The DOI matches its Crossref record; 26 of the 26 references it cites were found in a registry or an index.
Identification of Novel Inhibitors of M. tuberculosis Growth Using Whole Cell Based High-Throughput Screening
Open accessAbstract
Despite the urgent need for new antitubercular drugs, few are on the horizon. To combat the problem of emerging drug resistance, structurally unique chemical entities that inhibit new targets will be required. Here we describe our investigations using whole cell screening of a diverse collection of small molecules as a methodology for identifying novel inhibitors that target new pathways for Mycobacterium tuberculosis drug discovery. We find that conducting primary screens using model mycobacterial species may limit the potential for identifying new inhibitors with efficacy against M. tuberculosis. In addition, we confirm the importance of developing in vitro assay conditions that are reflective of in vivo biology for maximizing the proportion of hits from whole cell screening that are likely to have activity in vivo. Finally, we describe the identification and characterization of two novel inhibitors that target steps in M. tuberculosis cell wall biosynthesis. The first is a novel benzimidazole that targets mycobacterial membrane protein large 3 (MmpL3), a proposed transporter for cell wall mycolic acids. The second is a nitro-triazole that inhibits decaprenylphosphoryl-β-D-ribose 2'-epimerase (DprE1), an epimerase required for cell wall biosynthesis. These proteins are both among the small number of new targets that have been identified by forward chemical genetics using resistance generation coupled with genome sequencing. This suggests that methodologies currently employed for screening and target identification may lead to a bias in target discovery and that alternative methods should be explored.
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Cites
A Diarylquinoline Drug Active on the ATP Synthase of Mycobacterium tuberculosis
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PA-824 Kills Nonreplicating Mycobacterium tuberculosis by Intracellular NO Release
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Self-citationBreeding latitude drives individual schedules in a trans-hemispheric migrant bird
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Inhibition of mycolic acid transport across the Mycobacterium tuberculosis plasma membrane
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Cited by
Advances in the development of new tuberculosis drugs and treatment regimens
Zumla, A., Nahid, P., & Cole, S. T. (2013) · Nature Reviews Drug Discovery · doi:10.1038/nrd4001 · Cited by 893
The Mycobacterial Cell Wall—Peptidoglycan and Arabinogalactan
Alderwick, L. J., Harrison, J., Lloyd, G. S., & Birch, H. L. (2015) · Cold Spring Harbor Perspectives in Medicine · doi:10.1101/cshperspect.a021113 · Cited by 265
Crystal Structures of Membrane Transporter MmpL3, an Anti-TB Drug Target
Zhang, B., Li, J., Yang, X., Wu, L., Zhang, J., Yang, Y., Zhao, Y., Zhang, L., Yang, X., Yang, X., et al. (2019) · Cell · doi:10.1016/j.cell.2019.01.003 · Cited by 263
Self-citationStanley, S. A., Barczak, A. K., Silvis, M. R., Luo, S. S., Sogi, K., Vokes, M., Bray, M.-A., Carpenter, A. E., Moore, C. B., Siddiqi, N., et al. (2014) · PLoS Pathogens · doi:10.1371/journal.ppat.1003946 · Cited by 251
Self-citationLi, W., Upadhyay, A., Fontes, F. L., North, E. J., Wang, Y., Crans, D. C., Grzegorzewicz, A. E., Jones, V., Franzblau, S. G., Lee, R. E., et al. (2014) · Antimicrobial Agents and Chemotherapy · doi:10.1128/aac.03229-14 · Cited by 202
Metadata
- Authors
- Stanley, S. A., Grant, S. S., Kawate, T., Iwase, N., Shimizu, M., Wivagg, C., Silvis, M., Kazyanskaya, E., Aquadro, J., Golas, A., Fitzgerald, M., Dai, H., Zhang, L., & Hung, D. T.
- Venue
- ACS Chemical Biology
- Publisher
- American Chemical Society (ACS)
- Published
- 2012-05-21
- Volume
- 7
- Issue
- 8
- Pages
- 1377-1384
- ISSN
- 1554-8929 (ISSN-L)
- 1554-8937
- OpenAlex
- W1986288809
- Cited by
- 253
- References
- 26
- FWCI
- 18.01
- Type
- journal article
- Language
- en
- Open access
- green
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- Stanley, S. A., Grant, S. S., Kawate, T., Iwase, N., Shimizu, M., Wivagg, C., Silvis, M., Kazyanskaya, E., Aquadro, J., Golas, A., Fitzgerald, M., Dai, H., Zhang, L., & Hung, D. T. (2012). Identification of Novel Inhibitors of M. tuberculosis Growth Using Whole Cell Based High-Throughput Screening. ACS Chemical Biology. https://doi.org/10.1021/cb300151m
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