Ganfeborole
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Formula | C10H13BClNO4 |
Molar mass | 257.48 g·mol−1 |
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Ganfeborole (GSK3036656, GSK-070) is an experimental antibiotic which shows activity against Mycobacterium tuberculosis. It acts as a potent and selective inhibitor of the bacterial leucyl-tRNA synthetase enzyme, and is currently in clinical trials.[1][2][3]
References
[edit]- ^ Li X, Hernandez V, Rock FL, Choi W, Mak YS, Mohan M, et al. (October 2017). "Discovery of a Potent and Specific M. tuberculosis Leucyl-tRNA Synthetase Inhibitor: (S)-3-(Aminomethyl)-4-chloro-7-(2-hydroxyethoxy)benzo[c][1,2]oxaborol-1(3H)-ol (GSK656)". Journal of Medicinal Chemistry. 60 (19): 8011–8026. doi:10.1021/acs.jmedchem.7b00631. PMID 28953378.
- ^ Igarashi M, Ishizaki Y, Takahashi Y (November 2017). "New antituberculous drugs derived from natural products: current perspectives and issues in antituberculous drug development". The Journal of Antibiotics. 71: 15–25. doi:10.1038/ja.2017.126. PMID 29089593.
- ^ Diacon AH, Barry CE, Carlton A, Chen RY, Davies M, de Jager V, et al. (March 2024). "A first-in-class leucyl-tRNA synthetase inhibitor, ganfeborole, for rifampicin-susceptible tuberculosis: a phase 2a open-label, randomized trial". Nature Medicine. 30 (3): 896–904. doi:10.1038/s41591-024-02829-7. PMC 10957473. PMID 38365949.