. E. Genomics and the prospects for the discovery of new targets for antibacterial and antifungal agents. Curr. Pharm. Des. 2002, 8, 1091-1098. McDevitt, D.; Rosenberg, M. Exploiting genomics to discover new antibiotics. Trends Microbiol. 2001, 9, 611-617. Payne, D. J.; Holmes, D. J.; Rosenberg, M. Delivering novel targets and antibiotics from genomics. Curr. Opin. Invest. Drugs 2001, 2, 1028-1034. Holmes, D. J.; Throup, J. P.; Wallis, N. G.; Burnham, M. K. R.; Zalacain, M.; Biswas, S.; Chalker, A. F.; Ingraham, K. A.; Marra, A.; Bryant, A.; Woodnutt, G.; Warren, P. V.; Brown, J. R.; Rosenberg, M. The contribution of genomics to the discovery of new antibiotics. Focus Biotechnol. 2001, 1, 23-31. Lehoux, D. E.; Levesque, R. C. Detection of genes essential in specific niches by signature-tagged mutagenesis. Curr. Opin. Biotechnol. 2000, 11, 434-439. Reich, K. A. The search for essential genes. Res. Microbiol. 2000, 151, 319-324. Gray, C. P.; Keck, W. Bacterial targets and antibiotics. Genome-based drug discovery. Cell. Mol. Life Sci. 1999, 56, 779-787. Chopra, I. Prospects for antisense agents in the therapy of bacterial infections. Expert Opin. Invest. Drugs 1999, 8, 1203-1208. Kolstoe, A.-B. Dynamic bacterial genome organization. Mol. Microbiol. 1997, 24, 241-248. Miklos, G. L. G.; Rubin, G. M. The role of the genome project in determining gene function: insights from model organisms. Cell 1996, 86, 521-529.
6. Lerner, C. G.; Beutel, B. A. Antibacterial drug discovery in the post-genomics era. Curr. Drug Targets: Infect. Disord. 2002, 2, 109-119. Chan, P. F.; Macarron, R.; Payne, D. J.; Zalacain, M.; Holmes, D. J. Novel antibacterials: a genomics approach to drug discovery. Curr. Drug Targets: Infect. Disord. 2002, 2, 291-308. Volker, C.; Brown, J. R. Bioinformatics and the discovery of novel anti-microbial targets. Curr. Drug Targets: Infect. Disord. 2002, 2, 279-290. Chalker, A. F.; Lunsford, R. D. Rational identification of new antibacterial drug targets that are essential for viability using a genomics-based approach. Pharmacol. Ther. 2002, 95, 1-20. Isaacson, R. E. Genomics and the prospects for the discovery of new targets for antibacterial and antifungal agents. Curr. Pharm. Des. 2002, 8, 1091-1098. McDevitt, D.; Rosenberg, M. Exploiting genomics to discover new antibiotics. Trends Microbiol. 2001, 9, 611-617. Payne, D. J.; Holmes, D. J.; Rosenberg, M. Delivering novel targets and antibiotics from genomics. Curr. Opin. Invest. Drugs 2001, 2, 1028-1034. Holmes, D. J.; Throup, J. P.; Wallis, N. G.; Burnham, M. K. R.; Zalacain, M.; Biswas, S.; Chalker, A. F.; Ingraham, K. A.; Marra, A.; Bryant, A.; Woodnutt, G.; Warren, P. V.; Brown, J. R.; Rosenberg, M. The contribution of genomics to the discovery of new antibiotics. Focus Biotechnol. 2001, 1, 23-31. Lehoux, D. E.; Levesque, R. C. Detection of genes essential in specific niches by signature-tagged mutagenesis. Curr. Opin. Biotechnol. 2000, 11, 434-439. Reich, K. A. The search for essential genes. Res. Microbiol. 2000, 151, 319-324. Gray, C. P.; Keck, W. Bacterial targets and antibiotics. Genome-based drug discovery. Cell. Mol. Life Sci. 1999, 56, 779-787. Chopra, I. Prospects for antisense agents in the therapy of bacterial infections. Expert Opin. Invest. Drugs 1999, 8, 1203-1208. Kolstoe, A.-B. Dynamic bacterial genome organization. Mol. Microbiol. 1997, 24, 241-248. Miklos, G. L. G.; Rubin, G. M. The role of the genome project in determining gene function: insights from model organisms. Cell 1996, 86, 521-529.
7. Lerner, C. G.; Beutel, B. A. Antibacterial drug discovery in the post-genomics era. Curr. Drug Targets: Infect. Disord. 2002, 2, 109-119. Chan, P. F.; Macarron, R.; Payne, D. J.; Zalacain, M.; Holmes, D. J. Novel antibacterials: a genomics approach to drug discovery. Curr. Drug Targets: Infect. Disord. 2002, 2, 291-308. Volker, C.; Brown, J. R. Bioinformatics and the discovery of novel anti-microbial targets. Curr. Drug Targets: Infect. Disord. 2002, 2, 279-290. Chalker, A. F.; Lunsford, R. D. Rational identification of new antibacterial drug targets that are essential for viability using a genomics-based approach. Pharmacol. Ther. 2002, 95, 1-20. Isaacson, R. E. Genomics and the prospects for the discovery of new targets for antibacterial and antifungal agents. Curr. Pharm. Des. 2002, 8, 1091-1098. McDevitt, D.; Rosenberg, M. Exploiting genomics to discover new antibiotics. Trends Microbiol. 2001, 9, 611-617. Payne, D. J.; Holmes, D. J.; Rosenberg, M. Delivering novel targets and antibiotics from genomics. Curr. Opin. Invest. Drugs 2001, 2, 1028-1034. Holmes, D. J.; Throup, J. P.; Wallis, N. G.; Burnham, M. K. R.; Zalacain, M.; Biswas, S.; Chalker, A. F.; Ingraham, K. A.; Marra, A.; Bryant, A.; Woodnutt, G.; Warren, P. V.; Brown, J. R.; Rosenberg, M. The contribution of genomics to the discovery of new antibiotics. Focus Biotechnol. 2001, 1, 23-31. Lehoux, D. E.; Levesque, R. C. Detection of genes essential in specific niches by signature-tagged mutagenesis. Curr. Opin. Biotechnol. 2000, 11, 434-439. Reich, K. A. The search for essential genes. Res. Microbiol. 2000, 151, 319-324. Gray, C. P.; Keck, W. Bacterial targets and antibiotics. Genome-based drug discovery. Cell. Mol. Life Sci. 1999, 56, 779-787. Chopra, I. Prospects for antisense agents in the therapy of bacterial infections. Expert Opin. Invest. Drugs 1999, 8, 1203-1208. Kolstoe, A.-B. Dynamic bacterial genome organization. Mol. Microbiol. 1997, 24, 241-248. Miklos, G. L. G.; Rubin, G. M. The role of the genome project in determining gene function: insights from model organisms. Cell 1996, 86, 521-529.
8. Lerner, C. G.; Beutel, B. A. Antibacterial drug discovery in the post-genomics era. Curr. Drug Targets: Infect. Disord. 2002, 2, 109-119. Chan, P. F.; Macarron, R.; Payne, D. J.; Zalacain, M.; Holmes, D. J. Novel antibacterials: a genomics approach to drug discovery. Curr. Drug Targets: Infect. Disord. 2002, 2, 291-308. Volker, C.; Brown, J. R. Bioinformatics and the discovery of novel anti-microbial targets. Curr. Drug Targets: Infect. Disord. 2002, 2, 279-290. Chalker, A. F.; Lunsford, R. D. Rational identification of new antibacterial drug targets that are essential for viability using a genomics-based approach. Pharmacol. Ther. 2002, 95, 1-20. Isaacson, R. E. Genomics and the prospects for the discovery of new targets for antibacterial and antifungal agents. Curr. Pharm. Des. 2002, 8, 1091-1098. McDevitt, D.; Rosenberg, M. Exploiting genomics to discover new antibiotics. Trends Microbiol. 2001, 9, 611-617. Payne, D. J.; Holmes, D. J.; Rosenberg, M. Delivering novel targets and antibiotics from genomics. Curr. Opin. Invest. Drugs 2001, 2, 1028-1034. Holmes, D. J.; Throup, J. P.; Wallis, N. G.; Burnham, M. K. R.; Zalacain, M.; Biswas, S.; Chalker, A. F.; Ingraham, K. A.; Marra, A.; Bryant, A.; Woodnutt, G.; Warren, P. V.; Brown, J. R.; Rosenberg, M. The contribution of genomics to the discovery of new antibiotics. Focus Biotechnol. 2001, 1, 23-31. Lehoux, D. E.; Levesque, R. C. Detection of genes essential in specific niches by signature-tagged mutagenesis. Curr. Opin. Biotechnol. 2000, 11, 434-439. Reich, K. A. The search for essential genes. Res. Microbiol. 2000, 151, 319-324. Gray, C. P.; Keck, W. Bacterial targets and antibiotics. Genome-based drug discovery. Cell. Mol. Life Sci. 1999, 56, 779-787. Chopra, I. Prospects for antisense agents in the therapy of bacterial infections. Expert Opin. Invest. Drugs 1999, 8, 1203-1208. Kolstoe, A.-B. Dynamic bacterial genome organization. Mol. Microbiol. 1997, 24, 241-248. Miklos, G. L. G.; Rubin, G. M. The role of the genome project in determining gene function: insights from model organisms. Cell 1996, 86, 521-529.
9. Lerner, C. G.; Beutel, B. A. Antibacterial drug discovery in the post-genomics era. Curr. Drug Targets: Infect. Disord. 2002, 2, 109-119. Chan, P. F.; Macarron, R.; Payne, D. J.; Zalacain, M.; Holmes, D. J. Novel antibacterials: a genomics approach to drug discovery. Curr. Drug Targets: Infect. Disord. 2002, 2, 291-308. Volker, C.; Brown, J. R. Bioinformatics and the discovery of novel anti-microbial targets. Curr. Drug Targets: Infect. Disord. 2002, 2, 279-290. Chalker, A. F.; Lunsford, R. D. Rational identification of new antibacterial drug targets that are essential for viability using a genomics-based approach. Pharmacol. Ther. 2002, 95, 1-20. Isaacson, R. E. Genomics and the prospects for the discovery of new targets for antibacterial and antifungal agents. Curr. Pharm. Des. 2002, 8, 1091-1098. McDevitt, D.; Rosenberg, M. Exploiting genomics to discover new antibiotics. Trends Microbiol. 2001, 9, 611-617. Payne, D. J.; Holmes, D. J.; Rosenberg, M. Delivering novel targets and antibiotics from genomics. Curr. Opin. Invest. Drugs 2001, 2, 1028-1034. Holmes, D. J.; Throup, J. P.; Wallis, N. G.; Burnham, M. K. R.; Zalacain, M.; Biswas, S.; Chalker, A. F.; Ingraham, K. A.; Marra, A.; Bryant, A.; Woodnutt, G.; Warren, P. V.; Brown, J. R.; Rosenberg, M. The contribution of genomics to the discovery of new antibiotics. Focus Biotechnol. 2001, 1, 23-31. Lehoux, D. E.; Levesque, R. C. Detection of genes essential in specific niches by signature-tagged mutagenesis. Curr. Opin. Biotechnol. 2000, 11, 434-439. Reich, K. A. The search for essential genes. Res. Microbiol. 2000, 151, 319-324. Gray, C. P.; Keck, W. Bacterial targets and antibiotics. Genome-based drug discovery. Cell. Mol. Life Sci. 1999, 56, 779-787. Chopra, I. Prospects for antisense agents in the therapy of bacterial infections. Expert Opin. Invest. Drugs 1999, 8, 1203-1208. Kolstoe, A.-B. Dynamic bacterial genome organization. Mol. Microbiol. 1997, 24, 241-248. Miklos, G. L. G.; Rubin, G. M. The role of the genome project in determining gene function: insights from model organisms. Cell 1996, 86, 521-529.
10. Lerner, C. G.; Beutel, B. A. Antibacterial drug discovery in the post-genomics era. Curr. Drug Targets: Infect. Disord. 2002, 2, 109-119. Chan, P. F.; Macarron, R.; Payne, D. J.; Zalacain, M.; Holmes, D. J. Novel antibacterials: a genomics approach to drug discovery. Curr. Drug Targets: Infect. Disord. 2002, 2, 291-308. Volker, C.; Brown, J. R. Bioinformatics and the discovery of novel anti-microbial targets. Curr. Drug Targets: Infect. Disord. 2002, 2, 279-290. Chalker, A. F.; Lunsford, R. D. Rational identification of new antibacterial drug targets that are essential for viability using a genomics-based approach. Pharmacol. Ther. 2002, 95, 1-20. Isaacson, R. E. Genomics and the prospects for the discovery of new targets for antibacterial and antifungal agents. Curr. Pharm. Des. 2002, 8, 1091-1098. McDevitt, D.; Rosenberg, M. Exploiting genomics to discover new antibiotics. Trends Microbiol. 2001, 9, 611-617. Payne, D. J.; Holmes, D. J.; Rosenberg, M. Delivering novel targets and antibiotics from genomics. Curr. Opin. Invest. Drugs 2001, 2, 1028-1034. Holmes, D. J.; Throup, J. P.; Wallis, N. G.; Burnham, M. K. R.; Zalacain, M.; Biswas, S.; Chalker, A. F.; Ingraham, K. A.; Marra, A.; Bryant, A.; Woodnutt, G.; Warren, P. V.; Brown, J. R.; Rosenberg, M. The contribution of genomics to the discovery of new antibiotics. Focus Biotechnol. 2001, 1, 23-31. Lehoux, D. E.; Levesque, R. C. Detection of genes essential in specific niches by signature-tagged mutagenesis. Curr. Opin. Biotechnol. 2000, 11, 434-439. Reich, K. A. The search for essential genes. Res. Microbiol. 2000, 151, 319-324. Gray, C. P.; Keck, W. Bacterial targets and antibiotics. Genome-based drug discovery. Cell. Mol. Life Sci. 1999, 56, 779-787. Chopra, I. Prospects for antisense agents in the therapy of bacterial infections. Expert Opin. Invest. Drugs 1999, 8, 1203-1208. Kolstoe, A.-B. Dynamic bacterial genome organization. Mol. Microbiol. 1997, 24, 241-248. Miklos, G. L. G.; Rubin, G. M. The role of the genome project in determining gene function: insights from model organisms. Cell 1996, 86, 521-529.
11. Lerner, C. G.; Beutel, B. A. Antibacterial drug discovery in the post-genomics era. Curr. Drug Targets: Infect. Disord. 2002, 2, 109-119. Chan, P. F.; Macarron, R.; Payne, D. J.; Zalacain, M.; Holmes, D. J. Novel antibacterials: a genomics approach to drug discovery. Curr. Drug Targets: Infect. Disord. 2002, 2, 291-308. Volker, C.; Brown, J. R. Bioinformatics and the discovery of novel anti-microbial targets. Curr. Drug Targets: Infect. Disord. 2002, 2, 279-290. Chalker, A. F.; Lunsford, R. D. Rational identification of new antibacterial drug targets that are essential for viability using a genomics-based approach. Pharmacol. Ther. 2002, 95, 1-20. Isaacson, R. E. Genomics and the prospects for the discovery of new targets for antibacterial and antifungal agents. Curr. Pharm. Des. 2002, 8, 1091-1098. McDevitt, D.; Rosenberg, M. Exploiting genomics to discover new antibiotics. Trends Microbiol. 2001, 9, 611-617. Payne, D. J.; Holmes, D. J.; Rosenberg, M. Delivering novel targets and antibiotics from genomics. Curr. Opin. Invest. Drugs 2001, 2, 1028-1034. Holmes, D. J.; Throup, J. P.; Wallis, N. G.; Burnham, M. K. R.; Zalacain, M.; Biswas, S.; Chalker, A. F.; Ingraham, K. A.; Marra, A.; Bryant, A.; Woodnutt, G.; Warren, P. V.; Brown, J. R.; Rosenberg, M. The contribution of genomics to the discovery of new antibiotics. Focus Biotechnol. 2001, 1, 23-31. Lehoux, D. E.; Levesque, R. C. Detection of genes essential in specific niches by signature-tagged mutagenesis. Curr. Opin. Biotechnol. 2000, 11, 434-439. Reich, K. A. The search for essential genes. Res. Microbiol. 2000, 151, 319-324. Gray, C. P.; Keck, W. Bacterial targets and antibiotics. Genome-based drug discovery. Cell. Mol. Life Sci. 1999, 56, 779-787. Chopra, I. Prospects for antisense agents in the therapy of bacterial infections. Expert Opin. Invest. Drugs 1999, 8, 1203-1208. Kolstoe, A.-B. Dynamic bacterial genome organization. Mol. Microbiol. 1997, 24, 241-248. Miklos, G. L. G.; Rubin, G. M. The role of the genome project in determining gene function: insights from model organisms. Cell 1996, 86, 521-529.
12. Lerner, C. G.; Beutel, B. A. Antibacterial drug discovery in the post-genomics era. Curr. Drug Targets: Infect. Disord. 2002, 2, 109-119. Chan, P. F.; Macarron, R.; Payne, D. J.; Zalacain, M.; Holmes, D. J. Novel antibacterials: a genomics approach to drug discovery. Curr. Drug Targets: Infect. Disord. 2002, 2, 291-308. Volker, C.; Brown, J. R. Bioinformatics and the discovery of novel anti-microbial targets. Curr. Drug Targets: Infect. Disord. 2002, 2, 279-290. Chalker, A. F.; Lunsford, R. D. Rational identification of new antibacterial drug targets that are essential for viability using a genomics-based approach. Pharmacol. Ther. 2002, 95, 1-20. Isaacson, R. E. Genomics and the prospects for the discovery of new targets for antibacterial and antifungal agents. Curr. Pharm. Des. 2002, 8, 1091-1098. McDevitt, D.; Rosenberg, M. Exploiting genomics to discover new antibiotics. Trends Microbiol. 2001, 9, 611-617. Payne, D. J.; Holmes, D. J.; Rosenberg, M. Delivering novel targets and antibiotics from genomics. Curr. Opin. Invest. Drugs 2001, 2, 1028-1034. Holmes, D. J.; Throup, J. P.; Wallis, N. G.; Burnham, M. K. R.; Zalacain, M.; Biswas, S.; Chalker, A. F.; Ingraham, K. A.; Marra, A.; Bryant, A.; Woodnutt, G.; Warren, P. V.; Brown, J. R.; Rosenberg, M. The contribution of genomics to the discovery of new antibiotics. Focus Biotechnol. 2001, 1, 23-31. Lehoux, D. E.; Levesque, R. C. Detection of genes essential in specific niches by signature-tagged mutagenesis. Curr. Opin. Biotechnol. 2000, 11, 434-439. Reich, K. A. The search for essential genes. Res. Microbiol. 2000, 151, 319-324. Gray, C. P.; Keck, W. Bacterial targets and antibiotics. Genome-based drug discovery. Cell. Mol. Life Sci. 1999, 56, 779-787. Chopra, I. Prospects for antisense agents in the therapy of bacterial infections. Expert Opin. Invest. Drugs 1999, 8, 1203-1208. Kolstoe, A.-B. Dynamic bacterial genome organization. Mol. Microbiol. 1997, 24, 241-248. Miklos, G. L. G.; Rubin, G. M. The role of the genome project in determining gene function: insights from model organisms. Cell 1996, 86, 521-529.
13. Lerner, C. G.; Beutel, B. A. Antibacterial drug discovery in the post-genomics era. Curr. Drug Targets: Infect. Disord. 2002, 2, 109-119. Chan, P. F.; Macarron, R.; Payne, D. J.; Zalacain, M.; Holmes, D. J. Novel antibacterials: a genomics approach to drug discovery. Curr. Drug Targets: Infect. Disord. 2002, 2, 291-308. Volker, C.; Brown, J. R. Bioinformatics and the discovery of novel anti-microbial targets. Curr. Drug Targets: Infect. Disord. 2002, 2, 279-290. Chalker, A. F.; Lunsford, R. D. Rational identification of new antibacterial drug targets that are essential for viability using a genomics-based approach. Pharmacol. Ther. 2002, 95, 1-20. Isaacson, R. E. Genomics and the prospects for the discovery of new targets for antibacterial and antifungal agents. Curr. Pharm. Des. 2002, 8, 1091-1098. McDevitt, D.; Rosenberg, M. Exploiting genomics to discover new antibiotics. Trends Microbiol. 2001, 9, 611-617. Payne, D. J.; Holmes, D. J.; Rosenberg, M. Delivering novel targets and antibiotics from genomics. Curr. Opin. Invest. Drugs 2001, 2, 1028-1034. Holmes, D. J.; Throup, J. P.; Wallis, N. G.; Burnham, M. K. R.; Zalacain, M.; Biswas, S.; Chalker, A. F.; Ingraham, K. A.; Marra, A.; Bryant, A.; Woodnutt, G.; Warren, P. V.; Brown, J. R.; Rosenberg, M. The contribution of genomics to the discovery of new antibiotics. Focus Biotechnol. 2001, 1, 23-31. Lehoux, D. E.; Levesque, R. C. Detection of genes essential in specific niches by signature-tagged mutagenesis. Curr. Opin. Biotechnol. 2000, 11, 434-439. Reich, K. A. The search for essential genes. Res. Microbiol. 2000, 151, 319-324. Gray, C. P.; Keck, W. Bacterial targets and antibiotics. Genome-based drug discovery. Cell. Mol. Life Sci. 1999, 56, 779-787. Chopra, I. Prospects for antisense agents in the therapy of bacterial infections. Expert Opin. Invest. Drugs 1999, 8, 1203-1208. Kolstoe, A.-B. Dynamic bacterial genome organization. Mol. Microbiol. 1997, 24, 241-248. Miklos, G. L. G.; Rubin, G. M. The role of the genome project in determining gene function: insights from model organisms. Cell 1996, 86, 521-529.
14. Lerner, C. G.; Beutel, B. A. Antibacterial drug discovery in the post-genomics era. Curr. Drug Targets: Infect. Disord. 2002, 2, 109-119. Chan, P. F.; Macarron, R.; Payne, D. J.; Zalacain, M.; Holmes, D. J. Novel antibacterials: a genomics approach to drug discovery. Curr. Drug Targets: Infect. Disord. 2002, 2, 291-308. Volker, C.; Brown, J. R. Bioinformatics and the discovery of novel anti-microbial targets. Curr. Drug Targets: Infect. Disord. 2002, 2, 279-290. Chalker, A. F.; Lunsford, R. D. Rational identification of new antibacterial drug targets that are essential for viability using a genomics-based approach. Pharmacol. Ther. 2002, 95, 1-20. Isaacson, R. E. Genomics and the prospects for the discovery of new targets for antibacterial and antifungal agents. Curr. Pharm. Des. 2002, 8, 1091-1098. McDevitt, D.; Rosenberg, M. Exploiting genomics to discover new antibiotics. Trends Microbiol. 2001, 9, 611-617. Payne, D. J.; Holmes, D. J.; Rosenberg, M. Delivering novel targets and antibiotics from genomics. Curr. Opin. Invest. Drugs 2001, 2, 1028-1034. Holmes, D. J.; Throup, J. P.; Wallis, N. G.; Burnham, M. K. R.; Zalacain, M.; Biswas, S.; Chalker, A. F.; Ingraham, K. A.; Marra, A.; Bryant, A.; Woodnutt, G.; Warren, P. V.; Brown, J. R.; Rosenberg, M. The contribution of genomics to the discovery of new antibiotics. Focus Biotechnol. 2001, 1, 23-31. Lehoux, D. E.; Levesque, R. C. Detection of genes essential in specific niches by signature-tagged mutagenesis. Curr. Opin. Biotechnol. 2000, 11, 434-439. Reich, K. A. The search for essential genes. Res. Microbiol. 2000, 151, 319-324. Gray, C. P.; Keck, W. Bacterial targets and antibiotics. Genome-based drug discovery. Cell. Mol. Life Sci. 1999, 56, 779-787. Chopra, I. Prospects for antisense agents in the therapy of bacterial infections. Expert Opin. Invest. Drugs 1999, 8, 1203-1208. Kolstoe, A.-B. Dynamic bacterial genome organization. Mol. Microbiol. 1997, 24, 241-248. Miklos, G. L. G.; Rubin, G. M. The role of the genome project in determining gene function: insights from model organisms. Cell 1996, 86, 521-529.
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