ArticleAnalytical biochemistry2016
Fluorescence-based assay for polyprenyl phosphate-GlcNAc-1-phosphate transferase (WecA) and identification of novel antimycobacterial WecA inhibitors.
Article in Analytical biochemistry, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 19 papers.
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19 citing papers in PubMed, 29 citations in OpenAlex.
- Over-expression, purification, and kinetic analysis ofJournal of enzyme inhibition and medicinal chemistry · 2026Article
- New Insights of Muraymycin A1 and Its Analogs as DPAGT1 Inhibitors.Bioorganic chemistry · 2026Article
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- Emerging Extracellular Molecular Targets for Innovative Pharmacological Approaches to Resistant Mtb Infection.Biomolecules · 2023Review
- Concise Synthesis of Tunicamycin V and Discovery of a Cytostatic DPAGT1 Inhibitor.Angewandte Chemie (International ed. in English) · 2022Article
- OvercomingActa pharmaceutica Sinica. B · 2022Review
- Antibiotics and resistance: the two-sided coin of the mycobacterial cell wall.Cell surface (Amsterdam, Netherlands) · 2020Review
- Application of Mycobacterium smegmatis as a surrogate to evaluate drug leads against Mycobacterium tuberculosis.The Journal of antibiotics · 2020Article
- DPAGT1 Inhibitors of Capuramycin Analogues and Their Antimigratory Activities of Solid Tumors.Journal of medicinal chemistry · 2020Article
- Substrate Tolerance of Bacterial Glycosyltransferase MurG: Novel Fluorescence-Based Assays.ACS infectious diseases · 2020Article
- Liposidomycin, the first reported nucleoside antibiotic inhibitor of peptidoglycan biosynthesis translocase I: The discovery of liposidomycin and related compounds with a perspective on their application to new antibiotics.The Journal of antibiotics · 2019Review
- Structure-based drug discovery by targetingFuture medicinal chemistry · 2019Article
- A practical synthesis of a novel DPAGT1 inhibitor, aminouridyl phenoxypiperidinbenzyl butanamide (APPB) for in vivo studies.MethodsX · 2019Article
- Novel FR-900493 Analogues That Inhibit the Outgrowth ofACS omega · 2018Article
- Mycobacterial cell wall biosynthesis: a multifaceted antibiotic target.Parasitology · 2018Review
- Inhibition ofJournal of molecular pharmaceutics & organic process research · 2018Article
- Article
- Bacterial phosphoglycosyl transferases: initiators of glycan biosynthesis at the membrane interface.Glycobiology · 2017Review
- Stereocontrolled Total Synthesis of Muraymycin D1 Having a Dual Mode of Action against Mycobacterium tuberculosis.Journal of the American Chemical Society · 2016Article
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8 authors at 3 institutions in 2 countries.
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Abstract
Polyprenyl phosphate-GlcNAc-1-phosphate transferase (WecA) is an essential enzyme for the growth of Mycobacterium tuberculosis (Mtb) and some other bacteria. Mtb WecA catalyzes the transformation from UDP-GlcNAc to decaprenyl-P-P-GlcNAc, the first membrane-anchored glycophospholipid that is responsible for the biosynthesis of mycolylarabinogalactan in Mtb. Inhibition of WecA will block the entire biosynthesis of essential cell wall components of Mtb in both replicating and non-replicating states, making this enzyme a target for development of novel drugs. Here, we report a fluorescence-based method for the assay of WecA using a modified UDP-GlcNAc, UDP-Glucosamine-C6-FITC (1), a membrane fraction prepared from an M. smegmatis strain, and the E. coli B21WecA. Under the optimized conditions, UDP-Glucosamine-C6-FITC (1) can be converted to the corresponding decaprenyl-P-P-Glucosamine-C6-FITC (3) in 61.5% yield. Decaprenyl-P-P-Glucosamine-C6-FITC is readily extracted with n-butanol and can be quantified by ultraviolet-visible (UV-vis) spectrometry. Screening of the compound libraries designed for bacterial phosphotransferases resulted in the discovery of a selective WecA inhibitor, UT-01320 (12) that kills both replicating and non-replicating Mtb at low concentration. UT-01320 (12) also kills the intracellular Mtb in macrophages. We conclude that the WecA assay reported here is amenable to medium- and high-throughput screening, thus facilitating the discovery of novel WecA inhibitors.
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