ArticleThe Journal of biological chemistry2014
High throughput screen identifies small molecule inhibitors specific for Mycobacterium tuberculosis phosphoserine phosphatase.
Article in The Journal of biological chemistry, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 20 papers.
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Who cites it
20 citing papers in PubMed, 34 citations in OpenAlex.
- Emerging therapeutic drug targets in amino acid and protein biosynthesis pathways against ESKAPE and non-ESKAPE pathogens: a comprehensive review.Archives of microbiology · 2026Review
- Molecular insights into the functional mechanism of phosphoserine phosphatase SerB2 inFrontiers in microbiology · 2026Article
- Small Molecule Inhibitors ofInternational journal of molecular sciences · 2024Article
- Identification of Small Molecule Inhibitors Targeting Phosphoserine Phosphatase: A Novel Target for the Development of Antiamoebic Drugs.ACS omega · 2024Article
- Amino Acid Biosynthesis Inhibitors in Tuberculosis Drug Discovery.Pharmaceutics · 2024Review
- Improving enzyme functional annotation by integrating in vitro and in silico approaches: The example of histidinol phosphate phosphatases.Protein science : a publication of the Protein Society · 2024Article
- Pharmacophore mapping, 3D QSAR, molecular docking, and ADME prediction studies of novel Benzothiazinone derivatives.In silico pharmacology · 2024Article
- A morpheein equilibrium regulates catalysis in phosphoserine phosphatase SerB2 from Mycobacterium tuberculosis.Communications biology · 2023Article
- Identification of small molecules targeting homoserine acetyl transferase from Mycobacterium tuberculosis and Staphylococcus aureus.Scientific reports · 2022Article
- In silico functional and structural characterization revealed virulent proteins ofMolecular biology research communications · 2022Article
- Insights on recent approaches in drug discovery strategies and untapped drug targets against drug resistance.Future journal of pharmaceutical sciences · 2021Review
- L-serine synthesis via the phosphorylated pathway in humans.Cellular and molecular life sciences : CMLS · 2020Review
- Covalent Complex of DNA and Bacterial Topoisomerase: Implications in Antibacterial Drug Development.ChemMedChem · 2020Article
- Identification and Repurposing of Trisubstituted Harmine Derivatives as Novel Inhibitors ofMolecules (Basel, Switzerland) · 2020Article
- Rv2577 ofFrontiers in microbiology · 2020Article
- Comprehensive analysis of protein acetyltransferases of human pathogen Mycobacterium tuberculosis.Bioscience reports · 2019Article
- Targeting the Serine Pathway: A Promising Approach against Tuberculosis?Pharmaceuticals (Basel, Switzerland) · 2019Article
- Bacterial Virulence Factors: Secreted for Survival.Indian journal of microbiology · 2017Review
- The M. tuberculosis HAD phosphatase (Rv3042c) interacts with host proteins and is inhibited by Clofazimine.Cellular and molecular life sciences : CMLS · 2016Article
- Establishing Virulence Associated Polyphosphate Kinase 2 as a drug target for Mycobacterium tuberculosis.Scientific reports · 2016Article
Corrections and comments
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Authors and funding
7 authors at 4 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
The emergence of drug-resistant strains of Mycobacterium tuberculosis makes identification and validation of newer drug targets a global priority. Phosphoserine phosphatase (PSP), a key essential metabolic enzyme involved in conversion of O-phospho-l-serine to l-serine, was characterized in this study. The M. tuberculosis genome harbors all enzymes involved in l-serine biosynthesis including two PSP homologs: Rv0505c (SerB1) and Rv3042c (SerB2). In the present study, we have biochemically characterized SerB2 enzyme and developed malachite green-based high throughput assay system to identify SerB2 inhibitors. We have identified 10 compounds that were structurally different from known PSP inhibitors, and few of these scaffolds were highly specific in their ability to inhibit SerB2 enzyme, were noncytotoxic against mammalian cell lines, and inhibited M. tuberculosis growth in vitro. Surface plasmon resonance experiments demonstrated the relative binding for these inhibitors. The two best hits identified in our screen, clorobiocin and rosaniline, were bactericidal in activity and killed intracellular bacteria in a dose-dependent manner. We have also identified amino acid residues critical for these SerB2-small molecule interactions. This is the first study where we validate that M. tuberculosis SerB2 is a druggable and suitable target to pursue for further high throughput assay system screening.
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