ArticleJournal of molecular medicine (Berlin, Germany)2019
Identification of novel scaffolds targeting Mycobacterium tuberculosis.
Article in Journal of molecular medicine (Berlin, Germany), 2019. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 12 papers.
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Who cites it
12 citing papers in PubMed, 33 citations in OpenAlex.
- Defining the Mechanism of Action and Resistance of NewACS chemical biology · 2026Article
- AveloMask, a novel breath aerosol collection kit for airborneJournal of clinical microbiology · 2025Article
- Selective inhibition of Mycobacterium tuberculosis GpsI unveils a novel strategy to target the RNA metabolism.Nucleic acids research · 2025Article
- Switching Residues: A Platform for the Synthesis of Fidaxomicin Antibiotics.Angewandte Chemie (International ed. in English) · 2025Article
- TheMicrobiology spectrum · 2024Article
- Molecular Mechanisms of MmpL3 Function and Inhibition.Microbial drug resistance (Larchmont, N.Y.) · 2023Review
- Identification of Small Molecule Inhibitors against Mycobacteria in Activated Macrophages.Molecules (Basel, Switzerland) · 2022Article
- Cryo-EM structure and resistance landscape of M. tuberculosis MmpL3: An emergent therapeutic target.Structure (London, England : 1993) · 2021Article
- Novel fidaxomicin antibiotics through site-selective catalysis.Communications chemistry · 2021Article
- Rifabutin Is Inactivated by Mycobacterium abscessus Arr.Antimicrobial agents and chemotherapy · 2021Article
- Spirocycle MmpL3 Inhibitors with Improved hERG and Cytotoxicity Profiles as Inhibitors ofACS omega · 2021Article
- MmpL3 Inhibition: A New Approach to Treat Nontuberculous Mycobacterial Infections.International journal of molecular sciences · 2020Review
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Authors and funding
7 authors at 2 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Drug resistance in Mycobacterium tuberculosis is relentlessly progressing while only a handful of novel drug candidates are developed. Here we describe a GFP-based high-throughput screening of 386,496 diverse compounds to identify putative tuberculosis drug candidates. In an exploratory analysis of the model organism M. bovis BCG and M. smegmatis and the subsequent screening of the main library, we identified 6354 compounds with anti-mycobacterial activity. These hit compounds were predominantly selective for mycobacteria while dozens had activity in the low μM range. We tested toxicity against the human monocyte/macrophage cell line THP-1 and elaborated activity against M. tuberculosis growing in liquid broth, under unique conditions such as non-replicating persistence or inhibition of M. tuberculosis residing in macrophages. Finally, spontaneous compound-resistant M. tuberculosis mutants were selected and subsequently analyzed by whole genome sequencing. In addition to compounds targeting the well-described proteins Pks13 and MmpL3, we identified two novel scaffolds targeting the bifunctional guanosine pentaphosphate synthetase/ polyribonucleotide nucleotidyltransferase GpsI, or interacting with the aminopeptidase PepB, a probable pro-drug activator. KEY MESSAGES: A newly identified scaffold targets the bifunctional enzyme GpsI. The aminopeptidase PepB is interacting with a second novel scaffold. Phenotypic screenings regularly identify novel compounds targeting Pks13 and MmpL3.
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