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Interrogation of the pathogen box reveals small molecule ligands against the mycobacterial trehalose transporter LpqY-SugABC
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Radhakrishnan, Anjana, Brown, Chelsea M., Guy, Collette S., Cooper, Charlotte, Pacheco-Gómez, Raúl, Stansfeld, Phillip J. and Fullam, Elizabeth (2022) Interrogation of the pathogen box reveals small molecule ligands against the mycobacterial trehalose transporter LpqY-SugABC. RSC Medicinal Chemistry . doi:10.1039/D2MD00104G ISSN 2632-8682. (In Press)
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Official URL: http://dx.doi.org/10.1039/D2MD00104G
Abstract
Tuberculosis, caused by Mycobacterium tuberculosis, claims ∼1.5 million lives annually. Effective chemotherapy is essential to control TB, however the emergence of drug-resistant strains of TB have seriously threatened global attempts to control and eradicate this deadly pathogen. Trehalose recycling via the LpqY-SugABC importer is essential for the virulence and survival of Mtb and inhibiting or hijacking this transport system is an attractive approach for the development of novel anti-tubercular and diagnostic agents. Therefore, we interrogated the drug-like compounds in the open-source Medicines for Malaria Pathogen Box and successfully identified seven compounds from the TB, kinetoplastids and reference compound disease sets that recognise LpqY. The molecules have diverse chemical scaffolds, are not specific trehalose analogues, and may be used as novel templates to facilitate the development of therapeutics that kill Mtb with a novel mechanism of action via the mycobacterial trehalose LpqY-SugABC transport system.
| Item Type: | Journal Article | |||||||||||||||||||||||||||||||||
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| Subjects: | Q Science > QD Chemistry R Medicine > RS Pharmacy and materia medica |
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| Divisions: | Faculty of Science, Engineering and Medicine > Science > Chemistry Faculty of Science, Engineering and Medicine > Science > Life Sciences (2010- ) Faculty of Science, Engineering and Medicine > Science > Chemistry > Computational and Theoretical Chemistry Centre |
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| Library of Congress Subject Headings (LCSH): | Antitubercular agents, Tuberculosis -- Treatment, Mycobacterium tuberculosis, Mycobacterial diseases | |||||||||||||||||||||||||||||||||
| Journal or Publication Title: | RSC Medicinal Chemistry | |||||||||||||||||||||||||||||||||
| Publisher: | Royal Society of Chemistry | |||||||||||||||||||||||||||||||||
| ISSN: | 2632-8682 | |||||||||||||||||||||||||||||||||
| Official Date: | 16 August 2022 | |||||||||||||||||||||||||||||||||
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| DOI: | 10.1039/D2MD00104G | |||||||||||||||||||||||||||||||||
| Status: | Peer Reviewed | |||||||||||||||||||||||||||||||||
| Publication Status: | In Press | |||||||||||||||||||||||||||||||||
| Access rights to Published version: | Open Access (Creative Commons) | |||||||||||||||||||||||||||||||||
| Date of first compliant deposit: | 17 August 2022 | |||||||||||||||||||||||||||||||||
| Date of first compliant Open Access: | 17 August 2022 | |||||||||||||||||||||||||||||||||
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